Design and synthesis of 1,3-biarylsulfanyl derivatives as new anti-breast cancer agents

  • Bioorg Med Chem. 2011 Sep 15;19(18):5409-19. doi: 10.1016/j.bmc.2011.07.056.
Atul Kumar  1 ,  Vishwa Deepak Tripathi ,  Promod Kumar ,  Lalit Prakash Gupta ,  Akanksha ,  Ritu Trivedi ,  Hemant Bid ,  V L Nayak ,  Jawed A Siddiqui ,  Bandana Chakravarti ,  Ruchi Saxena ,  Anila Dwivedi ,  M I Siddiquee ,  U Siddiqui ,  Rituraj Konwar ,  Naibedya Chattopadhyay
Affiliations
  • 1. Medicinal and Process Chemistry Division, CSIR-Central Drug Research Institute, Lucknow 226 001, India. [email protected]
PMID: 21871812 DOI: 10.1016/j.bmc.2011.07.056
Abstract

A new series of 1,3-biarylsulfanyl derivatives (homodibenzyl core motif) have been designed and synthesized as new Estrogen Receptor ligands by chopping benzothiophene core of raloxifene to engender seco-raloxifene scaffold. All the synthesized compounds were screened for anti-proliferative, anti-osteoporotic, and anti-implantation activity. Compounds (35, 36) having basic amino anti-estrogenic side chain were exhibiting potential anti-proliferative activity in MCF-7, MDA-MB-231 and ishikawa cell lines. Some of the synthesized compounds having homodibenzyl motif (5, 8, 10) have shown moderate anti-osteoporotic activity.