公开(公告)号：US10059674B2

公开(公告)日：2018-08-28

申请号：US15152922

申请日：2016-05-12

Applicant: ACT PHARMA CO., LTD.

Inventor： Zhaopeng Liu ,  Yanna Liu ,  Yanqiu Shi ,  Chengmei Zhang

IPC: C07D231/54

CPC classification number: C07D231/54

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.