Camptothecin derivatives

Details Camptothecin derivatives Camptothecin derivatives

1984-11-29

1987-10-13

Daus, Donald G.

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

Organic compounds

Heterocyclic carbon compounds containing a hetero ring...

C07D491147, A61K 3147

Patent

active

RE0325180

ABSTRACT:
New camptothecin derivatives possessing either or both of high anti-tumor activity and slight toxicity, represented by the general formula: ##STR1## wherein X is H, CH.sub.2 OH, COOH, an alkyl group, an aralkyl group or the grouping CH.sub.2 OR.sup.1 or COOR.sup.2 wherein R.sup.1 is an alkyl group or an acyl group and R.sup.2 is a lower alkyl group, Y is H, OH or the grouping OR.sup.3 wherein R.sup.3 is a lower alkyl group or an acyl group, and Z is H or an acyl group, with the proviso that when X is CH.sub.2 OH, an alkyl group or an aralkyl group, both Y and Z are H, that when X is the grouping CH.sub.2 OR.sup.1 or COOR.sup.2, Y is H, that when Y is OH, both X and Z are H, [and] that when Y is the grouping OR.sup.3, X is H, and that X, Y and Z are not each simultaneously hydrogen, and water-soluble alkali metal salts thereof. These camptothecin derivatives are prepared by treating camptothecin with sulfuric acid and a persulfate or with sulfuric acid and a peroxide, if necessary, with an organic compound corresponding to the organic moiety of the substituent to be introduced directly into camptothecin, in an aqueous medium in the presence or absence of a transition metal ion, and optionally treating the resultant products, if necessary, after oxidation of the introduced substituent, with an alkylating agent or an acylating agent.

REFERENCES:
patent: 3894029 (1975-07-01), Winterfeldt et al.
patent: 4031098 (1977-06-01), Sugusawa
Govindachari, et al., Chemical Abstracts, vol. 78, 133,394p (1973), & attached Chemical Substance Index p. 3441CS.
Gunasekara, et al., Chemical Abstracts, vol. 92, 18799b(1980).
Lown, et al., Biochem. Pharmacol., 1980, vol. 29, No. 6, pp. 905-915 (06/80).
Baxmann, et al., Chem. Ber., vol. 111, pp. 3403-3411 (1978).

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