2'Halo derivatives of daunomycin, desmethoxy daunomycin, adriamycin and carminomycin

US4427664A · kind A · utility

Assignee

• The United States of America, as represented by the Department of Health and Human Services · US

Inventors

• Derek Horton · Columbus, US
• Waldemar Priebe · Houston, US

Key dates

• Filing date: Aug 17, 1982
• Grant date: Jan 24, 1984
• Expiry date: Aug 17, 2002

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07H15/252
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

The compounds are derived from aglycons which may be daunomycin, desmethoxy daunomycin, adriamycin and carminomycin. A preferred compound is ##STR1## (1) R'=H; R.sup.2 =OMe; X; Y (2) R'=OH; R.sup.2 =OMe; X; Y PA1 (3) R'=H; R.sup.2 =H; X; Y PA1 (4) R'=H; R.sup.2 =OH; X; Y where PA1 X=I, Cl, Br, or F and PA1 Y=OH or AcO (acetoxy) where Y is AcO or OH and R'=H and R.sup.2 =OMe. These compounds are effective showing high anti-leukemic activity against P388 murine leukemia.