Camptothecin-1-oxide derivatives

Details Camptothecin-1-oxide derivatives Camptothecin-1-oxide derivatives

1982-09-02

1985-04-23

Daus, Donald G.

Organic compounds -- part of the class 532-570 series

Organic compounds

Heterocyclic carbon compounds containing a hetero ring...

C07D49122, A61K 3147

Patent

active

045131384

ABSTRACT:
New 5- and/or 7-substituted camptothecin-1-oxide derivatives possessing anti-tumor activity with slight toxicity, represented by the general formula: ##STR1## wherein R is a hydrogen atom, an alkyl group, a hydroxyl group, an alkoxy group or an acyloxy group and R' is a hydrogen atom, an alkyl group, an aralkyl group, a hydroxymethyl group, an acyloxymethyl group or a carboxymethyl group, with the proviso that both of R and R' should not be hydrogen atoms. These 5- and/or 7-substituted camptothecin-1-oxide derivatives are prepared by treating the corresponding 5- and/or 7-substituted camptothecins with a peroxidant as an N-oxidizing reagent.

REFERENCES:
Lown, et al., Biochemical Pharmacology, vol. 29, No. 6, pp. 905-915, (1980).
Miyasaka, et al., Heyerocycles, vol. 16, No. 10, 1713-1717, (1981).
Boekelheide, et al., J. Am. Chem. Soc., vol. 76, pp. 1286-1291, (1954).
Herz, et al., J. Am. Chem. Soc., vol. 76, pp. 4184-4185, (1954).

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