1146210-64-1Relevant articles and documents
Synthesis, determination of absolute configuration, and biological evaluation of spiro-fused thiadiazoline inhibitors of kinesin spindle protein (KSP)
Angeles, Angie R.,Yang, Liping,Dai, Chaoyang,Brunskill, Andrew,Basso, Andrea D.,Siddiqui, M. Arshad
supporting information; experimental part, p. 6236 - 6239 (2011/01/12)
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.
SPIRO-CONDENSED 1, 3, 4-THIADIAZOLE DERIVATIVES FOR INHIBITING KSP KINESIN ACTIVITY
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Page/Page column 345-346, (2009/05/28)
The present invention relates to compounds of Formula (I), below, (wherein X, R1, R2, R3, p, E, ring A, and ring B are as defined herein). The present invention also relates to compositions (including pharmaceutically acceptable compositions) comprising t