Synthesis and antineoplastic activity of 1a-formyl and 1a-thioformyl derivatives of mitomycin C and 2-methylaziridine.

Abstract

A select number of 1-formyl- and 1-thioformyl-2-methylaziridine derivatives and the corresponding 1a-substituted mitomycin C analogues were synthesized and tested for antineoplastic activity by using an in vivo test with murine P388 leukemia. Select compounds were also tested in vivo with murine melanoma B16. Several of the mitomycin C derivatives displayed activity and some of the mitomycin C analogues were comparable in activity to the parent compound.

• Authors: P L Fishbein, H Kohn
• Journal: Journal of medicinal chemistry (J Med Chem) Vol. 30 Issue 10 Pg. 1767-73 (Oct 1987) ISSN: 0022-2623 [Print] United States
• PMID: 3116255 (Publication Type: Journal Article, Research Support, U.S. Gov't, P.H.S.)

Chemical References

• Aziridines
• Azirines
• Formates
• Mitomycins
• Mitomycin
• propyleneimine

Topics

• Animals
• Aziridines (chemical synthesis, therapeutic use)
• Azirines (chemical synthesis)
• Formates
• Leukemia P388 (drug therapy)
• Melanoma (drug therapy)
• Mice
• Mitomycin
• Mitomycins (chemical synthesis, therapeutic use)
• Structure-Activity Relationship