Diversity oriented synthesis of chromene-xanthene hybrids as anti-breast cancer agents

  • Bioorg Med Chem Lett. 2018 Feb 15;28(4):778-782. doi: 10.1016/j.bmcl.2017.12.065.
M Srinivas Lavanya Kumar  1 ,  Jyotsana Singh  2 ,  Sudipta Kumar Manna  1 ,  Saroj Maji  1 ,  Rituraj Konwar  3 ,  Gautam Panda  4
Affiliations
  • 1. CSIR-Central Drug Research Institute, BS 10/1, Sector 10, Jankipuram Extension, Sitapur Road, Lucknow 226031, India.
  • 2. Endocrinology Division, CSIR-Central Drug Research Institute, Sector 10, Jankipuram Extension, Sitapur Road, Lucknow 226031, UP, India.
  • 3. Academy of Scientific and Innovative Research, New Delhi 110001, India; Endocrinology Division, CSIR-Central Drug Research Institute, Sector 10, Jankipuram Extension, Sitapur Road, Lucknow 226031, UP, India.
  • 4. CSIR-Central Drug Research Institute, BS 10/1, Sector 10, Jankipuram Extension, Sitapur Road, Lucknow 226031, India; Academy of Scientific and Innovative Research, New Delhi 110001, India. Electronic address: [email protected].
PMID: 29352645 DOI: 10.1016/j.bmcl.2017.12.065
Abstract

A diverse library of chromene-xanthene hybrids were synthesized through intramolecular Friedel-Crafts reaction of the arenoxy carbinols. Examples include first incorporation of amino acid tyrosine into xanthene skeletons with polar functionalities. A careful structural evaluation revealed that tyrosine crafted chromene-xanthene hybrids exhibited good activities against breast Cancer cell lines MCF-7, MDA-MB-231. The lead compound 16 displays significant cell cycle arrest at G1 phase and induces Apoptosis in MDA-MB-231 cells.

Keywords
Anti-cancer; Chromene; Hybrid; Synthesis.