Author
K.K. Sreenivasan
Bio: K.K. Sreenivasan is an academic researcher from Manipal University. The author has contributed to research in topics: Topoisomerase & Ehrlich ascites carcinoma. The author has an hindex of 1, co-authored 1 publications receiving 84 citations.
Papers
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TL;DR: The compounds displayed promising anticancer activity under these test systems and shall serve as useful 'leads' for further design.
88 citations
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TL;DR: This work was supported by the Foundation for Science and Technology (FCT), Portugal (projects PTDC/QUI-QUI/113687/2009 and PEst-C/QUI/UI0081/2013) and SFRH/BD/61262/2009.
Abstract: This work was supported by the Foundation for Science and Technology (FCT), Portugal (projects PTDC/QUI-QUI/113687/2009 and PEst-C/QUI/UI0081/2013). A.G. (SFRH/BD/43531/2008) and M.J.M. (SFRH/BD/61262/2009) thank FCT for grants.
514 citations
TL;DR: The present review focuses on the pharmacological profile of chromone derivatives in the current literature with an update of recent research findings on this nucleus and the perspectives that they hold for future research.
331 citations
TL;DR: 6/6,7-Substituted-3-formylchromones (8a-g) were reacted with 2 equivalents thiobenzamide in refluxing toluene to furnish substituted-3-(5-phenyl-3H-[1,2,4]dithiazol- 3-yl)chromen-4-ones (10a-G) in high yields.
148 citations
TL;DR: The differential analysis of the solvation effects among the chromone isomers gave additional insight about the superior outline of the 3-substituted chromone derivatives, which act preferably as MAO-B inhibitors.
Abstract: Two series of novel chromone derivatives were synthesized and investigated for their ability to inhibit the activity of monoamine oxidase. The SAR data indicate that chromone derivatives with substituents in position 3 of γ-pyrone nucleus act preferably as MAO-B inhibitors, with IC(50) values in the nanomolar to micromolar range. Almost all chromone 3-carboxamides display selectivity toward MAO-B. Identical substitutions on position 2 of γ-pyrone nucleus result in complete loss of activity in both isoforms (chromones 2-12 except 3 and 5). Notably, chromone (19) exhibits an MAO-B IC(50) of 63 nM, greater than 1000-fold selectivity over MAO-A, and behaves as a quasi-reversible inhibitor. Docking experiments onto the MAO binding of the most active compound highlight different interaction patterns among the isoforms A and B. The differential analysis of the solvation effects among the chromone isomers gave additional insight about the superior outline of the 3-substituted chromone derivatives.
130 citations
TL;DR: A series of new chromone analogues bearing heterocyclic thioether moiety and aurone analogue bearing cyclic tertiary amine moiety were designed and synthesized under microwave irradiation to present many advantages, such as higher yields, shorter reaction time, mild condition, and readily isolation of the products.
91 citations