Synthesis, determination of absolute configuration, and biological evaluation of spiro-fused thiadiazoline inhibitors of kinesin spindle protein (KSP)

AR Angeles, L Yang, C Dai, A Brunskill, AD Basso…

文献索引：Angeles, Angie R.; Yang, Liping; Dai, Chaoyang; Brunskill, Andrew; Basso, Andrea D.; Siddiqui, M. Arshad Tetrahedron Letters, 2010 , vol. 51, # 48 p. 6236 - 6239

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被引用次数: 7

摘要

A facile and highly convergent synthesis of biologically active spiro-fused thiadiazoline KSP inhibitors is reported. The highlights of the synthesis include the Michael reaction and cyclization of thiosemicarbazone to 1, 3, 4-thiadiazoline. This chemistry lends itself to the preparation of (+)-2, a potent and orally bioavailable anti-cancer agent, and to the development of a structure–activity relationship program.