| Literature DB >> 28296398 |
Heather E Burks1, Tinya Abrams1, Christina A Kirby1, Jason Baird1, Alexander Fekete1, Lawrence G Hamann1, Sunkyu Kim1, Franco Lombardo1, Alice Loo1, Danuta Lubicka1, Kaitlin Macchi1, Donald P McDonnell2, Yuji Mishina1, John D Norris2, Jill Nunez1, Chitra Saran1, Yingchuan Sun1, Noel M Thomsen1, Chunrong Wang1, Jianling Wang1, Stefan Peukert1.
Abstract
Tetrahydroisoquinoline 40 has been identified as a potent ERα antagonist and selective estrogen receptor degrader (SERD), exhibiting good oral bioavailability, antitumor efficacy, and SERD activity in vivo. We outline the discovery and chemical optimization of the THIQ scaffold leading to THIQ 40 and showcase the racemization of the scaffold, pharmacokinetic studies in preclinical species, and the in vivo efficacy of THIQ 40 in a MCF-7 human breast cancer xenograft model.Entities:
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Year: 2017 PMID： 28296398 DOI： 10.1021/acs.jmedchem.6b01468
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446