Alpha-naphthalenesulfonamide base quintuple heterocyclic compound and anti-tumor activity thereof

Abstract

The invention relates to an alpha-naphthalenesulfonamide base quintuple heterocyclic compound and application thereof in anti-tumor treatment. Shown as research results, the alpha-naphthalenesulfonamide base quintuple heterocyclic compound, an isomer thereof, a stereomer or a mixture of the stereomer and a pharmaceutically acceptable salt or a precursor all have suppression effects on tumor cells, wherein the suppression ratios of about half compounds on the cell level are superior to that of ML-7 positive control medicine. The invention is expected to lay the foundation for developing anti-tumor medicaments.

Description

Technical field: The invention relates to α-naphthalene sulfonamide five-membered heterocyclic compounds and their application in antitumor therapy. Background technique: In 2003, U.S. Patent (US20030171357A1) disclosed a series of 3-aminopyrazole compounds that can be used as protein kinase inhibitors, especially related documents [P.Pevarello, et al.J.Med.Chem.2004, 47 (13) , 3367-3380]; P.Pevarello, et al.Bioorg.Med.Chem.Lett.2006, 16, 1084-1090; Daniele Fancelli, et al.J.Med.Chem.2005, 48, 3080-3084] It was found that as a CDK2 inhibitor, it can effectively inhibit the malignant growth of tumor cells, and has good selectivity for CDK2. Cyclin-dependent kinase (CDK) is a serine / threonine protein kinase, which determines whether the cell cycle proceeds in an orderly manner, and it is only active when combined with the corresponding cell cycle protein. There are seven main CDKs (CDK1-7), the content of which is basically stable throughout the cell cycle. CDK2, CDK4 and C...

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The α-naphthalenesulfonamido five-membered heterocyclic compound of the present invention a...

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