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DESIGN, SYNTHESIS, AND BIOLOGICAL EVALUATION OF 1-METHYL-1, 4-DIHYRDOINDENO1,2-CPYRAZOLE ANALOGUES AS POTENTIAL ANTICANER AGENTS TARGETING TUBULIN COLCHICINE BINDING SITE
DESIGN, SYNTHESIS, AND BIOLOGICAL EVALUATION OF 1-METHYL-1, 4-DIHYRDOINDENO1,2-CPYRAZOLE ANALOGUES AS POTENTIAL ANTICANER AGENTS TARGETING TUBULIN COLCHICINE BINDING SITE
The invention discloses an indenopyrazole small-molecule tubulin inhibitor, which is characterized by having a structure represented by general formula I:; ;wherein R represents NH2 or NHOH; the invention also discloses a preparation method of the indenopyrazole compound, or pharmaceutical salts thereof. The compound of the present invention is an indenopyrazole small-molecule tubulin inhibitor having a novel structure, and has very strong proliferation inhibition activity to human hepatocellular carcinoma (HepG2) cells, human prostate carcinoma (PC3) cells, human cervical carcinoma (HeLa) cells, human breast adenocarcinoma (MCF-7) cells, and human leukemia (K562) cells; the compound is similar to colchicine in mechanism of action, and thus capable of inhibiting tubulin polymerization; the compound is significant for enhancing the specificity and effectiveness of drugs, reducing toxic and side effects, preventing drug tolerance, and so on.
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