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Discovery of an acrylic acid Based Tetrahydroisoquinoline as an Orally Bioavailable Selective Estrogen Receptor Degrader for ERa+ Breast Cancer

Burks, Heather and Abrams, Tinya and Baird, Jason and Fekete, Alexander and Hamann, Lawrence and Kim, Sunkyu and Kirby, Christina and Lambardo, Franco and Loo, Alice and Lubicka, Danuta and Macchi, Kaitlin and McDonnell, Donald P. and Mishina, Yuji and Norris, John and Nunez, Jill and Saran, Chitra and Sun, Yingchuan and Thomsen, Noel and Wang, Chunrong and Peukert, Stefan and Wang, Jianling (2017) Discovery of an acrylic acid Based Tetrahydroisoquinoline as an Orally Bioavailable Selective Estrogen Receptor Degrader for ERa+ Breast Cancer. Journal of Medicinal Chemistry.

Abstract

Tetrahydroisoquinoline 37 has been identified as a potent ER antagonist and selective estrogen receptor degrader (SERD); exhibiting good oral bioavailability, anti-tumor efficacy as well as SERD activity in vivo. This paper summarizes the discovery of THIQ 37, chemical optimization of the THIQ scaffold, pharmacokinetics in preclinical species, as well as the in vivo efficacy of THIQ 37 in a MCF7 human breast cancer xenograft model.

Item Type: Article
Date Deposited: 29 Mar 2017 00:45
Last Modified: 29 Mar 2017 00:45
URI: https://oak.novartis.com/id/eprint/30198

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