Discovery of ARD-1676 as a Highly Potent and Orally Efficacious AR PROTAC Degrader with a Broad Activity against AR Mutants for the Treatment of AR + Human Prostate Cancer.

doi:10.1021/acs.jmedchem.3c01264

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Discovery of ARD-1676 as a Highly Potent and Orally Efficacious AR PROTAC Degrader with a Broad Activity against AR Mutants for the Treatment of AR + Human Prostate Cancer.

Journal of medicinal chemistry - 28 Sept 2023

Xiang Weiguo, Zhao Lijie, Han Xin, Xu Tianfeng, Kregel Steven, Wang Mi, Miao Bukeyan, Qin Chong, Wang Mingliang, McEachern Donna, Lu Jianfeng, Bai Longchuan, Yang Chao-Yie, Kirchhoff Paul D, Takyi-Williams John, Wang Lu, Wen Bo, Sun Duxin, Ator Mark, Mckean Robert, Chinnaiyan Arul M, Wang Shaomeng

Abstract excerpt

We report herein the discovery and extensive characterization of ARD-1676, a highly potent and orally efficacious PROTAC degrader of the androgen receptor (AR). ARD-1676 was designed using a new class of AR ligands and a novel cereblon ligand. It has DC50 values of 0.1 and 1.1 nM in AR+ VCaP and LNCaP cell lines, respectively, and IC50 values of 11.5 and 2.8 nM in VCaP and LNCaP cell lines, respectively. ARD-1676...

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PMID: 37683104
DOI: 10.1021/acs.jmedchem.3c01264

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