Camptothecin compound containing multiple organic hydroxy-acid group on 10-bit substituent, its production and composition

Abstract

A camptothecin compound containing multiple organic carboxylic group on 10-bit substituting group, its production, medicinal composition and use as antineoplastic are disclosed. A1 and A2 express C1-C6 straight chain alkyl residue, C3-C20 branched chain alkyl residue or H. A1 and A2 can't be H simultaneously, A1 and A2 are connected into ring, B represents organic carboxylic or other carboxylic salt functional group, when A1 expresses H, A2 represents aromatic nucleus base residue, C5-C6 naphthene residue and 4-6heterocyclic residue, C3-C20 is branched chain alkyl residue, and A2-B is selected from C((CH2)a-CONH-C((CH2)a-COOH)a)a, a=1, 2 or 3.

Description

Camptothecin compound containing multiple organic carboxylic acid groups on the 10-position substituent and its preparation method and composition technical field The present invention relates to a kind of plant alkaloid as cytotoxic drug, especially a kind of camptothecin compound, more specifically, the present invention relates to the camptothecin containing multiple organic carboxylic acid groups on the 10-position substituent Compounds, processes for their preparation, pharmaceutical compositions containing them and their use as medicaments, especially as antitumor medicaments. Background technique In 1966, American scientist Wall et al. first isolated camptothecin from camptotheca japonica in China, which aroused great interest because of its unique chemical structure and significant antitumor activity. However, camptothecin cannot enter clinical research due to its poor water solubility. In the 1970s, Chinese scholars opened the lactone ring with sodium hydroxide a...

AI Technical Summary

Problems solved by technology

However, camptothecin cannot enter clinical research due to its poor water solubility.

In the 1970s, Chinese scholars opened the lactone ring with sodium hydroxide and prepared it into a water-soluble sodium salt for clinical research. As a result, side effects such as severe bone marrow suppression, vomiting, diarrhea and severe hemorrhagic cystitis occurred, and the open ring The activity of the form was greatly reduced, so that the clinical study was terminated

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