Faculty Publications
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Item 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 .Item Synthesis and in vitro biological evaluation of new pyrazole chalcones and heterocyclic diamides as potential anticancer agents(Elsevier B.V., 2015) Sankappa Rai, U.; Isloor, A.M.; Shetty, P.; Pai, K.S.R.; Fun, H.-K.Synthesis and characterization of new heterocyclic pyrazole chalcones (4a-. e) and diamide (6a-. e) derivatives are described. Pyrazole chalcones were synthesized by the reaction of pyrazole aldehydes and suitable aromatic ketones. Diamides were synthesized by the reaction of phthalic acid and amines. Newly synthesized compounds were characterized by spectral studies and their biological activity was assessed in vitro using MCF-7 (human breast adenocarcinoma) and HeLa (human cervical tumor cells) cell lines. Few of the synthesized molecules inhibited the growth of the human breast cancer cell lines and human cervical tumor cell lines at low micromolar to nanomolar concentrations. © 2014 King Saud University.Item Calcium phosphate bioceramics with polyvinyl alcohol hydrogels for biomedical applications(Institute of Physics Publishing helen.craven@iop.org, 2019) Kumar, B.Y.S.; Isloor, A.M.; Sukumaran, S.; Venkatesan, J.; Mohan Kumar, G.C.M.Polyvinyl alcohol (PVA) hydrogels show desirable characteristics to use as a biomaterial especially for soft tissue replacement. However, their bio inertness restricts their application in vivo. In this study, polyvinyl alcohol was blended with bi-phasic calcium phosphate and to develop a composite hydrogel by a physical freeze-thawing method, followed by annealing treatment. The synthesized bi-phasic calcium phosphate (BCP) and composite hydrogels were characterized by SEM, XRD and FTIR. The concentration of BCP was optimized and it was found that BCP modifies the hydrogel network by developing the secondary electrostatic bonding between matrix and reinforcement. The highest tensile and compressive strength could reach 5.2 ± 0.6 MPa and 14.9 ± 0.3 MPa respectively for PVA/2.5BCP and they exhibit time-dependent, rapid self-recoverable and fatigue resistant behavior based on the cyclic loading-unloading compression test. Similar observations were found for viscoelastic properties which are relevant for the tissue engineering application. Friction study showed the composite hydrogel had a cartilage-like frictional response, dominated by the interstitial fluid support. Besides composite hydrogel showed excellent antimicrobial activity against bacterial species, Escherichia coli, Staphylococcus aureus and Candida albicans fungi, and the cytocompatibility towards L929 fibroblast cells provides a potential pathway to develop a hydrogel as a promising substitute for tissue engineering scaffold material. © 2019 IOP Publishing Ltd.