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

被引：23

作者：

Kumar, Atul ^{[1
]}

Tripathi, Vishwa Deepak ^{[1
]}

Kumar, Promod ^{[1
]}

Gupta, Lalit Prakash ^{[1
]}

Akanksha ^{[1
]}

Trivedi, Ritu ^{[2
]}

Bid, Hemant ^{[2
]}

Nayak, V. L. ^{[2
]}

Siddiqui, Jawed A. ^{[2
]}

Chakravarti, Bandana ^{[2
]}

Saxena, Ruchi ^{[2
]}

Dwivedi, Anila ^{[2
]}

Siddiquee, M. I. ^{[3
]}

Siddiqui, U. ^{[3
]}

Konwar, Rituraj ^{[2
]}

Chattopadhyay, Naibedya ^{[2
]}

机构：

[1] CSIR Cent Drug Res Inst, Med & Proc Chem Div, Lucknow 226001, Uttar Pradesh, India

[2] CSIR Cent Drug Res Inst, Div Endocrinol, Lucknow 226001, Uttar Pradesh, India

[3] CSIR Cent Drug Res Inst, Mol & Struct Biol Div, Lucknow 226001, Uttar Pradesh, India

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2011年 / 19卷 / 18期

关键词：

Anti-breast cancer; SERM; Anti-implantation; Raloxifene; Osteoporosis; ESTROGEN; TAMOXIFEN;

D O I：

10.1016/j.bmc.2011.07.056

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

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 secoraloxifene 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. (C) 2011 Elsevier Ltd. All rights reserved.

引用

页码：5409 / 5419

页数：11

共 21 条

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