Synthesis and identification of α-cyano bis(indolyl)chalcones as novel anticancer agents

[Display omitted] Microwave-assisted synthesis of 23 α-cyano bis(indolyl)chalcones (6a–w) and their in vitro anticancer activity against three human cancer cell lines have been discussed. Among the synthesized chalcones, compound 6n was found to be the most potent and selective against A549 lung can...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2014-11, Vol.24 (22), p.5170-5174
Hauptverfasser:	Kumar, Dalip, Maruthi Kumar, N., Tantak, Mukund P., Ogura, Maiko, Kusaka, Eriko, Ito, Takeo
Format:	Artikel
Sprache:	eng
Schlagworte:	Anticancer agents Antineoplastic Agents - chemical synthesis Antineoplastic Agents - pharmacology Bis(indole) Cell Line, Tumor Cell Survival - drug effects Cell Survival - physiology Chalcones Chalcones - chemical synthesis Chalcones - pharmacology Dose-Response Relationship, Drug Drug Screening Assays, Antitumor - methods Humans Microwave-assisted synthesis Tubulin inhibitors
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Zusammenfassung:	[Display omitted] Microwave-assisted synthesis of 23 α-cyano bis(indolyl)chalcones (6a–w) and their in vitro anticancer activity against three human cancer cell lines have been discussed. Among the synthesized chalcones, compound 6n was found to be the most potent and selective against A549 lung cancer cell line (IC50=0.8μM). In a preliminary mechanism of action studies some α-cyano bis(indolyl)chalcones were found to enhance tubulin polymerization suggesting these compounds could act as microtubule stabilizing agents.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2014.09.085