Harmine derivatives, intermediates used in their preparations, preparation processes and use thereof

摘要

This invention relates to compounds of general formula (I), wherein R1, R2, R3, R4 and R5 are as defined in the specification; intermediates used in their preparation, preparation processes and use thereof. The present invention produces new harmine derivatives with enhanced antitumor activity and lower nervous system toxicity by structurally modification of the parent structure of β-carboline of harmines at position 1, 2, 3, 7 and 9. The compounds of the present invention can be prepared easily with high yield. They can be used in manufacture of a variety of antitumor medicines and medicines used in treatment of tumor diseases in combination of light or radiation therapy.;

主权项

1. A compound of the following formula (I): and its pharmacologically acceptable salts, wherein R1 is methyl; R2 is COOC2H5; R3 is hydrogen; and R4 is phenylpropyl; whereby the compound is ethyl 9-phenylpropyl-1-methyl-β-carboline-3-carboxylate.