F-KCW-Department Publications

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    BIOLOGICALLY ACTIVE PERSPECTIVE SYNTHESIS OF HETEROANNULATED 8-NITROQUINOLINES WITH GREEN CHEMISTRY APPROACH
    (Elsevier, 2017-02-20) T, Arasakumar; S, Mathusalini; S, Gopalan; S, Shyamsivappan; A, Ata; P S, Mohan
    A new class of pyrazolo[4,3-c]quinoline (5a-i, 7a-b) and pyrano[3,2-c]quinoline (9a-i) derivatives were designed and synthesized in moderate to good yields by microwave conditions. To enhance the yield of pyrano[3,2-c]quinoline derivatives, multicomponent one-pot synthesis has been developed. The synthesized compounds were identified by spectral and elemental analyses. Compounds 9a and 9i showed good antibacterial activity against Gram-positive and Gram-negative bacterial strains. All of the new compounds exhibited weak to moderate antioxidant activity, compound 9d exerted significant antioxidant power. The cytotoxicity of these compounds were also evaluated against MCF-7 (breast) and A549 (Lung) cancer cell lines. Most of the compounds displayed moderate to good cytotoxic activity against these cell lines. Compound 9i was found to be significantly active in this assay and also induced cell death by apoptosis. Molecular docking studies were carried out using EGFR inhibitor in order to determine the molecular interactions.
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    ONE-POT APPROACH TO PYRIDO-4-PHENANTHRIDINONES BY PALLADIUM-CATALYZED ANNULATION OF 4-QUINOLONES WITH 2-BROMOBENZYL BROMIDES
    (Georg Thieme Verlag, 2019-01-01) T, Arasakumar; S, Shyamsivappan; S, Gopalan; A, Ata; P S, Mohan
    A straightforward approach toward the assembly of phenanthridinone heterocycles has been developed through the palladium-catalyzed N-benzylation/intramolecular coupling reactions of readily prepared 4-quinolones with commercially available 2-bromobenzyl bromide derivatives. The target products were prepared in moderate to good yields, with tolerance of various functional groups.
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    SYNTHESIS OF FIRST EVER 4-QUINOLONE-3-CARBOXYLIC ACID-APPENDED SPIROOXINDOLE-PYRROLIDINE DERIVATIVES AND THEIR BIOLOGICAL APPLICATIONS
    (Springer, 2017-02-01) T, Arasakumar; S, Mathusalini; A, Ata; R, Shankar; S, Gopalan; K, Lakshmi; P, Sakthivel; P S, Mohan
    A series of 4-quinolone-3-carboxylic acid-containing spirooxindole-pyrrolidine derivatives was synthesized via multicomponent 1,3-dipolar cycloaddition reactions of azomethine ylides with new (E)-4-oxo-6-(3-phenyl-acryloyl)-1,4-dihydroquinoline-3-carboxylic acids in good yields with high regioselectivity. The cycloadducts were characterized by analytical and spectral data including 1H, 13C, 2D NMR and mass spectroscopy. The structure of one of the compounds (8a) was investigated theoretically by computational techniques. DFT studies support the proposed mechanism for this cyclo addition reaction. Furthermore, antibacterial activities of the new compounds were evaluated against Gram-positive and Gram-negative bacterial strains. Compounds 8f, 8m and 8p showed potent inhibition activities against selected bacteria. The in vitro cytotoxicity of spirooxindole derivatives (8a–r) was evaluated against MCF-7 breast cancer cell line. Among the various compounds tested, compound 8f (IC50=18.35 μM) showed significant cytotoxic activity compared to the standard drug doxorubicin (IC50=15.00 μM).