915711-42-1Relevant articles and documents
Discovery of potent colony-stimulating factor 1 receptor inhibitors by replacement of hinge-binder moieties
Lee, Jung Wuk,Park, Jiwon,Kim, Jina,Kim, Jihyung,Choi, Changyu,Min, Kyung Hoon
, (2021/03/14)
Tumor-associated macrophages (TAMs) are predominantly associated with tumor growth. Colony-stimulating factor 1 receptor (CSF1R) acts as a key regulator of TAM survival and differentiation and is a molecular target for cancer therapies. Herein, novel CSF1
Pyrrolo[3,2-b ]quinoxaline derivatives as types I1/2 and II Eph tyrosine kinase inhibitors: Structure-based design, synthesis, and in vivo validation
Unzue, Andrea,Dong, Jing,Lafleur, Karine,Zhao, Hongtao,Frugier, Emilie,Caflisch, Amedeo,Nevado, Cristina
, p. 6834 - 6844 (2014/10/15)
The X-ray crystal structures of the catalytic domain of the EphA3 tyrosine kinase in complex with two type I inhibitors previously discovered in silico (compounds A and B) were used to design type I1/2 and II inhibitors. Chemical synthesis of a
Research and development of a novel process for nilotinib: A Bcr-Abl inhibitor
Amala,Bhujanga Rao,Sreenivas,Dubey
, p. 4599 - 4602 (2013/07/04)
In this study, an efficient, economic and novel process for the production of highly pure nilotinib (1), a Bcr-Abl inhibitor in described. The synthesis comprises the chlorination of 4-methyl-3-nitro benzoic acid (2) to get 4-methyl-3-nitro benzoyl chloride (2A). Condensation of compound (2) with 5-(4-methyl-1H-imidazol-1-yl)-3-(trifluoromethyl)-benzeneamine (11) to obtain 4-methyl-N-[3-(4-methyl-1Himidazol- 1-yl-5-(trifluoromethyl)phenyl]-3-nitro- benzamide hydrochloride (3). Reducing compound (3) with stannous chloride (or) raney nickel to obtain 4-methyl-N-[3-(4-methyl-1H-imidazol-1-yl-5- (trifluoromethyl)phenyl]-3-amino-benzamide (4). Reaction of compound (4) with cyanamide to obtain 4-methyl-N-[3-(4-methyl-1H-imidazol-1-yl-5-(trifluoromethyl) phenyl]-3-guanidino-benzamide (5). Condensation of the compound (5) with 3-dimethylamino-1-(3-pyridyl)-2-propen-1-one (8) to obtain nilotinib (1).