Faculty Publications

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Author: search.filters.author.Isloor, A.M.Subject: search.filters.subject.antioxidant activity

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    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.
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    Hantzsch reaction: Synthesis and characterization of some new 1,4-dihydropyridine derivatives as potent antimicrobial and antioxidant agents
    (2011) Vijesh, A.M.; Isloor, A.M.; Peethambar, S.K.; Shivananda, K.N.; Arulmoli, T.; Isloor, N.
    In the present study two new series of Hantzsch 1,4-dihydropyridine derivatives (1,4-DHPs) containing substituted pyrazole moiety (4a-f and 5a-f) were synthesized by the reaction of 3-aryl-1H-pyrazole-4-carbaldehydes with 1,3-dicarbonylcompounds (ethylacetoacetate and methylacetoacetate) and ammonium acetate. The newly synthesized compounds were characterized by IR, NMR, mass spectral study and also by C, H, N analyses. New compounds were screened for their antimicrobial activity by well plate method (zone of inhibition). Antioxidant studies of the synthesized compounds were also performed by measuring the DPPH radical scavenging assay. Compounds 4c, 4e and 4f were found to be potent antibacterial and antioxidant agents. The acute oral toxicity study for the compounds 4c, 4e and 4f were carried out and the experimental studies revealed that compounds 4c and 4e is safe up to 3000 mg/kg and no death of animals were recorded. However in compound 4f, we found mortality above 2000 mg and also significant behavioral changes in experimental animals. © 2011 Elsevier Masson SAS. All rights reserved.
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    Synthesis and evaluation of antioxidant, antimicrobial activities of new 2,4-disubstituted thiazoles
    (2012) Malladi, S.; Isloor, A.M.; Peethambar, S.K.; Shivananda, K.N.
    A new series of 2,4-disubstituted thiazole derivatives were synthesized by the reaction of various 3-aryl-1H-pyrazole-4- carbaldehyde thiosemicarbazones (2a-e) and phenacyl bromides. The compounds (3a-n) were characterized by IR, NMR, mass spectra and C, H, N analyses. All the synthesized compounds were screened for their antioxidant and antimicrobial activities. Antioxidant studies revealed that, compounds 3b, 3j and 3n showed significant scavenging activity whereas compounds 3e and 3n exhibited significant antimicrobial activity. The acute oral toxicity study for the compound 3e and 3n have revealed good safety profile till the uppermost dose (2000 mg/kg).
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    Synthesis, characterization, anticancer, and antioxidant activity of some new thiazolidin-4-ones in MCF-7 cells
    (2013) Isloor, A.M.; Dhanya, D.; Shetty, P.; Malladi, S.; Pai, K.S.R.; Maliyakkal, N.
    There are limited studies centring on the potential of thiazolidin-4-ones as anticancer agents. In this study, a new series of 2-(3-substituted-1H- pyrazol-4-yl)-3-(3-substituted-5-sulfanyl-1,2,4-triazol-4-yl)-1, 3-thiazolidin-4-one (4a-o) have been synthesized by cyclo-condensation reaction of 5-substituted-4-[(3-substituted-1H-pyrazol-4-ylmethylidene)amino]-2H-1,2,4- triazole-3-thione (3a-o) and thioglycolic acid. The structures of all the synthesized compounds were confirmed by elemental analysis, spectral techniques like IR, 1H NMR, and mass spectroscopy. Few compounds exhibited dose-dependent cytotoxic effect in MTT assay in human breast cancer (MCF-7) cells. Apoptotic degradation of DNA due to action of potent thiazolidin-4-ones was analysed by agarose gel electrophoresis and visualized by ethidium bromide staining (comet assay). A concentration-dependent increase in tail length and olive tail moment was observed when treated with thiazolidin-4-ones. In vitro antioxidant studies like DPPH and ABTS-free radical scavenging assays-indicated moderate activity of thiazolidin-4-ones. © 2012 Springer Science+Business Media, LLC.