Synthesis and evaluation of 2-substituted 1-methyl-1-(4-tolylsulfonyl)hydrazines as antineoplastic agents
作者:Robert T. Hrubiec、Krishnamurthy Shyam、Lucille A. Cosby、Ryosuke Furubayashi、Alan C. Sartorelli
DOI:10.1021/jm00157a033
日期:1986.7
Several N-2 substituted 1-methyl-1-(4-tolylsulfonyl)hydrazines were synthesized and evaluated for antineoplastic activity against the L1210 leukemia and the B16 melanoma. The most active compound to emerge from this study, 2-(methylsulfonyl)-1-methyl-1-(4-tolylsulfonyl)hydrazine, produced maximum percent T/C values with L1210 leukemia and B16 melanoma tumor bearing mice of 207 and 209, respectively
合成了几种N-2取代的1-甲基-1-(4-甲苯磺酰基)肼,并评估了其对L1210白血病和B16黑色素瘤的抗肿瘤活性。该研究中最活跃的化合物2-(甲基磺酰基)-1-甲基-1-(4-甲苯磺酰基)肼在L1210白血病和B16黑色素瘤荷瘤小鼠207和209中产生最大的T / C值,分别。虽然芳基,芳烷基或烷基磺酰基部分与N-2相连导致保留了针对两种肿瘤系统的活性,但相应的苯甲酰基,4-硝基苯甲酰基和(2-硝基苯基)亚磺酰基类似物仅显示出对L1210的活性白血病。