Beena Negi | Gargi College, University of Delhi (original) (raw)
Papers by Beena Negi
IJC-B Vol.60B(03) [March 2021], Mar 1, 2021
Over the past decade, a variety of benzothiazole derivatives have been reported with promising an... more Over the past decade, a variety of benzothiazole derivatives have been reported with promising anticancer activity. Benzothiazole and its analogues are capable of acting on a number of molecular targets and thus exerting their anticancer activity. To further develop benzothiazole derivatives as anticancer agents, we attempted to design and synthesize a library of benzothiazole-triazole derivatives. The synthesized hybrid compounds have been selected by National Cancer Institute, USA for the in vitro activity evaluation against 60 human cancer cell lines in a one dose screening panel. Most of the synthesized compounds showed 60-80% growth rate against renal cancer cell line UO-31.
Indian Journal of Chemistry -Section B (IJC-B), Mar 16, 2021
Table S1. Anticancer activity i.e. one-dose data for Benzothiazole-triazole hybrids retrieved fro... more Table S1. Anticancer activity i.e. one-dose data for Benzothiazole-triazole hybrids retrieved from NCI database Cell Line Mean Growth percent (4a) (5a) (5b) (4b) (4c) (4d) (5c) (5d) (5e) (5f) Leukemia CCRF-CEM
Bioorganic & Medicinal Chemistry Letters, 2013
Bioorganic & Medicinal Chemistry Letters, 2009
The Ear,Nose and Throat (ENT) senior house officer (SHO) position is a training post, and it is e... more The Ear,Nose and Throat (ENT) senior house officer (SHO) position is a training post, and it is expected that the SHO will become proficient in various procedures during a sixmonth ENT post 1 and ultimately by the end of basic surgical training (see http://www.entuk.org/career_ advice). These 'index' procedures include grommet insertion, adenoidectomy and tonsillectomy. Anecdotally, it is felt that current ENT SHOs are not performing as many procedures as previously, with consequent negative effects on training. One of the reasons for this may be the creation of NHS diagnostic and treatment centres (DTCs) and independent sector treatment centres (ISTCs), purely elective hospitals, which take patients from the waiting lists of standard NHS hospitals.
Archiv der Pharmazie, 2012
Mycobacterium tuberculosis is responsible for a large number of deaths worldwide. This bacterium ... more Mycobacterium tuberculosis is responsible for a large number of deaths worldwide. This bacterium is a matter of great concern as it has developed resistance against most of the anti-TB drugs available today. A series of new cyclohexane-1,2-diamine derivatives was synthesized and evaluated for their anti-tubercular activity against Mycobacterium tuberculosis H37Rv in vitro. These compounds were found to be moderate to weakly active. Two compounds showed significant activity with minimum inhibitory concentrations of 11.8 and 13.1 µM (Optical Density).
European Journal of Medicinal Chemistry, 2014
![Research paper thumbnail of Synthesis, antimalarial activity and cytotoxicity of substituted 3,6-diphenyl-[1,2,4,5]tetraoxanes](https://attachments.academia-assets.com/85101196/thumbnails/1.jpg)
](Bioorganic & Medicinal Chemistry, 2009
A series of 4-aminoquinoline-triazine conjugates with different substitution pattern have been sy... more A series of 4-aminoquinoline-triazine conjugates with different substitution pattern have been synthesized and evaluated for their in vitro antimalarial activity against chloroquine-sensitive and resistant strains of Plasmodium falciparum. Compounds 16, 19, 28 and 35 exhibited promising antimalarial activity against both strains of P. falciparum. Cytotoxicity of these compounds was tested against three cell lines. Several compounds did not show any cytotoxicity up to a high concentration (48 lM), others exhibited mild toxicities but selective index for antimalarial activity was high for most of these conjugates.
![Research paper thumbnail of Synthesis, antimalarial activity and cytotoxicity of substituted 3,6-diphenyl-[1,2,4,5]tetraoxanes](https://attachments.academia-assets.com/45701875/thumbnails/1.jpg)
](Bioorganic & Medicinal Chemistry, 2009
Substituted tetraoxanes with different substitution pattern on the aromatic ring were synthesized... more Substituted tetraoxanes with different substitution pattern on the aromatic ring were synthesized in order to explore the influence of different substituents in the antimalarial activity. Antimalarial activity of these compounds improves by the introduction of ethyl, iso-propyl or n-propyl groups in the aromatic ring but substitution with n-butyl or t-butyl leads decrease in antimalarial activity. Some of these compounds exhibit promising antimalarial activity. None of the compounds shows any toxicity against vero cells and three compounds (2a-2c) were tested against panel of six cell lines and none of these compounds showed any toxicity. X-ray crystal structure of compound 2w showed that tetraoxane ring is in the chair conformation with both the phenyl rings in the equatorial position. In addition, FeCl 3 mediated O-O bond scission of tetraoxanes (2a-2c) was also examined.
Current Research in Green and Sustainable Chemistry
Current protein & peptide science, Jan 24, 2016
Marine resources provide a large number of peptides with distinct biological activities. Several ... more Marine resources provide a large number of peptides with distinct biological activities. Several marine peptides exhibiting potent anticancer activity have been isolated from various marine life forms such as sponges, ascidians, mollusks, cyanobacteria, fungi, actinomycete, streptomyces etc. The marine peptides such as milnamide B, apratoxin, thiocoraline and apratoxin E isolated from marine organism have shown potent activity against various cancer cell lines. Among various potent peptides isolated from different marine organisms, dolastatin 10, didemnin B and aplidine have entered into clinical trials. The synthetic analogues of kahalalide F and dolastatin 10 namely, elisidepsin (PM02734) and D5 have also shown promising anticancer activities. The present review is aimed to identify and short list the potential anticancer peptides of marine origin and to discuss their in vitro, in vivo activity and their mechanism of action.
European journal of medicinal chemistry, Jan 13, 2018
A series of 22 novel metronidazole-triazole-styryl hybrids were synthesized and evaluated for the... more A series of 22 novel metronidazole-triazole-styryl hybrids were synthesized and evaluated for their in vitro antiamoebic activity against HM1: IMSS strain of Entamoeba histolytica. Some of the hybrids were found to be more active (IC = 0.12-0.35 μM) than the reference drug metronidazole (IC = 1.79 μM). The most active compounds were found to be non-toxic (up to 50 μM) against the Vero cells showing a good safety profile of these hybrids. The docking and ADMET studies were also conducted to investigate the probable mode of action. Docking studies showed significant binding affinity in the active site of E. histolytica thioredoxin reductase (EhTrR) protein.
European journal of medicinal chemistry, Jan 18, 2016
MRSA causes 60-70% of Staphylococcus aureus infection in hospitals and it has developed resistanc... more MRSA causes 60-70% of Staphylococcus aureus infection in hospitals and it has developed resistance against the currently available drugs. Interestingly, a series of 35 metronidazole-triazole hybrids on screening against MRSA were found to be active. Compound 22 was found to be effective at 4 μg/mL concentration against nine strains of MRSA. The inhibitory activity was further enhanced upto 1 μg/mL when this compound was used in combination with oxacillin in 1:1 ratio. All the compounds were found to be non-toxic in THP-1 cell line upto a concentration of 50 μM. The time-kill kinetics studies suggested bacteriostatic nature of the compounds. In silico studies show that these compounds interact with Thr600, Ser598, Asn464, His583 and Tyr446 in the active site of PBP2a crystal structure from MRSA.
Mycobacterium tuberculosis is responsible for a large number of deaths worldwide. This bacterium ... more Mycobacterium tuberculosis is responsible for a large number of deaths worldwide. This bacterium is a matter of great concern as it has developed resistance against most of the anti-TB drugs available today. A series of new cyclohexane-1,2-diamine derivatives was synthesized and evaluated for their anti-tubercular activity against Mycobacterium tuberculosis H37Rv in vitro. These compounds were found to be moderate to weakly active. Two compounds showed significant activity with minimum inhibitory concentrations of 11.8 and 13.1 µM (Optical Density).
Thymol and carvacrol are well known antioxidants found in the extract of the plants of thyme spec... more Thymol and carvacrol are well known antioxidants found in the extract of the plants of thyme species. The Schiff bases of 2-iso-propyl-5-methyl-phenol (thymol/1a), 2-tert-butyl-5-methyl-phenol (1b) and 5-iso-propyl-2-methyl-phenol (carvacrol/1c) exhibited much better antioxidant activity than thymol and carvacrol in DPPH assay. Ten compounds (4k, 4l, 4r, 5k, 5l, 5q, 5r, 6k, 6l and 6r) showed better or similar activity as compared to the reference compound ascorbic acid. Twenty-four most active compounds were also screened by ABTS method and showed 60–90% inhibition at 5 ug/mL concentration.
A library of unsymmetrical cyclohexane-1,2-diamine derivatives were synthesized and evaluated for... more A library of unsymmetrical cyclohexane-1,2-diamine derivatives were synthesized and evaluated for their activity against Mycobacterium tuberculosis H37Rv in vitro. Out of the 46 compounds synthesized,
eight compounds (11h, 13a, 13e, 13f, 14a, 14c, 14d, and 15d) were found to be active at or below 6.25 uM concentration, with negligible toxicity to human red blood cells at a concentration much higher than the MIC99. Compound 13a was the best active compound showing inhibition at 3.125–6.25 uM, and was found to be non-hemolytic up to 500 ug/mL concentration.
Tuberculosis (TB) is a serious health problem causing 1.5 million deaths worldwide. After the dis... more Tuberculosis (TB) is a serious health problem causing 1.5 million deaths worldwide. After the discovery of first-line anti-TB drugs, the mortality rate declined sharply, however, the emergence of drug-resistant strains and HIV co-infection have led to increased incidence of this disease. A number of new potential antitubercular drug candidates with novel modes of action have entered clinical trials in recent years. Compounds
such as gatifloxacin, moxifloxacin and linezolid, the already known antibiotics are currently being evaluated for their anti-TB activity. OPC-67683 and TMC207 have been approved for the treatment of MDR-TB patients recently, while PA-824, SQ109, PNU-100480, AZD5847, LL3858, SQ609, SQ641, BTZ043, DC-159a, CPZEN-45, Q-203, DNB1, TBA-354 are in various phases of clinical and preclinical developments. This review
evaluates the current status of TB drug development and future aspects.
![Research paper thumbnail of Synthesis, antimalarial activity and cytotoxicity of substituted 3,6-diphenyl-[1,2,4,5]tetraoxanes](https://attachments.academia-assets.com/46356267/thumbnails/1.jpg)
](Substituted tetraoxanes with different substitution pattern on the aromatic ring were synthesized... more Substituted tetraoxanes with different substitution pattern on the aromatic ring were synthesized in order to explore the influence of different substituents in the antimalarial activity. Antimalarial activity of these compounds improves by the introduction of ethyl, iso-propyl or n-propyl groups in the aromatic ring but substitution with n-butyl or t-butyl leads decrease in antimalarial activity. Some of these compounds exhibit promising antimalarial activity. None of the compounds shows any toxicity against vero cells and three compounds (2a–2c) were tested against panel of six cell lines and none of these compounds showed any toxicity. X-ray crystal structure of compound 2w showed that tetraoxane ring is in the chair conformation with both the phenyl rings in the equatorial position. In addition, FeCl 3 mediated O–O bond scission of tetraoxanes (2a–2c) was also examined.
Synthesis and antibacterial activity of metronidazole–triazole conjugates are reported. Total 21 ... more Synthesis and antibacterial activity of metronidazole–triazole conjugates are reported. Total 21 hybrid
compounds have been synthesized with different substitution pattern on the triazole ring in order to
study their influence on the antibacterial activity. These compounds demonstrated potent to weak antibacterial
activity against Gram-positive, and Gram-negative bacteria. Six compounds have shown equal
or better antibacterial activity against Gram-negative strains than the reference compound
IJC-B Vol.60B(03) [March 2021], Mar 1, 2021
Over the past decade, a variety of benzothiazole derivatives have been reported with promising an... more Over the past decade, a variety of benzothiazole derivatives have been reported with promising anticancer activity. Benzothiazole and its analogues are capable of acting on a number of molecular targets and thus exerting their anticancer activity. To further develop benzothiazole derivatives as anticancer agents, we attempted to design and synthesize a library of benzothiazole-triazole derivatives. The synthesized hybrid compounds have been selected by National Cancer Institute, USA for the in vitro activity evaluation against 60 human cancer cell lines in a one dose screening panel. Most of the synthesized compounds showed 60-80% growth rate against renal cancer cell line UO-31.
Indian Journal of Chemistry -Section B (IJC-B), Mar 16, 2021
Table S1. Anticancer activity i.e. one-dose data for Benzothiazole-triazole hybrids retrieved fro... more Table S1. Anticancer activity i.e. one-dose data for Benzothiazole-triazole hybrids retrieved from NCI database Cell Line Mean Growth percent (4a) (5a) (5b) (4b) (4c) (4d) (5c) (5d) (5e) (5f) Leukemia CCRF-CEM
Bioorganic & Medicinal Chemistry Letters, 2013
Bioorganic & Medicinal Chemistry Letters, 2009
The Ear,Nose and Throat (ENT) senior house officer (SHO) position is a training post, and it is e... more The Ear,Nose and Throat (ENT) senior house officer (SHO) position is a training post, and it is expected that the SHO will become proficient in various procedures during a sixmonth ENT post 1 and ultimately by the end of basic surgical training (see http://www.entuk.org/career_ advice). These 'index' procedures include grommet insertion, adenoidectomy and tonsillectomy. Anecdotally, it is felt that current ENT SHOs are not performing as many procedures as previously, with consequent negative effects on training. One of the reasons for this may be the creation of NHS diagnostic and treatment centres (DTCs) and independent sector treatment centres (ISTCs), purely elective hospitals, which take patients from the waiting lists of standard NHS hospitals.
Archiv der Pharmazie, 2012
Mycobacterium tuberculosis is responsible for a large number of deaths worldwide. This bacterium ... more Mycobacterium tuberculosis is responsible for a large number of deaths worldwide. This bacterium is a matter of great concern as it has developed resistance against most of the anti-TB drugs available today. A series of new cyclohexane-1,2-diamine derivatives was synthesized and evaluated for their anti-tubercular activity against Mycobacterium tuberculosis H37Rv in vitro. These compounds were found to be moderate to weakly active. Two compounds showed significant activity with minimum inhibitory concentrations of 11.8 and 13.1 µM (Optical Density).
European Journal of Medicinal Chemistry, 2014
Bioorganic & Medicinal Chemistry, 2009
A series of 4-aminoquinoline-triazine conjugates with different substitution pattern have been sy... more A series of 4-aminoquinoline-triazine conjugates with different substitution pattern have been synthesized and evaluated for their in vitro antimalarial activity against chloroquine-sensitive and resistant strains of Plasmodium falciparum. Compounds 16, 19, 28 and 35 exhibited promising antimalarial activity against both strains of P. falciparum. Cytotoxicity of these compounds was tested against three cell lines. Several compounds did not show any cytotoxicity up to a high concentration (48 lM), others exhibited mild toxicities but selective index for antimalarial activity was high for most of these conjugates.
Bioorganic & Medicinal Chemistry, 2009
Substituted tetraoxanes with different substitution pattern on the aromatic ring were synthesized... more Substituted tetraoxanes with different substitution pattern on the aromatic ring were synthesized in order to explore the influence of different substituents in the antimalarial activity. Antimalarial activity of these compounds improves by the introduction of ethyl, iso-propyl or n-propyl groups in the aromatic ring but substitution with n-butyl or t-butyl leads decrease in antimalarial activity. Some of these compounds exhibit promising antimalarial activity. None of the compounds shows any toxicity against vero cells and three compounds (2a-2c) were tested against panel of six cell lines and none of these compounds showed any toxicity. X-ray crystal structure of compound 2w showed that tetraoxane ring is in the chair conformation with both the phenyl rings in the equatorial position. In addition, FeCl 3 mediated O-O bond scission of tetraoxanes (2a-2c) was also examined.
Current Research in Green and Sustainable Chemistry
Current protein & peptide science, Jan 24, 2016
Marine resources provide a large number of peptides with distinct biological activities. Several ... more Marine resources provide a large number of peptides with distinct biological activities. Several marine peptides exhibiting potent anticancer activity have been isolated from various marine life forms such as sponges, ascidians, mollusks, cyanobacteria, fungi, actinomycete, streptomyces etc. The marine peptides such as milnamide B, apratoxin, thiocoraline and apratoxin E isolated from marine organism have shown potent activity against various cancer cell lines. Among various potent peptides isolated from different marine organisms, dolastatin 10, didemnin B and aplidine have entered into clinical trials. The synthetic analogues of kahalalide F and dolastatin 10 namely, elisidepsin (PM02734) and D5 have also shown promising anticancer activities. The present review is aimed to identify and short list the potential anticancer peptides of marine origin and to discuss their in vitro, in vivo activity and their mechanism of action.
European journal of medicinal chemistry, Jan 13, 2018
A series of 22 novel metronidazole-triazole-styryl hybrids were synthesized and evaluated for the... more A series of 22 novel metronidazole-triazole-styryl hybrids were synthesized and evaluated for their in vitro antiamoebic activity against HM1: IMSS strain of Entamoeba histolytica. Some of the hybrids were found to be more active (IC = 0.12-0.35 μM) than the reference drug metronidazole (IC = 1.79 μM). The most active compounds were found to be non-toxic (up to 50 μM) against the Vero cells showing a good safety profile of these hybrids. The docking and ADMET studies were also conducted to investigate the probable mode of action. Docking studies showed significant binding affinity in the active site of E. histolytica thioredoxin reductase (EhTrR) protein.
European journal of medicinal chemistry, Jan 18, 2016
MRSA causes 60-70% of Staphylococcus aureus infection in hospitals and it has developed resistanc... more MRSA causes 60-70% of Staphylococcus aureus infection in hospitals and it has developed resistance against the currently available drugs. Interestingly, a series of 35 metronidazole-triazole hybrids on screening against MRSA were found to be active. Compound 22 was found to be effective at 4 μg/mL concentration against nine strains of MRSA. The inhibitory activity was further enhanced upto 1 μg/mL when this compound was used in combination with oxacillin in 1:1 ratio. All the compounds were found to be non-toxic in THP-1 cell line upto a concentration of 50 μM. The time-kill kinetics studies suggested bacteriostatic nature of the compounds. In silico studies show that these compounds interact with Thr600, Ser598, Asn464, His583 and Tyr446 in the active site of PBP2a crystal structure from MRSA.
Mycobacterium tuberculosis is responsible for a large number of deaths worldwide. This bacterium ... more Mycobacterium tuberculosis is responsible for a large number of deaths worldwide. This bacterium is a matter of great concern as it has developed resistance against most of the anti-TB drugs available today. A series of new cyclohexane-1,2-diamine derivatives was synthesized and evaluated for their anti-tubercular activity against Mycobacterium tuberculosis H37Rv in vitro. These compounds were found to be moderate to weakly active. Two compounds showed significant activity with minimum inhibitory concentrations of 11.8 and 13.1 µM (Optical Density).
Thymol and carvacrol are well known antioxidants found in the extract of the plants of thyme spec... more Thymol and carvacrol are well known antioxidants found in the extract of the plants of thyme species. The Schiff bases of 2-iso-propyl-5-methyl-phenol (thymol/1a), 2-tert-butyl-5-methyl-phenol (1b) and 5-iso-propyl-2-methyl-phenol (carvacrol/1c) exhibited much better antioxidant activity than thymol and carvacrol in DPPH assay. Ten compounds (4k, 4l, 4r, 5k, 5l, 5q, 5r, 6k, 6l and 6r) showed better or similar activity as compared to the reference compound ascorbic acid. Twenty-four most active compounds were also screened by ABTS method and showed 60–90% inhibition at 5 ug/mL concentration.
A library of unsymmetrical cyclohexane-1,2-diamine derivatives were synthesized and evaluated for... more A library of unsymmetrical cyclohexane-1,2-diamine derivatives were synthesized and evaluated for their activity against Mycobacterium tuberculosis H37Rv in vitro. Out of the 46 compounds synthesized,
eight compounds (11h, 13a, 13e, 13f, 14a, 14c, 14d, and 15d) were found to be active at or below 6.25 uM concentration, with negligible toxicity to human red blood cells at a concentration much higher than the MIC99. Compound 13a was the best active compound showing inhibition at 3.125–6.25 uM, and was found to be non-hemolytic up to 500 ug/mL concentration.
Tuberculosis (TB) is a serious health problem causing 1.5 million deaths worldwide. After the dis... more Tuberculosis (TB) is a serious health problem causing 1.5 million deaths worldwide. After the discovery of first-line anti-TB drugs, the mortality rate declined sharply, however, the emergence of drug-resistant strains and HIV co-infection have led to increased incidence of this disease. A number of new potential antitubercular drug candidates with novel modes of action have entered clinical trials in recent years. Compounds
such as gatifloxacin, moxifloxacin and linezolid, the already known antibiotics are currently being evaluated for their anti-TB activity. OPC-67683 and TMC207 have been approved for the treatment of MDR-TB patients recently, while PA-824, SQ109, PNU-100480, AZD5847, LL3858, SQ609, SQ641, BTZ043, DC-159a, CPZEN-45, Q-203, DNB1, TBA-354 are in various phases of clinical and preclinical developments. This review
evaluates the current status of TB drug development and future aspects.
Substituted tetraoxanes with different substitution pattern on the aromatic ring were synthesized... more Substituted tetraoxanes with different substitution pattern on the aromatic ring were synthesized in order to explore the influence of different substituents in the antimalarial activity. Antimalarial activity of these compounds improves by the introduction of ethyl, iso-propyl or n-propyl groups in the aromatic ring but substitution with n-butyl or t-butyl leads decrease in antimalarial activity. Some of these compounds exhibit promising antimalarial activity. None of the compounds shows any toxicity against vero cells and three compounds (2a–2c) were tested against panel of six cell lines and none of these compounds showed any toxicity. X-ray crystal structure of compound 2w showed that tetraoxane ring is in the chair conformation with both the phenyl rings in the equatorial position. In addition, FeCl 3 mediated O–O bond scission of tetraoxanes (2a–2c) was also examined.
Synthesis and antibacterial activity of metronidazole–triazole conjugates are reported. Total 21 ... more Synthesis and antibacterial activity of metronidazole–triazole conjugates are reported. Total 21 hybrid
compounds have been synthesized with different substitution pattern on the triazole ring in order to
study their influence on the antibacterial activity. These compounds demonstrated potent to weak antibacterial
activity against Gram-positive, and Gram-negative bacteria. Six compounds have shown equal
or better antibacterial activity against Gram-negative strains than the reference compound