Abstract
A new series of bis indolyl tri keto diazo compounds and 3,5-bis(3′-indolyl) triazinones were designed and synthesized as anticancer agents. Their anticancer activity was screened in vitro towards four different human cancer cell lines like HeLa, MCF-7, MDA-MB-231 and A549 cell lines. Among them, compounds 17a and 17b showed potent cytotoxicity with inhibition (IC50) values of 4.6 and 1.3 µM on Human Cervical cancer cell line, respectively. The in silico simulation studies using ADT 1.5.6 tools revealed unique π–π interactions of indole ring of compound 17b with colchicines active site residue Tyr312 could be a valid reason behind its maximum potency when compared to remaining compounds in responsible of its higher activity.
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The authors will thankful to University Grants Commission, New Delhi, India for financial assistance in the form of Major Research Project F.No. 42-285/2013 (SR).
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Sreenivasulu, R., Durgesh, R., Jadav, S.S. et al. Synthesis, anticancer evaluation and molecular docking studies of bis(indolyl) triazinones, Nortopsentin analogs. Chem. Pap. 72, 1369–1378 (2018). https://doi.org/10.1007/s11696-017-0372-8
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DOI: https://doi.org/10.1007/s11696-017-0372-8