AI Article Synopsis
- 3,5-diaryl-4,5-dihydropyrazoles are effective inhibitors of KSP, showing strong effectiveness in living systems.
- These inhibitors can be tuned for better performance by adding weakly basic amines, which improve their properties.
- It was crucial to carefully tweak the strength of the amine to keep their effectiveness in resistant cells while ensuring they dissolve well in water.
Article Abstract
3,5-diaryl-4,5-dihydropyrazoles were discovered to be potent KSP inhibitors with excellent in vivo potency. These enzyme inhibitors possess desirable physical properties that can be readily modified by incorporation of a weakly basic amine. Careful adjustment of amine basicity was essential for preserving cellular potency in a multidrug resistant cell line while maintaining good aqueous solubility.
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| http://dx.doi.org/10.1016/j.bmcl.2007.07.046 | DOI Listing |
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