Abstract: 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.
Abstract: The invention relates to trehalose derivatives with general formula (I), a preparation method and uses thereof, wherein 6,6?-bis(2,3-dimethoxybenzoyl)-?,?-D-trehalose has anti-colon cancer 26-L5 cell invasion activity which is better than that of a natural product Brartemicin, IC50 is 0.10 ?g/mL (0.15 ?M), and when the IC50 is 10 ?g/mL, 6,6?-bis(2,3-dimethoxybenzoyl)-?,?-D-trehalose has no cytotoxicity, shows high-selectivity anti-tumor invasion activity and can be used for preparing medicaments for preventing and treating invasion and metastasis of colon cancer and the like.
Abstract: The invention relates to trehalose derivatives with general formula (I), a preparation method and uses thereof, wherein 6,6?-bis(2,3-dimethoxybenzoyl)-?,?-D-trehalose has anti-colon cancer 26-L5 cell invasion activity which is better than that of a natural product Brartemicin, IC50 is 0.10 ?g/mL (0.15 ?M), and when the IC50 is 10 ?g/mL, 6,6?-bis(2,3-dimethoxybenzoyl)-?,?-D-trehalose has no cytotoxicity, shows high-selectivity anti-tumor invasion activity and can be used for preparing medicaments for preventing and treating invasion and metastasis of colon cancer and the like.