Camptothecin derivatives

Organic compounds -- part of the class 532-570 series – Organic compounds – Heterocyclic carbon compounds containing a hetero ring...

Patent

Rate now

  [ 0.00 ] – not rated yet Voters 0   Comments 0

Details

424258, C07D491147, A61K 3147

Patent

active

043992820

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 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), Sugasawa
Baxmann et al., Chem. Ber., 111, 3403-3411 (1978).
Lown et al., Biochem. Pharmacol. 1980, 29(6), pp. 905-915 (6/80), Chemical Abstract, vol. 93, 61075 (1980).

LandOfFree

Say what you really think

Search LandOfFree.com for the USA inventors and patents. Rate them and share your experience with other people.

Rating

Camptothecin derivatives does not yet have a rating. At this time, there are no reviews or comments for this patent.

If you have personal experience with Camptothecin derivatives, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Camptothecin derivatives will most certainly appreciate the feedback.

Rate now

     

Profile ID: LFUS-PAI-O-815598

  Search
All data on this website is collected from public sources. Our data reflects the most accurate information available at the time of publication.