Stereoelectronic factors influencing the biological activity and DNA interaction of synthetic antitumor agents modeled on CC-1065.
Basic Information
ID: ALA1124266
Journal: J Med Chem
Title: Stereoelectronic factors influencing the biological activity and DNA interaction of synthetic antitumor agents modeled on CC-1065.
Authors: Warpehoski MA, Gebhard I, Kelly RC, Krueger WC, Li LH, McGovren JP, Prairie MD, Wicnienski N, Wierenga W.
Abstract: The synthesis, physicochemical properties, and biological activities of a series of novel spiro cyclopropyl compounds, modeled on the potent antitumor antibiotic CC-1065 (1), are described. Many of these synthetic analogues are significantly more effective than 1 against murine tumors. In particular, compound 27 exhibits high activity and potency. Structure-activity analysis supports a molecular mechanism for biological action involving hydrophobic interaction of the drug with DNA and acid-catalyzed alkylation of DNA.
CiteXplore: 3346875
DOI: 10.1021/jm00398a017
Patent ID: ┄