KIF18A inhibitors(Changchun Genescience)

A novel class of kinesin KIF18A inhibitors were discovered through modification of the clinical compound AMG650. Structure-activity relationship (SAR) study led to the discovery of compound 16 with an alkenyl motif, a highly potent KIF18A inhibitor, which displayed a favorable pharmacological profile and excellent efficacy in a mouse model of an OVCAR-3 xenograft tumor. Oral administration of 16 can induce a dose-dependent antitumor efficacy in the OVCAR-3 model without significant reduction in body weight. Compound 16 showed potential as a candidate for the clinical treatment of ovarian cancer.

ADVERTISEMENT RETURN TO ISSUEPREVPatent HighlightNEXTNovel Amide Compounds as KIF18A Inhibitors for Treating CancerRam W. Sabnis*Ram W. SabnisSmith, Gambrell & Russell LLP, 1230 Peachtree Street NE, Suite 3100, Atlanta, Georgia 30309, United States*Email: [email protected]More by Ram W. Sabnishttp://orcid.org/0000-0001-7289-0581Cite this: ACS Med. Chem. Lett. 2021, 12, 5, 690–691Publication Date (Web):April 29, 2021Publication History Received11 April 2021Published online29 April 2021Published inissue 13 May 2021https://doi.org/10.1021/acsmedchemlett.1c00206Copyright © Published 2021 by American Chemical SocietyRIGHTS & PERMISSIONSArticle Views1030Altmetric-Citations-LEARN ABOUT THESE METRICSArticle Views are the COUNTER-compliant sum of full text article downloads since November 2008 (both PDF and HTML) across all institutions and individuals. These metrics are regularly updated to reflect usage leading up to the last few days.Citations are the number of other articles citing this article, calculated by Crossref and updated daily. Find more information about Crossref citation counts.The Altmetric Attention Score is a quantitative measure of the attention that a research article has received online. Clicking on the donut icon will load a page at altmetric.com with additional details about the score and the social media presence for the given article. Find more information on the Altmetric Attention Score and how the score is calculated. Share Add toView InAdd Full Text with ReferenceAdd Description ExportRISCitationCitation and abstractCitation and referencesMore Options Share onFacebookTwitterWechatLinked InReddit PDF (576 KB) Get e-AlertsSUBJECTS:Assays,Cells,Inhibition,Cancer,Cell physiology Get e-Alerts