Vicky Jain | Marwadi Education Foundation (original) (raw)
Papers by Vicky Jain
AIMS Environmental Science
A study was carried to investigate by placing a side stream filter in a cooling tower to observe ... more A study was carried to investigate by placing a side stream filter in a cooling tower to observe the water conservation in the system. For any coal based power plant cycles of concentration plays important role for water conservation. The cycles of concentration in cooling tower was increased by installation of membrane system. The drain of the side stream filter was disposed to effluent treatment plant (ETP), while the filtered water will be recycled to the cooling tower inlet. The water parameter was measured by using various flow rates, pressure, and other factors. Significant water savings were demonstrated in the pilot. Maximum make-up water and outflow were both reduced by 14% and 48%, respectively. To save the most water, permeate recovery must be as high as possible. Water savings were minimal due to silica scaling on the membranes. Selected membranes are capable of lower total dissolved system (TDS) rejection than the 88% of total required membranes in the primary study, wh...
An entry from the Cambridge Structural Database, the world's repository for small molecule cr... more An entry from the Cambridge Structural Database, the world's repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available from the CCDC and typically includes 3D coordinates, cell parameters, space group, experimental conditions and quality measures.
An environment friendly synthesis of 1,4-dihydropyr idine derivatives was developed by one pot mu... more An environment friendly synthesis of 1,4-dihydropyr idine derivatives was developed by one pot multi component reaction of pyrazole aldehyde, EAA/MAA, 3-amino crotononitrile and Fe +3 montmorillonite clay K-10/ HY-zeolite under microwa ve irradiation in aqueous medium. The structures of all synthesized compounds were well characterize d by Mass, FT-IR, H NMR and elemental analysis.
Herein we have reported some new coumarinyl chalcones synthesized by conventional method as well ... more Herein we have reported some new coumarinyl chalcones synthesized by conventional method as well as microwave assisted method of synthesis. The reaction of 3-acetyl 4-hydroxy coumarin 2a-c with substituted 1, 3-diphenyl-1H-pyrazole-4-carbaldehyde 6a-h in the presence of piperidine as catalyst and chloroform as a solvent, yielded a series of chalcones 7a-x. The structures of all synthesized compounds are well characterized by Mass, FT-IR, 1 H NMR, 13 C NMR and elemental analysis. After obtaining experimental data regarding the yield and the time taken for the synthesis by both the methods, convenient and microwave assisted method, it was proved that the microwave assisted method is convenient for synthesis of this type of coumarinyl chalcones 7a-x.
Journal of Medicinal Chemistry, 2021
Designing hybrid molecules with dual functions is one approach to improve the therapeutic efficac... more Designing hybrid molecules with dual functions is one approach to improve the therapeutic efficacy of combination treatment. We have previously conjugated phthalazine and bis(hydroxymethyl)pyrrole pharmacophores to form hybrids bearing antiangiogenesis and DNA interstrand cross-linking activities. To improve the bioavailability, we adopted a benzology approach to design and synthesize a new series of 1,2-bis(hydroxymethyl)benzo[g]pyrrolo[2,1-a]phthalazines. These new hybrids retained the dual functions and could be formulated into vehicles for intravenous and oral administration. Among them, we demonstrated that compound 19a with dimethylamine at the C6 position markedly suppressed the tumor growth of human small cell lung cancer cell line H526, squamous lung cancer cell line H520, and renal cancer cell line 786-O in nude mice, implying that compound 19a is a broad-spectrum anticancer agent. Our results implicated that the conjugation of antiangiogenic and DNA cross-linking is likely to be a helpful approach to improving the efficacy of combination therapy.
Experimental and Molecular Therapeutics, 2019
Angiogenesis is a hallmark of cancer development, especially in lung cancer and colorectal cancer... more Angiogenesis is a hallmark of cancer development, especially in lung cancer and colorectal cancer. Unfortunately, the rapid development of resistance to anti-angiogenesis agents has limited the clinical benefits for the treatment. To improve the efficacy of anti-angiogenesis agents, we designed and synthesized a series of new hybrid molecules that are composed of benzophthalazine (anti-angiogenesis moiety) and bis(hydroxymethyl)pyrrole (DNA interstrand crosslinking moiety). We demonstrate that these compounds are the dual function inducing DNA crosslinking and anti-angiogenesis. 1,2-Bis(hydroxymethyl)benzopyrrolo[2,1- a ]phthalazine derivatives displayed potent cytotoxicity to leukemia and a batch of solid tumor cell lines. Among them, small cell lung cancer (SCLC) cells were the most susceptible cells with the IC 50 values ranged from dozens of nanomolar to submicromolar. Significantly, we observed total tumor remission by treatment of SCLC H526 (TP53 WT) xenografts with formulated compound 8 at the dose of 20mg/kg, 5 times/week for 2 weeks. In addition, compound 8 was also more potent than cisplatin in suppression of growth of SCLC H211 (TP53 mutant) xenografts. Combination treatment of H211 cells with compound 8 and cisplatin displayed the synergistically cell killing. Our preliminary results further showed that co-treatment of compound 8 and low dose cisplatin significantly suppressed tumor growth and prolonged the survival rate of mice bearing H211 xenografts. In contract to cisplatin, treatment of mice with compound 8 did not cause body weight lost, indicating low systematic toxicity of compound 8. In summary, our results indicate that bis(hydroxymethyl)benzopyrrolo[2,1- a ]phthalazine hybrids, either alone or in combination with other therapeutic drugs, are potent anticancer agents against SCLC and deserve for future development. Note: This abstract was not presented at the meeting. Citation Format: Tai-Lin Chen, Vicky Jain, Yi-Wen Lin, Tsann-Long Su, Te-Chang Lee. Development of1,2-bis(hydroxymethyl)benzo[g]pyrrolo[2,1-a]phthalazine hybrids as potent anticancer agents to small cell lung cancer [abstract]. In: Proceedings of the American Association for Cancer Research Annual Meeting 2019; 2019 Mar 29-Apr 3; Atlanta, GA. Philadelphia (PA): AACR; Cancer Res 2019;79(13 Suppl):Abstract nr 3852.
![Research paper thumbnail of Design and Synthesis of 1,2-Bis(hydroxymethyl)pyrrolo[2,1-a]phthalazine Hybrids as Potent Anticancer Agents that Inhibit Angiogenesis and Induce DNA Interstrand Cross-links](https://attachments.academia-assets.com/94140226/thumbnails/1.jpg)
](Journal of Medicinal Chemistry, 2019
Hybrid molecules are composed of two pharmacophores with different biological activities. Here, w... more Hybrid molecules are composed of two pharmacophores with different biological activities. Here, we conjugated phthalazine moieties (anti-angiogenetic pharmacophore) and bis(hydroxymethyl)pyrrole moieties (DNA crosslinking agent) to form a series of bis(hydroxymethyl)pyrrolo[2,1-a]phthalazine hybrids. These conjugates were cytotoxic to a variety of cancer cell lines by inducing DNA damage, arresting cell cycle progression at the G2/M phase, triggering apoptosis and inhibiting vascular endothelial growth factor receptor 2 (VEGFR-2) in endothelial cells. Among them, compound 29d encapsulated in a liposomal formulation (e.g., 29dL) significantly suppressed the growth of small cell lung cancer cell (H526) xenografts in mice. Based on immunohistochemical staining, the tumor xenografts in mice treated with 29dL showed time-dependent decreases in the intensity of CD31, a marker of blood vessels, whereas the intensity of -H2AX, a marker of DNA damage, increased. The present data revealed that the conjugation of anti-angiogenic and DNA-damaging agents can generate potential hybrid agents for cancer treatment.
Tetrahedron Letters, 2015
Abstract An unprecedent, efficient, and convenient lab-scale protocol for stable deuteration of M... more Abstract An unprecedent, efficient, and convenient lab-scale protocol for stable deuteration of Mesalamine, with mixed catalyst 10% Pd/C (10 wt %) and 10% Pt/C (25 wt %) at 145 °C, using D2O as deuterium source, in hydrogen atmosphere, is reported. The nature of reactive species with Pd/C–Pt/C–D2O–H2 system is suggested to be of electrophilic nature D+ type. Download : Download high-res image (59KB) Download : Download full-size image
Life
A library of 1,4-dihydropyridine-based 1,2,3-triazol derivatives has been designed, synthesized, ... more A library of 1,4-dihydropyridine-based 1,2,3-triazol derivatives has been designed, synthesized, and evaluated their cytotoxic potential on colorectal adenocarcinoma (Caco-2) cell lines. All compounds were characterized and identified based on their 1H and 13C NMR (Nuclear Magnetic Resonance) spectroscopic data. Furthermore, molecular docking of best anticancer hits with target proteins (protein kinase CK2α, tankyrase1, and tankyrase2) has been performed. Our results implicated that most of these compounds have significant antiproliferative activity with IC50 values between 0.63 ± 0.05 and 5.68 ± 0.14 µM. Moreover, the mechanism of action of most active compounds 13ab′ and 13ad′ suggested that they induce cell death through apoptosis in the late apoptotic phase as well as dead phase, and they could promote cell cycle arrest at the G2/M phase. Furthermore, the molecular docking study illustrated that 13ad′ possesses better binding interaction with the catalytic residues of target pro...
Molecular Cancer Therapeutics, 2019
Angiogenesis plays a critical role in sustaining the microenvironment, growth, and metastatic pot... more Angiogenesis plays a critical role in sustaining the microenvironment, growth, and metastatic potential of a variety of tumors, such as lung cancer, colorectal cancer, and renal cancer. However, the rapid development of resistance to anti-angiogenesis agents has limited the clinical benefits. To improve the therapeutic efficacy, the designed dual functional inhibitors, composed of benzophthalazine (anti-angiogenesis moiety) and bis(hydroxymethyl)pyrrole (DNA interstrand crosslinking moiety), were synthesized. We first demonstrated that 1,2-bis(hydroxymethyl)benzopyrrolo[2,1-a]phthalazines displayed dual functions, inducing DNA crosslinking and inhibiting angiogenesis. By aid of DIVAA, we confirmed the in vivo anti-angiogenetic activity. They were cytotoxic to a panel of cancer cell lines, including leukemia, colorectal, renal, and lung cancer cells. Among them, small cell lung cancer (SCLC) cells were the most susceptible cells with the IC50 values ranged from subnanomolar to microm...
Synthetic Communications, 2015
A practical, mild, and high-yielding synthetic approach for the synthesis of unknown tetrahydropy... more A practical, mild, and high-yielding synthetic approach for the synthesis of unknown tetrahydropyrimidinyl substituted 3-coumarins as hybrid scaffolds, potentially useful new chemical entities (NCEs), via metal-and catalyst-free multicomponent cyclization is described. The enhanced nucleophilicity of 3-amino coumarins versus 4-amino coumarin is explained via the difference in 13 C NMR δ values (Δδ) of vinylic carbons. X-ray crystal analysis defines the structure of a representative set of example.
Herein we report a tandem cyclization protocol towards hitherto unprepared hybrid scaffolds of co... more Herein we report a tandem cyclization protocol towards hitherto unprepared hybrid scaffolds of coumarin and imidazole core. The synthetic methodology initiates with linking of aromatic amines with coumarin at 4-position, followed by tandem cyclization with the help of nitromethane leading to the synthesis of title compounds in high to excellent yields (80-97%). Detailed characterization including 1 H NMR, 13 C NMR and HRMS for all newly synthesized compounds has been reported.
AIMS Environmental Science
A study was carried to investigate by placing a side stream filter in a cooling tower to observe ... more A study was carried to investigate by placing a side stream filter in a cooling tower to observe the water conservation in the system. For any coal based power plant cycles of concentration plays important role for water conservation. The cycles of concentration in cooling tower was increased by installation of membrane system. The drain of the side stream filter was disposed to effluent treatment plant (ETP), while the filtered water will be recycled to the cooling tower inlet. The water parameter was measured by using various flow rates, pressure, and other factors. Significant water savings were demonstrated in the pilot. Maximum make-up water and outflow were both reduced by 14% and 48%, respectively. To save the most water, permeate recovery must be as high as possible. Water savings were minimal due to silica scaling on the membranes. Selected membranes are capable of lower total dissolved system (TDS) rejection than the 88% of total required membranes in the primary study, wh...
An entry from the Cambridge Structural Database, the world's repository for small molecule cr... more An entry from the Cambridge Structural Database, the world's repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available from the CCDC and typically includes 3D coordinates, cell parameters, space group, experimental conditions and quality measures.
An environment friendly synthesis of 1,4-dihydropyr idine derivatives was developed by one pot mu... more An environment friendly synthesis of 1,4-dihydropyr idine derivatives was developed by one pot multi component reaction of pyrazole aldehyde, EAA/MAA, 3-amino crotononitrile and Fe +3 montmorillonite clay K-10/ HY-zeolite under microwa ve irradiation in aqueous medium. The structures of all synthesized compounds were well characterize d by Mass, FT-IR, H NMR and elemental analysis.
Herein we have reported some new coumarinyl chalcones synthesized by conventional method as well ... more Herein we have reported some new coumarinyl chalcones synthesized by conventional method as well as microwave assisted method of synthesis. The reaction of 3-acetyl 4-hydroxy coumarin 2a-c with substituted 1, 3-diphenyl-1H-pyrazole-4-carbaldehyde 6a-h in the presence of piperidine as catalyst and chloroform as a solvent, yielded a series of chalcones 7a-x. The structures of all synthesized compounds are well characterized by Mass, FT-IR, 1 H NMR, 13 C NMR and elemental analysis. After obtaining experimental data regarding the yield and the time taken for the synthesis by both the methods, convenient and microwave assisted method, it was proved that the microwave assisted method is convenient for synthesis of this type of coumarinyl chalcones 7a-x.
Journal of Medicinal Chemistry, 2021
Designing hybrid molecules with dual functions is one approach to improve the therapeutic efficac... more Designing hybrid molecules with dual functions is one approach to improve the therapeutic efficacy of combination treatment. We have previously conjugated phthalazine and bis(hydroxymethyl)pyrrole pharmacophores to form hybrids bearing antiangiogenesis and DNA interstrand cross-linking activities. To improve the bioavailability, we adopted a benzology approach to design and synthesize a new series of 1,2-bis(hydroxymethyl)benzo[g]pyrrolo[2,1-a]phthalazines. These new hybrids retained the dual functions and could be formulated into vehicles for intravenous and oral administration. Among them, we demonstrated that compound 19a with dimethylamine at the C6 position markedly suppressed the tumor growth of human small cell lung cancer cell line H526, squamous lung cancer cell line H520, and renal cancer cell line 786-O in nude mice, implying that compound 19a is a broad-spectrum anticancer agent. Our results implicated that the conjugation of antiangiogenic and DNA cross-linking is likely to be a helpful approach to improving the efficacy of combination therapy.
Experimental and Molecular Therapeutics, 2019
Angiogenesis is a hallmark of cancer development, especially in lung cancer and colorectal cancer... more Angiogenesis is a hallmark of cancer development, especially in lung cancer and colorectal cancer. Unfortunately, the rapid development of resistance to anti-angiogenesis agents has limited the clinical benefits for the treatment. To improve the efficacy of anti-angiogenesis agents, we designed and synthesized a series of new hybrid molecules that are composed of benzophthalazine (anti-angiogenesis moiety) and bis(hydroxymethyl)pyrrole (DNA interstrand crosslinking moiety). We demonstrate that these compounds are the dual function inducing DNA crosslinking and anti-angiogenesis. 1,2-Bis(hydroxymethyl)benzopyrrolo[2,1- a ]phthalazine derivatives displayed potent cytotoxicity to leukemia and a batch of solid tumor cell lines. Among them, small cell lung cancer (SCLC) cells were the most susceptible cells with the IC 50 values ranged from dozens of nanomolar to submicromolar. Significantly, we observed total tumor remission by treatment of SCLC H526 (TP53 WT) xenografts with formulated compound 8 at the dose of 20mg/kg, 5 times/week for 2 weeks. In addition, compound 8 was also more potent than cisplatin in suppression of growth of SCLC H211 (TP53 mutant) xenografts. Combination treatment of H211 cells with compound 8 and cisplatin displayed the synergistically cell killing. Our preliminary results further showed that co-treatment of compound 8 and low dose cisplatin significantly suppressed tumor growth and prolonged the survival rate of mice bearing H211 xenografts. In contract to cisplatin, treatment of mice with compound 8 did not cause body weight lost, indicating low systematic toxicity of compound 8. In summary, our results indicate that bis(hydroxymethyl)benzopyrrolo[2,1- a ]phthalazine hybrids, either alone or in combination with other therapeutic drugs, are potent anticancer agents against SCLC and deserve for future development. Note: This abstract was not presented at the meeting. Citation Format: Tai-Lin Chen, Vicky Jain, Yi-Wen Lin, Tsann-Long Su, Te-Chang Lee. Development of1,2-bis(hydroxymethyl)benzo[g]pyrrolo[2,1-a]phthalazine hybrids as potent anticancer agents to small cell lung cancer [abstract]. In: Proceedings of the American Association for Cancer Research Annual Meeting 2019; 2019 Mar 29-Apr 3; Atlanta, GA. Philadelphia (PA): AACR; Cancer Res 2019;79(13 Suppl):Abstract nr 3852.
Journal of Medicinal Chemistry, 2019
Hybrid molecules are composed of two pharmacophores with different biological activities. Here, w... more Hybrid molecules are composed of two pharmacophores with different biological activities. Here, we conjugated phthalazine moieties (anti-angiogenetic pharmacophore) and bis(hydroxymethyl)pyrrole moieties (DNA crosslinking agent) to form a series of bis(hydroxymethyl)pyrrolo[2,1-a]phthalazine hybrids. These conjugates were cytotoxic to a variety of cancer cell lines by inducing DNA damage, arresting cell cycle progression at the G2/M phase, triggering apoptosis and inhibiting vascular endothelial growth factor receptor 2 (VEGFR-2) in endothelial cells. Among them, compound 29d encapsulated in a liposomal formulation (e.g., 29dL) significantly suppressed the growth of small cell lung cancer cell (H526) xenografts in mice. Based on immunohistochemical staining, the tumor xenografts in mice treated with 29dL showed time-dependent decreases in the intensity of CD31, a marker of blood vessels, whereas the intensity of -H2AX, a marker of DNA damage, increased. The present data revealed that the conjugation of anti-angiogenic and DNA-damaging agents can generate potential hybrid agents for cancer treatment.
Tetrahedron Letters, 2015
Abstract An unprecedent, efficient, and convenient lab-scale protocol for stable deuteration of M... more Abstract An unprecedent, efficient, and convenient lab-scale protocol for stable deuteration of Mesalamine, with mixed catalyst 10% Pd/C (10 wt %) and 10% Pt/C (25 wt %) at 145 °C, using D2O as deuterium source, in hydrogen atmosphere, is reported. The nature of reactive species with Pd/C–Pt/C–D2O–H2 system is suggested to be of electrophilic nature D+ type. Download : Download high-res image (59KB) Download : Download full-size image
Life
A library of 1,4-dihydropyridine-based 1,2,3-triazol derivatives has been designed, synthesized, ... more A library of 1,4-dihydropyridine-based 1,2,3-triazol derivatives has been designed, synthesized, and evaluated their cytotoxic potential on colorectal adenocarcinoma (Caco-2) cell lines. All compounds were characterized and identified based on their 1H and 13C NMR (Nuclear Magnetic Resonance) spectroscopic data. Furthermore, molecular docking of best anticancer hits with target proteins (protein kinase CK2α, tankyrase1, and tankyrase2) has been performed. Our results implicated that most of these compounds have significant antiproliferative activity with IC50 values between 0.63 ± 0.05 and 5.68 ± 0.14 µM. Moreover, the mechanism of action of most active compounds 13ab′ and 13ad′ suggested that they induce cell death through apoptosis in the late apoptotic phase as well as dead phase, and they could promote cell cycle arrest at the G2/M phase. Furthermore, the molecular docking study illustrated that 13ad′ possesses better binding interaction with the catalytic residues of target pro...
Molecular Cancer Therapeutics, 2019
Angiogenesis plays a critical role in sustaining the microenvironment, growth, and metastatic pot... more Angiogenesis plays a critical role in sustaining the microenvironment, growth, and metastatic potential of a variety of tumors, such as lung cancer, colorectal cancer, and renal cancer. However, the rapid development of resistance to anti-angiogenesis agents has limited the clinical benefits. To improve the therapeutic efficacy, the designed dual functional inhibitors, composed of benzophthalazine (anti-angiogenesis moiety) and bis(hydroxymethyl)pyrrole (DNA interstrand crosslinking moiety), were synthesized. We first demonstrated that 1,2-bis(hydroxymethyl)benzopyrrolo[2,1-a]phthalazines displayed dual functions, inducing DNA crosslinking and inhibiting angiogenesis. By aid of DIVAA, we confirmed the in vivo anti-angiogenetic activity. They were cytotoxic to a panel of cancer cell lines, including leukemia, colorectal, renal, and lung cancer cells. Among them, small cell lung cancer (SCLC) cells were the most susceptible cells with the IC50 values ranged from subnanomolar to microm...
Synthetic Communications, 2015
A practical, mild, and high-yielding synthetic approach for the synthesis of unknown tetrahydropy... more A practical, mild, and high-yielding synthetic approach for the synthesis of unknown tetrahydropyrimidinyl substituted 3-coumarins as hybrid scaffolds, potentially useful new chemical entities (NCEs), via metal-and catalyst-free multicomponent cyclization is described. The enhanced nucleophilicity of 3-amino coumarins versus 4-amino coumarin is explained via the difference in 13 C NMR δ values (Δδ) of vinylic carbons. X-ray crystal analysis defines the structure of a representative set of example.
Herein we report a tandem cyclization protocol towards hitherto unprepared hybrid scaffolds of co... more Herein we report a tandem cyclization protocol towards hitherto unprepared hybrid scaffolds of coumarin and imidazole core. The synthetic methodology initiates with linking of aromatic amines with coumarin at 4-position, followed by tandem cyclization with the help of nitromethane leading to the synthesis of title compounds in high to excellent yields (80-97%). Detailed characterization including 1 H NMR, 13 C NMR and HRMS for all newly synthesized compounds has been reported.