Scaffold hopping from indoles to indazoles yields dual MCL-1/BCL-2 inhibitors from MCL-1 selective leads-Reference-Cited by-同舟云学术

Scaffold hopping from indoles to indazoles yields dual MCL-1/BCL-2 inhibitors from MCL-1 selective leads

Published:2022 Issue:8 Volume:13 Page:963-969
ISSN:2632-8682
Container-title:RSC Medicinal Chemistry
language:en
Short-container-title:RSC Med. Chem.

Author:

Drennen Brandon¹,Goodis Christopher C.¹,Bowen Nathan²,Yu Wenbo¹,Vickers Gregory²,Wilder Paul T.³,MacKerell Alexander D.¹⁴,Fletcher Steven¹⁴^ORCID

Affiliation:

1. University of Maryland School of Pharmacy, Department of Pharmaceutical Sciences, 20 N. Pine St., Baltimore, MD 21201, USA

2. Department of Chemistry, Cardiff University, CF10 3AT, UK

3. University of Maryland School of Medicine, 20 S. Greene St., Baltimore, MD 21201, USA

4. University of Maryland Greenebaum Cancer Center, 20 S. Greene St., Baltimore, MD 21201, USA

Abstract

The anti-tumour efficacies of selective inhibitors of anti-apoptotic BCL-2 family proteins are often compromised by the concomitant upregulation of sister proteins. Herein, we describe our efforts to develop dual MCL-1/BCL-2 inhibitors.

Funder

National Institutes of Health

University of Maryland

Publisher

Royal Society of Chemistry (RSC)

Subject

Organic Chemistry,Drug Discovery,Pharmaceutical Science,Pharmacology,Molecular Medicine,Biochemistry

Link

http://pubs.rsc.org/en/content/articlepdf/2022/MD/D2MD00095D

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