Pyrrolo[2,3-d]pyrimidine derivative and application in preparation of anti-malignant tumor medicament thereof

Abstract

The invention relates to a novel pyrrolo[2,3-d]pyrimidine derivative and an application in preparation of anti-malignant tumor medicaments thereof. The pyrrolo-pyrimidine compound of the invention is an ideal folic acid-dependent enzyme inhibitor, and has the advantages of less first-pass effect, high effective bioavailability, few dosage, less side effect, and the like when used for the prevention or treatment of various tumors such as leukemia, breast cancers, lung cancers, pancreas cancers, bladder cancers, stomach cancers, mesothelial cancers, colorectal cancers, and the like.

Description

technical field [0001] The present invention relates to a pyrrolopyrimidine derivative, its pharmaceutically acceptable salt and their use in preparing anti-malignant tumor drugs. Background technique [0002] Cancer is an enemy that endangers human health. At present, there is no effective drug that can cure most cancers. Although chemotherapy drugs have certain curative effects on cancer, they have large toxic and side effects. . [0003] Folate-dependent enzymes include dihydrofolate reductase (DHFR), thymidylate synthase (TS) and glycinamide ribonucleotide formyltransferase (glycinamide ribonucleotide formyltransferase) , GARFT) and so on. Dihydrofolate reductase plays a central role in the folic acid metabolic cycle. It catalyzes the reduction of dihydrofolate to tetrahydrofolate, and then generates various active derivatives of tetrahydrofolate under the action of other enzymes. Tetrahydrofolate derivatives are important coenzymes in cell one-carbon metabolism. Tet...

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Problems solved by technology

[0002] Cancer is an enemy that endangers human health. At present, there is no effective drug that can cure most cancers. Although chemotherapy drugs have a certain effect on cancer, they have large toxic and side effects.

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