1,2-Bis(sulfonyl)hydrazines. 3. Effects of structural modification on antineoplastic activity.

Abstract

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.

• Authors: K Shyam, R T Hrubiec, R Furubayashi, L A Cosby, A C Sartorelli
• Journal: Journal of medicinal chemistry (J Med Chem) Vol. 30 Issue 11 Pg. 2157-61 (Nov 1987) ISSN: 0022-2623 [Print] United States
• PMID: 3669023 (Publication Type: Journal Article, Research Support, U.S. Gov't, P.H.S.)

Chemical References

• Antineoplastic Agents
• Methylhydrazines

Topics

• Animals
• Antineoplastic Agents (chemical synthesis, pharmacology)
• Leukemia L1210 (drug therapy)
• Melanoma, Experimental (drug therapy)
• Methylhydrazines (chemical synthesis, pharmacology)
• Mice
• Structure-Activity Relationship