Asmaa Kassem - Academia.edu (original) (raw)

Papers by Asmaa Kassem

Molecules, Sep 3, 2022

This article is an open access article distributed under the terms and conditions of the Creative... more This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY

Materials Science and Engineering: B

Molecules

This study represents the design and synthesis of a new set of triazole-coumarin-glycosyl hybrids... more This study represents the design and synthesis of a new set of triazole-coumarin-glycosyl hybrids and their tetrazole hybrid analogues possessing various sugar moieties and modified analogues. All the newly synthesized derivatives were screened for their cytotoxic activities against a panel of human cancer cell lines. The coumarin derivatives 10, 13 and 15 derivatives revealed potent cytotoxic activities against Paca-2, Mel-501, PC-3 and A-375 cancer cell lines. These promising analogues were further examined for their inhibitory assessment against EGFR, VEGFR-2 and CDK-2/cyclin A2 kinases. The coumarin-tetrazole 10 displayed broad superior inhibitory activity against all screened enzymes compared with the reference drugs, erlotinib, sorafenib and roscovitine, respectively. The impact of coumarin-tetrazole 10 upon cell cycle and apoptosis induction was determined to detect its mechanism of action. Additionally, it upregulated the levels of casp-3, casp-7 and cytochrome-c proteins an...

In "Women and War in Roman Epic", Elina Pyy discusses the narrative and ideolog... more In "Women and War in Roman Epic", Elina Pyy discusses the narrative and ideological functions of gender in the works of Virgil, Lucan, Statius, Silius Italicus and Valerius Flaccus. By examining the themes of violence, death, guilt, grief, and anger in their epics, she offers an account of the intertextual tradition of the genre and its socio-political background. Through a combination of classical narratology and Julia Kristeva’s subjectivity theory, Pyy scrutinises how gendered marginality is constructed in the genre and how it contributes to the fashioning of Roman imperial identity. Focusing on the ambiguous elements of epic, the study looks beyond the binary oppositions between the Self and the Other, male and female, and Roman and barbarian.

Frankness, Greek Culture, and the Roman Empire, 2020

Frankness, Greek Culture, and the Roman Empire discusses the significance of parrhesia (free and ... more Frankness, Greek Culture, and the Roman Empire discusses the significance of parrhesia (free and frank speech) in Greek culture of the Roman empire. The term parrhesia first emerged in the context of the classical Athenian democracy and was long considered a key democratic and egalitarian value. And yet, references to frank speech pervade the literature of the Roman empire, a time when a single autocrat ruled over most of the known world, Greek cities were governed at the local level by entrenched oligarchies, and the social hierarchy was becoming increasingly stratified. This volume challenges the traditional view that the meaning of the term changed radically after Alexander the Great, and shows rather that parrhesia retained both political and ethical significance well into the Roman empire. By examining references to frankness in political writings, rhetoric, philosophy, historiography, biographical literature, and finally satire, the volume also explores the dynamics of political power in the Roman empire, where politics was located in interpersonal relationships as much as, if not more than, in institutions. The contested nature of the power relations in such interactionsbetween emperors and their advisors, between orators and the cities they counseled, and among fellow members of the oligarchic elite in provincial citiesreveals the political implications of a prominent post-classical intellectual development that reconceptualizes true freedom as belonging to the man who behavesand speaksfreely. At the same time, because the role of frank speaker is valorized, those who claim it also lay themselves open to suspicions of self-promotion and hypocrisy. This volume will be of interest to students and scholars of rhetoric and political thought in the ancient world, and to anyone interested in ongoing debates about intellectual freedom, limits on speech, and the advantages of presenting oneself as a truth-teller.

Arabian Journal of Chemistry, 2020

Modified Cotton fabrics with poly (3-(furan-2-carboamido) propionic acid) and poly (3-(furan-2-ca... more Modified Cotton fabrics with poly (3-(furan-2-carboamido) propionic acid) and poly (3-(furan-2-carboamido) propionic acid)/gelatin hydrogel for UV protection, antibacterial and electrical properties,

Physical Chemistry Chemical Physics, 2020

The kinetics methane activation (MgO+ + CH4) was studied experimentally and computationally by ru... more The kinetics methane activation (MgO+ + CH4) was studied experimentally and computationally by running and analyzing reactive atomistic simulations.

Journal of Heterocyclic Chemistry, 2019

With aiding of microwave radiation, new series of fused-thiazolopyrimidines and fused-triazolopyr... more With aiding of microwave radiation, new series of fused-thiazolopyrimidines and fused-triazolopyrimidines each with cycloheptane have been synthesized through the reaction of cycloheptane-thione with α-haloketones or hydrazonoyl chlorides in short-time intervals as well as high yield. Moreover, reaction of 2,7-bis(2-chlorobenzylidene)cycloheptan-1-one with o-aminothiophenol and heterocyclic amines afforded benzo[b]cyclohepta[e][1,4]thiazepine derivative and cycloheptapyrimidines fused with different azoles, respectively. The structure for all products was discussed and proved based on the results of spectral data and elemental analysis. Evaluation of the antimicrobial activity of selected products indicated that most of derivatives showed their potent activity exceeds the reference antibiotic in some cases.

Chemical and Pharmaceutical Bulletin, 2019

New sugar hydrazones incorporating furan and/or 1,3,4-thiadiazole ring systems were synthesized b... more New sugar hydrazones incorporating furan and/or 1,3,4-thiadiazole ring systems were synthesized by reaction of the corresponding hydrazide with different aldose sugars. Heterocyclization of the formed hydrazones afforded the derived acyclic nucleoside analogues possessing the 1,3,4-oxadiazoline as modified nucleobase via acetylation followed by the heterocyclization process. The anticancer activity of the synthesized compounds was studied against human liver carcinoma cell (HepG-2) and at human normal retina pigmented epithelium cells (RPE-1). High activities were revealed by compounds 3, 12 and 14 with IC 50 values near to that of the reference drug doxorubicin.

Journal of Enzyme Inhibition and Medicinal Chemistry, 2019

A series of N 1 ,N 3-bis (1-oxopropan-2-yl) isophthalamide-based derivatives 4-16 were prepared a... more A series of N 1 ,N 3-bis (1-oxopropan-2-yl) isophthalamide-based derivatives 4-16 were prepared and their structures were confirmed by different spectral tools. The cytotoxic potentiality of novel compounds 4-16 was assessed by the MTT assay method on colon, lung and breast tumour cell lines. Compound 5 gave the most significant specificity anticancer activity with safety response on normal cell lines. In vitro enzyme assay and several apoptotic parameters were examined to elucidate the mode of action of compound 5. Molecular docking studies also were simulated to put insight and give better understanding to its structural features.

Mini-Reviews in Medicinal Chemistry, 2020

Background & Objective:Quinazolines and their fused systems are noteworthy in pharmaceutical chem... more Background & Objective:Quinazolines and their fused systems are noteworthy in pharmaceutical chemistry due to their wide range of biological activities.Methods:A direct and efficient approach for the synthesis of new series of fused quinazolines with triazole, thiazole, benzimidazole and tetrazole has been preceded via the reaction of quinazoline thione derivative with halogenated compounds or cyclocondensation of arylidene of quinazoline derivative with heterocyclic amines. Also, dibenzo[b,e][1,4]thiazepine derivatives was synthesized through the reaction of 2,6-bis-(2-chloro-benzylidene)-cyclohexanone with o-aminothiophenol.Results:The structures of all new synthesized heterocyclic compounds were confirmed and discussed on the bases of spectral data. The utility of the preparation and design of the above mentioned compounds has been shown to be clear in the results of their antimicrobial activity which revealed that some derivatives have potent activity exceeding or similar to the...

European Journal of Medicinal Chemistry, 2019

A new series of 4-phenylcoumarin derivatives was synthesized starting from (2-oxo-4-phenyl-2H-chr... more A new series of 4-phenylcoumarin derivatives was synthesized starting from (2-oxo-4-phenyl-2H-chromen-7-yloxy) acetic acid hydrazide 3. Evaluation of the target compounds for their antiviral activity against hepatitis A virus revealed that the ethylthiosemicarbazide derivative 7b was the most potent virucidal agent (IC 50 =3.1µg/mL, TI = 83). The Schiff′s bases 14c and 14b demonstrated the highest virustatic effects against viral adsorption and replication, respectively (14c; IC 50 =8.5 µg/mL, TI = 88 and 14b; IC 50 =10.7µg/mL, TI = 91). Furthermore, compounds 7b, 14b and 14c were tested against HAV 3C protease and showed significant inhibition effects (Ki= 1.903, 0.104 and 0.217 µM, respectively). The remarkable inhibitory effect expressed by the three target compounds against HAV 3C protease prompted us to expand our research on HRV 3C protease, a structurally related enzyme of the same family, and interestingly, the three target compounds displayed significant inhibitory effect against HRV 3C protease (IC 50 = 16.10, 4.

Ancient Macedonians in Greek and Roman Sources, 2018

Bioorganic & Medicinal Chemistry, 2018

A new set of 4-phenylcoumarin derivatives was designed and synthesized aiming to introduce new tu... more A new set of 4-phenylcoumarin derivatives was designed and synthesized aiming to introduce new tubulin polymerization inhibitors as anti-breast cancer candidates. All the target compounds were evaluated for their cytotoxic effects against MCF-7 cell line, where compounds 2f, 3a, 3b, 3 f, 7a and 7b, showed higher cytotoxic effect (IC 50 =4.3-21.2 µg/mL) than the reference drug doxorubicin (IC 50 = 26.1 µg/mL), additionally, compounds 1 and 6b exhibited the same potency as doxorubicin (IC 50 = 25.2 and 28.0 µg/mL, respectively). The thiazolidinone derivatives 3a, 3b and 3 f with potent and selective anticancer effects towards MCF-7 cells (IC 50 = 11.1, 16.7 and 21.2 µg/mL) were further assessed for tubulin polymerization inhibition effects which showed that the three compounds were potent tubulin polymerization suppressors with IC 50 values of 9.37, 2.89 and 6.13 µM, respectively, compared to the reference drug colchicine (IC 50 = 6.93 µM). The mechanistic effects on cell cycle progression and induction of apoptosis in MCF-7 cells were determined for compound 3a due to its potent and selective cytotoxic effects 2 in addition to its promising tubulin polymerization inhibition potency. The results revealed that compound 3a induced cell cycle cessation at G2/M phase and accumulation of cells in pre-G1 phase and prevented its mitotic cycle, in addition to its activation of caspase-7 mediating apoptosis of MCF-7 cells. Molecular modeling studies for compounds 3a, 3b and 3 f were carried out on tubulin crystallography, the results indicated that the compounds showed binding mode similar to the co-crystalized ligand; colchicine. Moreover, pharmacophore constructed models and docking studies revealed that thiazolidinone, acetamide and coumarin moieties are crucial for the activity. Molecular dynamics (MD) studies were carried out for the three compounds over 100Ps. MD results of compound 3a showed that it reached the stable state after 30Ps which was in agreement with the calculated potential and kinetic energy of compound 3a.

This study explores the development of ancient festival culture in the Greek East of the Roman Em... more This study explores the development of ancient festival culture in the Greek East of the Roman Empire, paying particular attention to the fundamental religious changes that occurred. After analysing how Greek city festivals developed in the first two Imperial centuries, it concentrates on the major Roman festivals that were adopted in the Eastern cities and traces their history up to the time of Justinian and beyond. It addresses several key questions for the religious history of later antiquity: who were the actors behind these adoptions? How did the closed religious communities, Jews and pre-Constantinian Christians, articulate their resistance? How did these festivals change when the empire converted to Christianity? Why did emperors not yield to the long-standing pressure of the Church to abolish them? And finally, how did these very popular festivals - despite their pagan tradition - influence the form of the newly developed Christian liturgy?

Research on Chemical Intermediates, 2015

Abstract1,3-Thiazol derivatives have been synthesized via reaction of 1-(1-(5,6-dimethoxy-2-oxobe... more Abstract1,3-Thiazol derivatives have been synthesized via reaction of 1-(1-(5,6-dimethoxy-2-oxobenzo[d]thiazol-3(2H)-yl)propan-2-ylidene)-4-substituted thiosemicarbazide with different halides, namely, ethyl bromoacetate, ethyl-2-bromopropionate, phenacyl bromide, p-bromophenacyl bromide and/or substituted hydrazonoyl halides. The new compounds were evaluated as antimicrobial agents.

Book Review Greek City Walls of the Archaic Period, 900-480 BC By Rune Frederiksen (Oxford Monogr... more Book Review Greek City Walls of the Archaic Period, 900-480 BC By Rune Frederiksen (Oxford Monographs on Classical Archaeology). Pp. xxx + 238, figs. 114, tables 15, maps 4. Oxford University Press, Oxford 2011. $170. ISBN 978-0-19-957812-2 (cloth). 117.1 Claire Balandier This book, based on a Ph.D. thesis defended at the University of Copenhagen in 2004, is a most welcome addition to the archaeological studies of city walls. Frederiksen tries to fill a gap in the studies on fortifications of the Archaic period, since almost nothing has been published on this topic. However, this elegant volume only partly fills the lacuna. In fact, the material covered in the book is broader than its title. In the first half of the book, the author not only treats different aspects of fortification and city wall studies from the Iron Age to the Early Hellenistic period, he also devotes parts of the discussion to the relationship between poleis and city walls. The second half of the book is devoted to a catalogue of the fortified sites. After an introductory chapter (1-7) that summarizes the history of research on archaic walls, the second chapter inventories the different types of fortifications and raises the fundamental question of the relationship between polis and fortification. I prefer to use the Greek word "polis" instead of "city," since the latter's meaning is not the same in all languages. The English expression "city wall" itself raises a problem, and we should rather speak of "town walls" or "urban fortification" because these walls protected mainly the astu or urban center of a polis, or sometimes a secondary built-up area and even perioikoi agglomerations. The sixth chapter (62-9) discusses the dating of city walls-a crucial problem in studies of fortifications. The author argues

The Cambridge Ancient History

... expected. Gonville and Caius College, Cambridge RP DUNCAN-JONES THE FALL OF THE ROMAN REPUBLI... more ... expected. Gonville and Caius College, Cambridge RP DUNCAN-JONES THE FALL OF THE ROMAN REPUBLIC PA BRUNT: The Fall of the Roman Republic and Related Essays. Pp. xii + 545. Oxford: Clarendon Press, 1988. £60. ...

Neoplasma, 2009

Nitrogen mustards cis-1-methoxy-2-deoxy-2-[N,N-bis(2´-chloroethyl)amino]spirobrassinol (4) and tr... more Nitrogen mustards cis-1-methoxy-2-deoxy-2-[N,N-bis(2´-chloroethyl)amino]spirobrassinol (4) and trans-1-methoxy-2-deoxy-2-[N,N-bis(2´-chloroethyl)amino]spirobrassinol (5) derived from 1-methoxyspirobrassinol, an indole phytoalexin produced by the Japanese radish Raphanus sativus var. hortensis were designed as prospective dual-action compounds with DNA-alkylating effect and glutathione-depleting effects that may sensitize cancer cells to alkylating agents. Both new compounds demonstrated cytostatic/cytotoxic effects on various leukemia and ovarian cancer cell lines and dsDNA-destabilizing effects in vitro. Compound 4, the more promising of the two compounds, exerts earlier onset of anticancer effects on Jurkat cells via induction of apoptosis compared to the traditional alkylating anticancer agent melphalan. In addition, it demonstrated higher potency on ovarian cancer OVCAR-3 cell line and lower fold resistance between Jurkat and Jurkat-M cells selected for the resistance to melphalan. Therefore, compound 4 may be less affected by certain cancer drug resistance mechanisms than melphalan and it may become a prototype of a new class of anticancer active nitrogen mustards that combine DNA-damaging and DNA-damage-sensitizing properties.

Molecules, Sep 3, 2022

This article is an open access article distributed under the terms and conditions of the Creative... more This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY

Materials Science and Engineering: B

Molecules

This study represents the design and synthesis of a new set of triazole-coumarin-glycosyl hybrids... more This study represents the design and synthesis of a new set of triazole-coumarin-glycosyl hybrids and their tetrazole hybrid analogues possessing various sugar moieties and modified analogues. All the newly synthesized derivatives were screened for their cytotoxic activities against a panel of human cancer cell lines. The coumarin derivatives 10, 13 and 15 derivatives revealed potent cytotoxic activities against Paca-2, Mel-501, PC-3 and A-375 cancer cell lines. These promising analogues were further examined for their inhibitory assessment against EGFR, VEGFR-2 and CDK-2/cyclin A2 kinases. The coumarin-tetrazole 10 displayed broad superior inhibitory activity against all screened enzymes compared with the reference drugs, erlotinib, sorafenib and roscovitine, respectively. The impact of coumarin-tetrazole 10 upon cell cycle and apoptosis induction was determined to detect its mechanism of action. Additionally, it upregulated the levels of casp-3, casp-7 and cytochrome-c proteins an...

In "Women and War in Roman Epic", Elina Pyy discusses the narrative and ideolog... more In "Women and War in Roman Epic", Elina Pyy discusses the narrative and ideological functions of gender in the works of Virgil, Lucan, Statius, Silius Italicus and Valerius Flaccus. By examining the themes of violence, death, guilt, grief, and anger in their epics, she offers an account of the intertextual tradition of the genre and its socio-political background. Through a combination of classical narratology and Julia Kristeva’s subjectivity theory, Pyy scrutinises how gendered marginality is constructed in the genre and how it contributes to the fashioning of Roman imperial identity. Focusing on the ambiguous elements of epic, the study looks beyond the binary oppositions between the Self and the Other, male and female, and Roman and barbarian.

Frankness, Greek Culture, and the Roman Empire, 2020

Frankness, Greek Culture, and the Roman Empire discusses the significance of parrhesia (free and ... more Frankness, Greek Culture, and the Roman Empire discusses the significance of parrhesia (free and frank speech) in Greek culture of the Roman empire. The term parrhesia first emerged in the context of the classical Athenian democracy and was long considered a key democratic and egalitarian value. And yet, references to frank speech pervade the literature of the Roman empire, a time when a single autocrat ruled over most of the known world, Greek cities were governed at the local level by entrenched oligarchies, and the social hierarchy was becoming increasingly stratified. This volume challenges the traditional view that the meaning of the term changed radically after Alexander the Great, and shows rather that parrhesia retained both political and ethical significance well into the Roman empire. By examining references to frankness in political writings, rhetoric, philosophy, historiography, biographical literature, and finally satire, the volume also explores the dynamics of political power in the Roman empire, where politics was located in interpersonal relationships as much as, if not more than, in institutions. The contested nature of the power relations in such interactionsbetween emperors and their advisors, between orators and the cities they counseled, and among fellow members of the oligarchic elite in provincial citiesreveals the political implications of a prominent post-classical intellectual development that reconceptualizes true freedom as belonging to the man who behavesand speaksfreely. At the same time, because the role of frank speaker is valorized, those who claim it also lay themselves open to suspicions of self-promotion and hypocrisy. This volume will be of interest to students and scholars of rhetoric and political thought in the ancient world, and to anyone interested in ongoing debates about intellectual freedom, limits on speech, and the advantages of presenting oneself as a truth-teller.

Arabian Journal of Chemistry, 2020

Modified Cotton fabrics with poly (3-(furan-2-carboamido) propionic acid) and poly (3-(furan-2-ca... more Modified Cotton fabrics with poly (3-(furan-2-carboamido) propionic acid) and poly (3-(furan-2-carboamido) propionic acid)/gelatin hydrogel for UV protection, antibacterial and electrical properties,

Physical Chemistry Chemical Physics, 2020

The kinetics methane activation (MgO+ + CH4) was studied experimentally and computationally by ru... more The kinetics methane activation (MgO+ + CH4) was studied experimentally and computationally by running and analyzing reactive atomistic simulations.

Journal of Heterocyclic Chemistry, 2019

With aiding of microwave radiation, new series of fused-thiazolopyrimidines and fused-triazolopyr... more With aiding of microwave radiation, new series of fused-thiazolopyrimidines and fused-triazolopyrimidines each with cycloheptane have been synthesized through the reaction of cycloheptane-thione with α-haloketones or hydrazonoyl chlorides in short-time intervals as well as high yield. Moreover, reaction of 2,7-bis(2-chlorobenzylidene)cycloheptan-1-one with o-aminothiophenol and heterocyclic amines afforded benzo[b]cyclohepta[e][1,4]thiazepine derivative and cycloheptapyrimidines fused with different azoles, respectively. The structure for all products was discussed and proved based on the results of spectral data and elemental analysis. Evaluation of the antimicrobial activity of selected products indicated that most of derivatives showed their potent activity exceeds the reference antibiotic in some cases.

Chemical and Pharmaceutical Bulletin, 2019

New sugar hydrazones incorporating furan and/or 1,3,4-thiadiazole ring systems were synthesized b... more New sugar hydrazones incorporating furan and/or 1,3,4-thiadiazole ring systems were synthesized by reaction of the corresponding hydrazide with different aldose sugars. Heterocyclization of the formed hydrazones afforded the derived acyclic nucleoside analogues possessing the 1,3,4-oxadiazoline as modified nucleobase via acetylation followed by the heterocyclization process. The anticancer activity of the synthesized compounds was studied against human liver carcinoma cell (HepG-2) and at human normal retina pigmented epithelium cells (RPE-1). High activities were revealed by compounds 3, 12 and 14 with IC 50 values near to that of the reference drug doxorubicin.

Journal of Enzyme Inhibition and Medicinal Chemistry, 2019

A series of N 1 ,N 3-bis (1-oxopropan-2-yl) isophthalamide-based derivatives 4-16 were prepared a... more A series of N 1 ,N 3-bis (1-oxopropan-2-yl) isophthalamide-based derivatives 4-16 were prepared and their structures were confirmed by different spectral tools. The cytotoxic potentiality of novel compounds 4-16 was assessed by the MTT assay method on colon, lung and breast tumour cell lines. Compound 5 gave the most significant specificity anticancer activity with safety response on normal cell lines. In vitro enzyme assay and several apoptotic parameters were examined to elucidate the mode of action of compound 5. Molecular docking studies also were simulated to put insight and give better understanding to its structural features.

Mini-Reviews in Medicinal Chemistry, 2020

Background & Objective:Quinazolines and their fused systems are noteworthy in pharmaceutical chem... more Background & Objective:Quinazolines and their fused systems are noteworthy in pharmaceutical chemistry due to their wide range of biological activities.Methods:A direct and efficient approach for the synthesis of new series of fused quinazolines with triazole, thiazole, benzimidazole and tetrazole has been preceded via the reaction of quinazoline thione derivative with halogenated compounds or cyclocondensation of arylidene of quinazoline derivative with heterocyclic amines. Also, dibenzo[b,e][1,4]thiazepine derivatives was synthesized through the reaction of 2,6-bis-(2-chloro-benzylidene)-cyclohexanone with o-aminothiophenol.Results:The structures of all new synthesized heterocyclic compounds were confirmed and discussed on the bases of spectral data. The utility of the preparation and design of the above mentioned compounds has been shown to be clear in the results of their antimicrobial activity which revealed that some derivatives have potent activity exceeding or similar to the...

European Journal of Medicinal Chemistry, 2019

A new series of 4-phenylcoumarin derivatives was synthesized starting from (2-oxo-4-phenyl-2H-chr... more A new series of 4-phenylcoumarin derivatives was synthesized starting from (2-oxo-4-phenyl-2H-chromen-7-yloxy) acetic acid hydrazide 3. Evaluation of the target compounds for their antiviral activity against hepatitis A virus revealed that the ethylthiosemicarbazide derivative 7b was the most potent virucidal agent (IC 50 =3.1µg/mL, TI = 83). The Schiff′s bases 14c and 14b demonstrated the highest virustatic effects against viral adsorption and replication, respectively (14c; IC 50 =8.5 µg/mL, TI = 88 and 14b; IC 50 =10.7µg/mL, TI = 91). Furthermore, compounds 7b, 14b and 14c were tested against HAV 3C protease and showed significant inhibition effects (Ki= 1.903, 0.104 and 0.217 µM, respectively). The remarkable inhibitory effect expressed by the three target compounds against HAV 3C protease prompted us to expand our research on HRV 3C protease, a structurally related enzyme of the same family, and interestingly, the three target compounds displayed significant inhibitory effect against HRV 3C protease (IC 50 = 16.10, 4.

Ancient Macedonians in Greek and Roman Sources, 2018

Bioorganic & Medicinal Chemistry, 2018

A new set of 4-phenylcoumarin derivatives was designed and synthesized aiming to introduce new tu... more A new set of 4-phenylcoumarin derivatives was designed and synthesized aiming to introduce new tubulin polymerization inhibitors as anti-breast cancer candidates. All the target compounds were evaluated for their cytotoxic effects against MCF-7 cell line, where compounds 2f, 3a, 3b, 3 f, 7a and 7b, showed higher cytotoxic effect (IC 50 =4.3-21.2 µg/mL) than the reference drug doxorubicin (IC 50 = 26.1 µg/mL), additionally, compounds 1 and 6b exhibited the same potency as doxorubicin (IC 50 = 25.2 and 28.0 µg/mL, respectively). The thiazolidinone derivatives 3a, 3b and 3 f with potent and selective anticancer effects towards MCF-7 cells (IC 50 = 11.1, 16.7 and 21.2 µg/mL) were further assessed for tubulin polymerization inhibition effects which showed that the three compounds were potent tubulin polymerization suppressors with IC 50 values of 9.37, 2.89 and 6.13 µM, respectively, compared to the reference drug colchicine (IC 50 = 6.93 µM). The mechanistic effects on cell cycle progression and induction of apoptosis in MCF-7 cells were determined for compound 3a due to its potent and selective cytotoxic effects 2 in addition to its promising tubulin polymerization inhibition potency. The results revealed that compound 3a induced cell cycle cessation at G2/M phase and accumulation of cells in pre-G1 phase and prevented its mitotic cycle, in addition to its activation of caspase-7 mediating apoptosis of MCF-7 cells. Molecular modeling studies for compounds 3a, 3b and 3 f were carried out on tubulin crystallography, the results indicated that the compounds showed binding mode similar to the co-crystalized ligand; colchicine. Moreover, pharmacophore constructed models and docking studies revealed that thiazolidinone, acetamide and coumarin moieties are crucial for the activity. Molecular dynamics (MD) studies were carried out for the three compounds over 100Ps. MD results of compound 3a showed that it reached the stable state after 30Ps which was in agreement with the calculated potential and kinetic energy of compound 3a.

This study explores the development of ancient festival culture in the Greek East of the Roman Em... more This study explores the development of ancient festival culture in the Greek East of the Roman Empire, paying particular attention to the fundamental religious changes that occurred. After analysing how Greek city festivals developed in the first two Imperial centuries, it concentrates on the major Roman festivals that were adopted in the Eastern cities and traces their history up to the time of Justinian and beyond. It addresses several key questions for the religious history of later antiquity: who were the actors behind these adoptions? How did the closed religious communities, Jews and pre-Constantinian Christians, articulate their resistance? How did these festivals change when the empire converted to Christianity? Why did emperors not yield to the long-standing pressure of the Church to abolish them? And finally, how did these very popular festivals - despite their pagan tradition - influence the form of the newly developed Christian liturgy?

Research on Chemical Intermediates, 2015

Abstract1,3-Thiazol derivatives have been synthesized via reaction of 1-(1-(5,6-dimethoxy-2-oxobe... more Abstract1,3-Thiazol derivatives have been synthesized via reaction of 1-(1-(5,6-dimethoxy-2-oxobenzo[d]thiazol-3(2H)-yl)propan-2-ylidene)-4-substituted thiosemicarbazide with different halides, namely, ethyl bromoacetate, ethyl-2-bromopropionate, phenacyl bromide, p-bromophenacyl bromide and/or substituted hydrazonoyl halides. The new compounds were evaluated as antimicrobial agents.

Book Review Greek City Walls of the Archaic Period, 900-480 BC By Rune Frederiksen (Oxford Monogr... more Book Review Greek City Walls of the Archaic Period, 900-480 BC By Rune Frederiksen (Oxford Monographs on Classical Archaeology). Pp. xxx + 238, figs. 114, tables 15, maps 4. Oxford University Press, Oxford 2011. $170. ISBN 978-0-19-957812-2 (cloth). 117.1 Claire Balandier This book, based on a Ph.D. thesis defended at the University of Copenhagen in 2004, is a most welcome addition to the archaeological studies of city walls. Frederiksen tries to fill a gap in the studies on fortifications of the Archaic period, since almost nothing has been published on this topic. However, this elegant volume only partly fills the lacuna. In fact, the material covered in the book is broader than its title. In the first half of the book, the author not only treats different aspects of fortification and city wall studies from the Iron Age to the Early Hellenistic period, he also devotes parts of the discussion to the relationship between poleis and city walls. The second half of the book is devoted to a catalogue of the fortified sites. After an introductory chapter (1-7) that summarizes the history of research on archaic walls, the second chapter inventories the different types of fortifications and raises the fundamental question of the relationship between polis and fortification. I prefer to use the Greek word "polis" instead of "city," since the latter's meaning is not the same in all languages. The English expression "city wall" itself raises a problem, and we should rather speak of "town walls" or "urban fortification" because these walls protected mainly the astu or urban center of a polis, or sometimes a secondary built-up area and even perioikoi agglomerations. The sixth chapter (62-9) discusses the dating of city walls-a crucial problem in studies of fortifications. The author argues

The Cambridge Ancient History

... expected. Gonville and Caius College, Cambridge RP DUNCAN-JONES THE FALL OF THE ROMAN REPUBLI... more ... expected. Gonville and Caius College, Cambridge RP DUNCAN-JONES THE FALL OF THE ROMAN REPUBLIC PA BRUNT: The Fall of the Roman Republic and Related Essays. Pp. xii + 545. Oxford: Clarendon Press, 1988. £60. ...

Neoplasma, 2009

Nitrogen mustards cis-1-methoxy-2-deoxy-2-[N,N-bis(2´-chloroethyl)amino]spirobrassinol (4) and tr... more Nitrogen mustards cis-1-methoxy-2-deoxy-2-[N,N-bis(2´-chloroethyl)amino]spirobrassinol (4) and trans-1-methoxy-2-deoxy-2-[N,N-bis(2´-chloroethyl)amino]spirobrassinol (5) derived from 1-methoxyspirobrassinol, an indole phytoalexin produced by the Japanese radish Raphanus sativus var. hortensis were designed as prospective dual-action compounds with DNA-alkylating effect and glutathione-depleting effects that may sensitize cancer cells to alkylating agents. Both new compounds demonstrated cytostatic/cytotoxic effects on various leukemia and ovarian cancer cell lines and dsDNA-destabilizing effects in vitro. Compound 4, the more promising of the two compounds, exerts earlier onset of anticancer effects on Jurkat cells via induction of apoptosis compared to the traditional alkylating anticancer agent melphalan. In addition, it demonstrated higher potency on ovarian cancer OVCAR-3 cell line and lower fold resistance between Jurkat and Jurkat-M cells selected for the resistance to melphalan. Therefore, compound 4 may be less affected by certain cancer drug resistance mechanisms than melphalan and it may become a prototype of a new class of anticancer active nitrogen mustards that combine DNA-damaging and DNA-damage-sensitizing properties.