Ontology highlight
ABSTRACT:
SUBMITTER: Watts E
PROVIDER: S-EPMC6421522 | biostudies-literature | 2019 Mar
REPOSITORIES: biostudies-literature
Journal of medicinal chemistry 20190221 5
Concomitant inhibition of anaplastic lymphoma kinase (ALK) and bromodomain-4 (BRD4) is a potential therapeutic strategy for targeting two key oncogenic drivers that co-segregate in a significant fraction of high-risk neuroblastoma patients, mutation of ALK and amplification of MYCN. Starting from known dual polo-like kinase (PLK)-1-BRD4 inhibitor BI-2536, we employed structure-based design to redesign this series toward compounds with a dual ALK-BRD4 profile. These efforts led to compound ( R)-2 ...[more]