1,2-Bis(sulfonyl)hydrazines. 3. Effects of structural modification on antineoplastic activity.
A series of 1,2-bis(sulfonyl)hydrazines was synthesized and evaluated for antineoplastic activity against the L1210 leukemia and the B16 melanoma. The most active agent to emerge from this study, 1,2-bis(methylsulfonyl)-1-methylhydrazine, produced a maximum % T/C for mice bearing the L1210 leukemia or the B16 melanoma of 340% and 278%, respectively. Two N-chloroethyl analogues, conceived as bifunctional alkylating agents, were also synthesized and evaluated for antineoplastic activity against the L1210 leukemia and the B16 melanoma. Although such a modification resulted in retention of antineoplastic activity against both tumor cell lines, it did not result in enhanced antineoplastic activity.
Shyam
K
K
Department of Pharmacology, Yale University School of Medicine, New Haven, Connecticut 06510.
Hrubiec
R T
RT
Furubayashi
R
R
Cosby
L A
LA
Sartorelli
A C
AC
D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000494:pharmacology*; D007939:Leukemia L1210 / Q000188:drug therapy; D008546:Melanoma, Experimental / Q000188:drug therapy; D008763:Methylhydrazines / Q000138:chemical synthesis / Q000494:pharmacology*; D051379:Mice; D013329:Structure-Activity Relationship
D000970:Antineoplastic Agents; D008763:Methylhydrazines