2. Academic Validation
  3. Synthesis and anticancer activity of novel curcumin-quinolone hybrids

Synthesis and anticancer activity of novel curcumin-quinolone hybrids

  • Bioorg Med Chem Lett. 2015 Sep 1;25(17):3601-5. doi: 10.1016/j.bmcl.2015.06.068.
Saiharish Raghavan 1,  Prasath Manogaran 2,  Krishna Kumari Gadepalli Narasimha 3,  Balasubramanian Kalpattu Kuppusami 1,  Palanivelu Mariyappan 1,  Anjana Gopalakrishnan 2,  Ganesh Venkatraman 4
Affiliations

Affiliations

  • 1 Department of Medicinal Chemistry, Sri Ramachandra University, Chennai 600 116, India.
  • 2 Department of Human Genetics, Sri Ramachandra University, Chennai 600 116, India.
  • 3 Department of Medicinal Chemistry, Sri Ramachandra University, Chennai 600 116, India. Electronic address: drkrishna2011@gmail.com.
  • 4 Department of Human Genetics, Sri Ramachandra University, Chennai 600 116, India. Electronic address: ganeshv@sriramachandra.edu.in.
PMID: 26174555 DOI: 10.1016/j.bmcl.2015.06.068
Abstract

A number of new curcumin-quinolone hybrids were synthesised from differently substituted 3-formyl-2-quinolones and vanillin and their in vitro cytotoxicity was determined on a panel of representative cell lines (A549, MCF7, SKOV3 and H460) using MTT assay. The most potent compound 14, was analysed for its mode of action using various Cell Biology experiments. SKOV3 cells treated with compound 14 showed distorted cell morphology under phase contrast imaging and induction of Apoptosis was confirmed by Annexin V/PE assay. Further experiments on generation of Reactive Oxygen Species (ROS) and cell cycle analysis revealed that these hybrids induce Apoptosis by ROS generation and arrest cell cycle progression in S and G2/M phase.

Keywords

Annexin-V; Cell cycle analysis; Curcumin–quinolone hybrids; MTT assay.

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