title: Synthesis and identification of α-cyano bis(indolyl)chalcones as novel anticancer agents.
abstract: 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 = 0.8 μM). 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.
authors.affiliation: Department of Chemistry, Birla Institute of Technology and Science, Pilani 333 031, India. Electronic address: dalipk@pilani.bits-pilani.ac.in.
authors.forename: Dalip
authors.initials: D
authors.lastname: Kumar
authors.affiliation: Department of Chemistry, Birla Institute of Technology and Science, Pilani 333 031, India.
authors.forename: N
authors.initials: N
authors.lastname: Maruthi Kumar
authors.affiliation: Department of Chemistry, Birla Institute of Technology and Science, Pilani 333 031, India.
authors.forename: Mukund P
authors.initials: MP
authors.lastname: Tantak
authors.affiliation: Department of Energy and Hydrocarbon Chemistry, Graduate School of Engineering, Kyoto University, Kyoto 615-8510, Japan.
authors.forename: Maiko
authors.initials: M
authors.lastname: Ogura
authors.affiliation: Department of Energy and Hydrocarbon Chemistry, Graduate School of Engineering, Kyoto University, Kyoto 615-8510, Japan.
authors.forename: Eriko
authors.initials: E
authors.lastname: Kusaka
authors.affiliation: Department of Energy and Hydrocarbon Chemistry, Graduate School of Engineering, Kyoto University, Kyoto 615-8510, Japan. Electronic address: takeoito.kyoto@gmail.com.
authors.forename: Takeo
authors.initials: T
authors.lastname: Ito
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects / Q000502:physiology; D047188:Chalcones / Q000138:chemical synthesis* / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D004354:Drug Screening Assays, Antitumor / Q000379:methods; D006801:Humans
chemical_list: D000970:Antineoplastic Agents; D047188:Chalcones
keywords: Anticancer agents; Bis(indole); Chalcones; Microwave-assisted synthesis; Tubulin inhibitors