Browsing by Author "Satyamoorthy, K."

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6-[3-(4-Fluorophenyl)-1H-pyrazol-4-yl]-3-[(2-naphthyloxy)methyl][1,2,4]triazolo[3,4-b][1,3,4]thiadiazole as a potent antioxidant and an anticancer agent induces growth inhibition followed by apoptosis in HepG2 cells
(2010) Sunil, D.; Isloor, A.M.; Shetty, P.; Satyamoorthy, K.; Bharath, Prasad, A.S.
In this paper we have investigated the in vitro antioxidant property of two triazolo-thiadiazoles, 6-[3-(4-fluorophenyl)-1H-pyrazol-4-yl]-3-[(2-naphthyloxy)methyl][1,2,4]triazolo[3,4-b][1,3,4]thiadiazole (FPNT) and 6-[3-(4-chlororophenyl)-1H-pyrazol-4-yl]-3-[(phenyloxy)methyl][1,2,4]triazolo[3,4-b][1,3,4]thiadiazole (CPPT) by spectrophotometric DPPH and ABTS radical scavenging methods as well as by lipid peroxide assay. The anticancer activity along with possible mechanism of action of triazolo-thiadiazoles in Hep G2 cells was explored using MTT assay, [3H] thymidine assay, flow cytometry and chromatin condensation studies. Both FPNT and CPPT exhibited a dose dependent cytotoxic effect on hepatocellular carcinoma cell line, HepG2. The IC50 value was very low for both the compounds when compared to standard drug, doxorubicin. Incorporation of [3H] thymidine in conjunction with cell cycle analysis suggested that FPNT inhibited the growth of HepG2 cells. Flow cytometric studies revealed more percentage of cells in sub-G1 phase, indicating apoptosis, which was further confirmed through chromatin condensation studies by Hoechst staining. FPNT was found to be a potent antioxidant when compared to the standard in DPPH, ABTS radical scavenging assays and lipid peroxidation studies. 2010 .
6-[3-(4-Fluorophenyl)-1H-pyrazol-4-yl]-3-[(2-naphthyloxy)methyl][1,2,4]triazolo[3,4-b][1,3,4]thiadiazole as a potent antioxidant and an anticancer agent induces growth inhibition followed by apoptosis in HepG2 cells
(2010) Dhanya, D.; Isloor, A.M.; Shetty, P.; Satyamoorthy, K.; Bharath Prasad, A.S.
In this paper we have investigated the in vitro antioxidant property of two triazolo-thiadiazoles, 6-[3-(4-fluorophenyl)-1H-pyrazol-4-yl]-3-[(2-naphthyloxy)methyl][1,2,4]triazolo[3,4-b][1,3,4]thiadiazole (FPNT) and 6-[3-(4-chlororophenyl)-1H-pyrazol-4-yl]-3-[(phenyloxy)methyl][1,2,4]triazolo[3,4-b][1,3,4]thiadiazole (CPPT) by spectrophotometric DPPH and ABTS radical scavenging methods as well as by lipid peroxide assay. The anticancer activity along with possible mechanism of action of triazolo-thiadiazoles in Hep G2 cells was explored using MTT assay, [3H] thymidine assay, flow cytometry and chromatin condensation studies. Both FPNT and CPPT exhibited a dose dependent cytotoxic effect on hepatocellular carcinoma cell line, HepG2. The IC50 value was very low for both the compounds when compared to standard drug, doxorubicin. Incorporation of [3H] thymidine in conjunction with cell cycle analysis suggested that FPNT inhibited the growth of HepG2 cells. Flow cytometric studies revealed more percentage of cells in sub-G1 phase, indicating apoptosis, which was further confirmed through chromatin condensation studies by Hoechst staining. FPNT was found to be a potent antioxidant when compared to the standard in DPPH, ABTS radical scavenging assays and lipid peroxidation studies. © 2010 .
Synthesis, characterization and in vitro cytotoxic properties of some new Schiff and Mannich bases in Hep G2 cells
(2011) Sunil, D.; Isloor, A.M.; Shetty, P.; Chandrakantha, B.; Satyamoorthy, K.
A series of 5-substituted-4-amino-3-mercapto- 1,2,4-triazoles were synthesized and were treated with various 3-substituted pyrazole aldehydes to obtain a series of new Schiff bases (3a-l). Few of the selected Schiff bases were converted into Mannich bases by reaction with diphenylamine/morpholine in presence of formaldehyde in ethanol media (4a-e, 5a-e). These newly synthesized compounds were characterized by elemental analysis, IR, NMR and mass spectrometry studies. A comparative study on the cytotoxic activities of few selected Schiff and Mannich bases was done in HepG2 cells using MTT assay. Few of the screened Schiff bases, 3a, 3d, 3e, 3g and 3h showed dose dependent cytotoxic activity, 3a being the most potent with an IC50 value of 0.018 g/l comparable to the standard drug doxorubicin. Among the Mannich bases, 5b was the most active with an IC50 value of 0.034 g/l. The Schiff bases were found to be more active, when compared to Mannich bases derived from them. The morpholine derived Mannich bases were more potent than those obtained from diphenyl amine. Springer Science+Business Media, LLC 2010.
Synthesis, characterization and in vitro cytotoxic properties of some new Schiff and Mannich bases in Hep G2 cells
(Birkhauser Boston, 2011) Dhanya, D.; Isloor, A.M.; Shetty, P.; Chandrakantha, B.; Satyamoorthy, K.
A series of 5-substituted-4-amino-3-mercapto- 1,2,4-triazoles were synthesized and were treated with various 3-substituted pyrazole aldehydes to obtain a series of new Schiff bases (3a-l). Few of the selected Schiff bases were converted into Mannich bases by reaction with diphenylamine/morpholine in presence of formaldehyde in ethanol media (4a-e, 5a-e). These newly synthesized compounds were characterized by elemental analysis, IR, NMR and mass spectrometry studies. A comparative study on the cytotoxic activities of few selected Schiff and Mannich bases was done in HepG2 cells using MTT assay. Few of the screened Schiff bases, 3a, 3d, 3e, 3g and 3h showed dose dependent cytotoxic activity, 3a being the most potent with an IC50 value of 0.018 g/l comparable to the standard drug doxorubicin. Among the Mannich bases, 5b was the most active with an IC50 value of 0.034 g/l. The Schiff bases were found to be more active, when compared to Mannich bases derived from them. The morpholine derived Mannich bases were more potent than those obtained from diphenyl amine. © Springer Science+Business Media, LLC 2010.
Synthesis, characterization, antioxidant, and anticancer studies of 6-[3-(4-chlorophenyl)-1H-pyrazol-4-yl]-3-[(2-naphthyloxy) methyl][1,2,4] triazolo[3,4-b][1,3,4]thiadiazole in HepG2 cell lines
(2011) Sunil, D.; Isloor, A.M.; Shetty, P.; Satyamoorthy, K.; Prasad, A.S.B.
Triazolo- thiadiazoles exhibit a variety of pharmacological properties, due to their cytotoxicity. In continuation of a previous study on triazolo-thiadiazoles, the authors have synthesized a new thiadiazole, 6-[3-(4-chlorophenyl)- 1-H-pyrazol-4-yl]-3-[(2-naphthyloxy)methyl] [1,2,4]triazolo[3,4-b][1,3,4]thiadiazole (CPNT), which was further characterized by advanced spectral techniques and elemental analysis. The compound exhibited a dose-dependent cytotoxic effect on hepatocellular carcinoma cell line, HepG2 with very low IC50 value of 0.8 ?g/ml in 24 h when compared with standard drug, doxorubicin. Incorporation of [3H] thymidine in conjunction with cell cycle analysis suggested that CPNT inhibited the growth of HepG2 cells. Flow cytometric studies revealed more percentage of cells in subG1 phase, indicating apoptosis, which was further confirmed through chromatin condensation studies by Hoechst staining. In vitro antioxidant activity of CPNT was determined by DPPH and ABTS free radical scavenging assays which revealed increasing scavenging activity with increasing concentration of the compound when compared with reference ascorbic acid. Springer Science+Business Media, LLC 2010.
Synthesis, characterization, antioxidant, and anticancer studies of 6-[3-(4-chlorophenyl)-1H-pyrazol-4-yl]-3-[(2-naphthyloxy) methyl][1,2,4] triazolo[3,4-b][1,3,4]thiadiazole in HepG2 cell lines
(2011) Dhanya, D.; Isloor, A.M.; Shetty, P.; Satyamoorthy, K.; Prasad, A.S.B.
Triazolo- thiadiazoles exhibit a variety of pharmacological properties, due to their cytotoxicity. In continuation of a previous study on triazolo-thiadiazoles, the authors have synthesized a new thiadiazole, 6-[3-(4-chlorophenyl)- 1-H-pyrazol-4-yl]-3-[(2-naphthyloxy)methyl] [1,2,4]triazolo[3,4-b][1,3,4]thiadiazole (CPNT), which was further characterized by advanced spectral techniques and elemental analysis. The compound exhibited a dose-dependent cytotoxic effect on hepatocellular carcinoma cell line, HepG2 with very low IC50 value of 0.8 ?g/ml in 24 h when compared with standard drug, doxorubicin. Incorporation of [3H] thymidine in conjunction with cell cycle analysis suggested that CPNT inhibited the growth of HepG2 cells. Flow cytometric studies revealed more percentage of cells in subG1 phase, indicating apoptosis, which was further confirmed through chromatin condensation studies by Hoechst staining. In vitro antioxidant activity of CPNT was determined by DPPH and ABTS free radical scavenging assays which revealed increasing scavenging activity with increasing concentration of the compound when compared with reference ascorbic acid. © Springer Science+Business Media, LLC 2010.