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Merck

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

Bioorganic & medicinal chemistry (2011-08-30)
Atul Kumar, 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
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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Sigma-Aldrich
Tamoxifene, ≥99%