2. Academic Validation
  3. Synthesis and identification of α-cyano bis(indolyl)chalcones as novel anticancer agents

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

  • Bioorg Med Chem Lett. 2014 Nov 15;24(22):5170-4. doi: 10.1016/j.bmcl.2014.09.085.
Dalip Kumar 1,  N Maruthi Kumar 2,  Mukund P Tantak 2,  Maiko Ogura 3,  Eriko Kusaka 3,  Takeo Ito 4
Affiliations

Affiliations

  • 1 Department of Chemistry, Birla Institute of Technology and Science, Pilani 333 031, India. Electronic address: dalipk@pilani.bits-pilani.ac.in.
  • 2 Department of Chemistry, Birla Institute of Technology and Science, Pilani 333 031, India.
  • 3 Department of Energy and Hydrocarbon Chemistry, Graduate School of Engineering, Kyoto University, Kyoto 615-8510, Japan.
  • 4 Department of Energy and Hydrocarbon Chemistry, Graduate School of Engineering, Kyoto University, Kyoto 615-8510, Japan. Electronic address: takeoito.kyoto@gmail.com.
PMID: 25442306 DOI: 10.1016/j.bmcl.2014.09.085
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.

Keywords

Anticancer agents; Bis(indole); Chalcones; Microwave-assisted synthesis; Tubulin inhibitors.

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