Optimized S-trityl-L-cysteine-based inhibitors of kinesin spindle protein with potent in vivo antitumor activity in lung cancer xenograft models
…, SK Talapatra, D Podgórski, SP MacKay…
Index: Good, James A. D.; Wang, Fang; Rath, Oliver; Kaan, Hung Yi Kristal; Talapatra, Sandeep K.; Podgorski, Dawid; MacKay, Simon P.; Kozielski, Frank Journal of Medicinal Chemistry, 2013 , vol. 56, # 5 p. 1878 - 1893
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Citation Number: 18
Abstract
The mitotic kinesin Eg5 is critical for the assembly of the mitotic spindle and is a promising chemotherapy target. Previously, we identified S-trityl-l-cysteine as a selective inhibitor of Eg5 and developed triphenylbutanamine analogues with improved potency, favorable drug- like properties, but moderate in vivo activity. We report here their further optimization to produce extremely potent inhibitors of Eg5 (K iapp< 10 nM) with broad-spectrum activity ...
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