43156-01-0Relevant academic research and scientific papers
Indole derivatives, Abl kinase inhibiting composition and pharmaceutical compositions for prevention and treatment of abnormal cell growth diseases comprising the same
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Paragraph 0253; 0255; 0256, (2016/10/10)
PURPOSE: An indole derivative compound, and an Abl kinase inhibitor composition and a pharmaceutical composition for preventing and treating abnormal cell growth diseases containing the same are provided to treat diseases caused by abnormal cell growth, function, or behavior, especially cancer, immune diseases, cardiovascular diseases, viral infectious diseases, inflammatory diseases, endocrine diseases, and neurological diseases. CONSTITUTION: An indole derivative of chemical formula 1 or a pharmaceutically acceptable salt is provided. A pharmaceutical composition for suppressing wild type Abl kinase and mutant type Abl (T315I) kinase contains the compound as an active ingredient and a pharmaceutically acceptable carrier or diluents. A pharmaceutical composition for treating proliferative diseases, immune diseases, cardiovascular diseases, neurological diseases, inflammatory diseases, endocrine diseases, or viral infectious diseases contains the compound as an active ingredient and a pharmaceutically acceptable carrier or diluents.
New benzimidazole-2-urea derivates as tubulin inhibitors
Wang, Wenna,Kong, Dexin,Cheng, Huimin,Tan, Li,Zhang, Zhang,Zhuang, Xiaoxi,Long, Huoyou,Zhou, Yang,Xu, Yong,Yang, Xiaohong,Ding, Ke
, p. 4250 - 4253 (2014/09/29)
Emerging drug resistance and other drawbacks limit tubulin inhibitors' therapeutic applications and developing novel tubulin inhibitors still attracts intensive efforts. We describe the discovery and structure-activity relationship study of a series of benzimidazole-2-urea derivatives as novel β tubulin inhibitors. The representative compound 6o potently suppressed the proliferation of a panel of human cancer cells (NCI-H460, Colo205, K562, A431, HepG2, Hela, MDA-MB-435S) with IC50 values of 0.040, 0.050, 0.006, 0.026, 1.774, 0.452 and 0.052 μM, respectively. Compound 6o obviously inhibited NCI-H460 spindles formation and induced cell cycle arrest at G2/M phase at 0.10 μM. Computational study suggested that 6o interacts with β tubulin in a novel binding mode. Our results suggested that benzimidazole-2-urea derivatives might be promising tubulin inhibitors with novel binding mode for further development.
Discovery of new benzothiazole-based inhibitors of breakpoint cluster region-abelson kinase including the T315i mutant
Hong, Seunghee,Kim, Jinhee,Yun, Sun-Mi,Lee, Hyunseung,Park, Yoonsu,Hong, Soon-Sun,Hong, Sungwoo
, p. 3531 - 3545 (2013/06/27)
The existence of drug resistance caused by mutations in the break-point cluster region-Abelson tyrosine kinase (Bcr-Abl) kinase domain remains a clinical challenge due to limited effective treatment options for chronic myeloid leukemia (CML). Herein we report a novel series of benzothiazole-based inhibitors that are effective against wild-type and T315I mutant Bcr-Abl kinases. The original hit compound, nocodazole, was extensively modified through a structure-based drug design strategy, especially by varying the groups at the C2 and C6 positions of the scaffold. In addition, the introduction of water-solubilizing groups at the terminal ethyl group resulted in enhanced physicochemical properties and potency in cellular inhibition. Several compounds inhibited the kinase activity of both wild-type Bcr-Abl and the T315I mutant with IC50 values in the picomolar range and exhibited good antiproliferative effects on Ba/F3 cell lines transformed with either wild-type or T315I mutant Bcr-Abl.
Synthesis and spectral properties of methyl 5-[(o-, m-, and p-r)- phenoxy]-2-benzimidazolecarbamate
Cortes,Anaya
, p. 745 - 748 (2007/10/03)
The preparation of eleven novel methyl 5-[(o-, m-, p-R)-phenoxy-2- benzimidazolecarbamates with possible pharmacological activity as anthelmintics is described. The structure of all products was corroborated by it, 1H-nmr, 13C-nmr and mass spectra.
