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Issue 7, 2017
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Rational design and synthesis of novel phenylsulfonyl-benzamides as anti-prostate cancer agents§

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Abstract

Prostate cancer is a major cause of male death worldwide and the identification of new efficient treatments is constantly needed. Different non-steroidal androgen receptor antagonists are approved also in the case of castration-resistant cancer forms. Using a rational approach and molecular modelling studies to modify the structure of antiandrogen drug bicalutamide, a new series of phenylsulfonyl-benzamide derivatives was designed and synthesised. Their antiproliferative activities were evaluated in four different human prostate cancer cell lines and several new compounds showed significantly improved IC50 values in the low μM range. The cytotoxicity profile was also evaluated for the novel structures in the HEK293 cell line.

Graphical abstract: Rational design and synthesis of novel phenylsulfonyl-benzamides as anti-prostate cancer agents

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Supplementary files

Article information


Submitted
05 Apr 2017
Accepted
03 May 2017
First published
26 May 2017

This article is Open Access

Med. Chem. Commun., 2017,8, 1414-1420
Article type
Research Article

Rational design and synthesis of novel phenylsulfonyl-benzamides as anti-prostate cancer agents

M. Bassetto, S. Ferla, G. Giancotti, F. Pertusati, A. D. Westwell, A. Brancale and C. McGuigan, Med. Chem. Commun., 2017, 8, 1414
DOI: 10.1039/C7MD00164A

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