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

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

Affiliation

  • 1 Medicinal and Process Chemistry Division, CSIR-Central Drug Research Institute, Lucknow 226 001, India. dratulsax@gmail.com
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.

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