Synthesis and biological evaluation of bicalutamide analogues for the potential treatment of prostate cancer

Kandil, Sahar B. ORCID: https://orcid.org/0000-0003-1806-9623, McGuigan, Christopher ORCID: https://orcid.org/0000-0001-8409-710X and Westwell, Andrew D. ORCID: https://orcid.org/0000-0002-5166-9236 2021. Synthesis and biological evaluation of bicalutamide analogues for the potential treatment of prostate cancer. Molecules 26 (1) , 56. 10.3390/molecules26010056

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Abstract

The androgen receptor (AR) is a pivotal target for the treatment of prostate cancer (PC) even when the disease progresses toward androgen-independent or castration-resistant forms. In this study, a series of 15 bicalutamide analogues (sulfide, deshydroxy, sulfone, and O-acetylated) were prepared and their antiproliferative activity evaluated against four different human prostate cancer cell lines (22Rv1, DU-145, LNCaP, and VCap). Bicalutamide and enzalutamide were used as positive controls. Seven of these compounds displayed remarkable enhancement in anticancer activity across the four PC cell lines. The deshydroxy analogue (16) was the most active compound with IC50 = 6.59–10.86 µM. Molecular modeling offers a plausible explanation of the higher activity of the sulfide analogues compared to their sulfone counterparts.

Item Type:	Article
Date Type:	Publication
Status:	Published
Schools:	Pharmacy
Additional Information:	This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/ licenses/by/4.0/)
Publisher:	MDPI
ISSN:	1420-3049
Date of First Compliant Deposit:	4 January 2021
Date of Acceptance:	22 December 2020
Last Modified:	08 May 2023 00:28
URI:	https://orca.cardiff.ac.uk/id/eprint/137284

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