Department Of Chemistry

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    Chitosan-supported copper as an efficient and recyclable heterogeneous catalyst for A3/decarboxylative A3-coupling reaction
    (Elsevier Ltd, 2018) Kaur, Pavneet; Kumar, Bhupinder; Kumar, Vinod; Kumar, Rakesh
    Chitosan-supported copper (chit@copper) based heterogeneous catalysts have been explored for A3-coupling and decarboxylative A3-coupling. The developed protocol employs low catalyst loading, solventless condition and easy work-up for the synthesis of diversely substituted propargylamines. More importantly, the catalyst could be recovered and reused without any significant loss in the activity. This offer huge advantages as recyclability issues are rarely addressed in decarboxylative A3-coupling. Leaching studies were carried out using AAS and ICPMS analysis. It is envisaged that chit@copper catalysts can have potential applications in terms of efficiency and recyclability in the emerging area of decarboxylative C?H bond activation/functionalization strategies. ? 2018 Elsevier Ltd
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    Mechanisms of tubulin binding ligands to target cancer cells: Updates on their therapeutic potential and clinical trials
    (Bentham Science Publishers B.V., 2017) Kumar, Bhupinder; Kumar, Rakesh; Skvortsova, Ira; Kumar, Vinod
    Background: A number of chemically diverse substances bind to the tubulin and inhibit cell proliferation by disrupting microtubule dynamics. There are four binding sites for the ligands binding to the tubulin; taxane/epothilone and laulimalide/peloruside binding ligands stabilize microtubule while vinca and colchicine binding site agents promote microtubule depolymerization. Most of the tubulin binding ligands disturb the tubulin-microtubule dynamic equilibrium but these may exhibit anticancer activities through different mechanisms. Taxanes and epothilones are widely used cytotoxic agents and are found effective against different types of human malignancies. However, taxanes are susceptible to pgp mediated multi-drug resistance, dose limiting hematopoietic toxicity and cumulative neurotoxicity. Vinca alkaloids are already in clinical practice, but ligands binding to the colchicine site are still in the different stages of clinical trials. Objective: In the current review article, plausible mechanistic details about the interactions of ligands at the binding pocket and subsequent changes in the tubulin structure are described. The review article also illustrated different formulations of the tubulin binding agents in combination with other chemotherapeutic agents and their therapeutic potential against various human malignancies. Conclusion: Tubulin targeting agents emerged as one of the most successful anticancer drugs and a number of structurally different chemical compounds are in advance stages of clinical development. ? 2017 Bentham Science Publishers.