AI Article Synopsis
- - A new group of kinesin inhibitors, specifically KIF18A inhibitors, was created by modifying the existing clinical drug AMG650.
- - A structure-activity relationship (SAR) study led to the identification of a compound with an alkenyl structure that is a highly effective KIF18A inhibitor.
- - This compound demonstrated strong anti-tumor effects in a mouse model of ovarian cancer (OVCAR-3 xenograft), with the ability to be taken orally and little impact on weight loss, indicating its potential for clinical use.
Article Abstract
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 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 can induce a dose-dependent antitumor efficacy in the OVCAR-3 model without significant reduction in body weight. Compound showed potential as a candidate for the clinical treatment of ovarian cancer.
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Source |
|---|---|
| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC11472545 | PMC |
| http://dx.doi.org/10.1021/acsmedchemlett.4c00383 | DOI Listing |
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