AI Article Synopsis
- A structure-activity relationship analysis identified a new compound, AZD4877, as a promising kinesin spindle protein (KSP) inhibitor with strong biochemical potency and good pharmaceutical properties.
- AZD4877 caused cells to stop dividing and led to a monopolar spindle phenotype, which is a specific result of KSP inhibition, ultimately resulting in cellular death.
- The compound demonstrated a favorable pharmacokinetic profile and impressive effectiveness in living organisms, making it a strong candidate for cancer treatment in clinical development.
Article Abstract
Structure-activity relationship analysis identified (+)-N-(3-aminopropyl)-N-[1-(5-benzyl-3-methyl-4-oxo-[1,2]thiazolo[5,4-d]pyrimidin-6-yl)-2-methylpropyl]-4-methylbenzamide (AZD4877), from a series of novel kinesin spindle protein (KSP) inhibitors, as exhibiting both excellent biochemical potency and pharmaceutical properties suitable for clinical development. The selected compound arrested cells in mitosis leading to the formation of the monopolar spindle phenotype characteristic of KSP inhibition and induction of cellular death. A favorable pharmacokinetic profile and notable in vivo efficacy supported the selection of this compound as a clinical candidate for the treatment of cancer.
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| http://dx.doi.org/10.1021/jm200629m | DOI Listing |
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