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Structure–activity relationship of S-trityl-L-cysteine analogues as inhibitors of the human mitotic kinesin Eg5

…, F Liger, B Marquet, C Laggner, B Joseph…

文献索引:DeBonis, Salvatore; Skoufias, Dimitrios A.; Indorato, Rose-Laure; Liger, Francois; Marquet, Bernard; Laggner, Christian; Joseph, Benoit; Kozielski, Frank Journal of Medicinal Chemistry, 2008 , vol. 51, # 5 p. 1115 - 1125

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被引用次数: 48

摘要

The human kinesin Eg5 is a potential drug target for cancer chemotherapy. Eg5 specific inhibitors cause cells to block in mitosis with a characteristic monoastral spindle phenotype. Prolonged metaphase block eventually leads to apoptotic cell death. S-trityl-L-cysteine (STLC) is a tight-binding inhibitor of Eg5 that prevents mitotic progression. It has proven antitumor activity as shown in the NCI 60 tumor cell line screen. It is of considerable ...