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• W2314056341 abstract "A new benzophenone-diketopiperazine-type potent antimicrotubule agent was developed by modifying the structure of the clinical candidate plinabulin (1). Although the right-hand imidazole ring with a branched alkyl chain at the 5-position in 1 was critical for the potency of the antimicrotubule activity, we successfully substituted this moiety with a simpler 2-pyridyl structure by converting the left-hand ring from a phenyl to a benzophenone structure without decreasing the potency. The resultant compound 6b (KPU-300) exhibited a potent cytotoxicity, with an IC50 value of 7.0 nM against HT-29 cells, by strongly binding to tubulin (K d = 1.3 μM) and inducing microtubule depolymerization." @default.
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• W2314056341 date "2014-07-28" @default.
• W2314056341 modified "2023-09-27" @default.
• W2314056341 title "Development of a New Benzophenone–Diketopiperazine-Type Potent Antimicrotubule Agent Possessing a 2-Pyridine Structure" @default.
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• W2314056341 doi "https://doi.org/10.1021/ml5001883" @default.
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