SYNTHESIS AND ANTITUMOR ACTIVITY OF NOVEL N '-(2-BENZYLTHIOBENZENESULFONYL)-1H-PYRAZOLE-1-AMIDINE DERIVATIVES

[摘要]：A series of N'-(2-benzylthio-4-chlorobenzenesulfonyl)-1H-pyrazole-1-amidines (23-36) were synthesized by the reaction of 3-amino-2-(benzenesulfonyl)guanidines (18-22) with adequate 1,3-diketones. The compounds 23, 24, 26, 30, 31, 34 and 35 were tested in vitro in the full NCI 60 cell panel. The most potent compound in the series (26) showed substantial activity toward some cell lines of leukemia and cancer cells of lung, colon, CNS, melanoma, renal, prostate and breast (GI(50) in the range 2.30-9.47 mu M).

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