193979-47-4Relevant articles and documents
Organophotoredox-Catalyzed C-H Alkylation of Imidazoheterocycles with Malonates: Total Synthesis of Zolpidem
Chaubey, Narendra R.,Kapdi, Anant R.,Maity, Biswanath
, p. 1524 - 1530 (2021)
Organophotocatalytic C-H bond functionalization has attracted a lot of attention in the past several years due to the possibility of catalyzing reactions in a metal- and peroxide-free environment. Continuing on these lines, an organophotoredox-catalyzed C-H functionalization of imidazo[1,2- a ]pyridines and related heterocycles with bromomalonates under mild conditions is reported, providing excellent yields of the products at room temperature. This is the first report involving malonates as coupling partners leading to the synthesis of a range of functionalized products including total synthesis of zolpidem, a sedative-hypnotic drug molecule.
Structure-based discovery of potent and selective small-molecule inhibitors targeting signal transducer and activator of transcription 3 (STAT3)
Huang, Qiuyao,Zhong, Yan,Li, Bingbing,Ouyang, Shumin,Deng, Lin,Mo, Jianshan,Shi, Shuo,Lv, Nan,Wu, Ruibo,Liu, Peiqing,Hu, Wenhao,Zhang, Xiaolei,Wang, Yuanxiang
, (2021/05/17)
STAT3 has been validated as an attractive anticancer target due to its important roles in cancer initiation and progression. However, discovery of potent and selective STAT3 small-molecule inhibitors with druglike properties is still challenging. In this study, two series of substituted 2-phenylquinolines and 2-arylimidazo[1,2-a]pyridines were designed through structure-based drug discovery approach by condensing the privileged structures of STX-119 and SH4-54. Our study has resulted in the discovery of a number of highly potent and selective STAT3 inhibitors, exemplified by compound 39 with the privileged structure of 2-phenylimidazo[1,2-a]pyridine, which selectively inhibits phosphorylation of STAT3 and suppresses subsequent signaling pathway. Moreover, 39 inhibits cell growth, migration and invasion of human triple negative breast cancer (TNBC) cells lines. Consistently, it achieves significant and dose-dependent tumor growth inhibition in both cell line-derived and patient-derived xenograft tumor models in mice. These results clearly indicate that 39 is a highly potent and selective STAT3 inhibitor.
A cyanogen methylation imidazopyridine compound of preparation method (by machine translation)
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Paragraph 0081; 0082, (2019/03/02)
The invention discloses a cyanogen methylation imidazopyridine compound of preparation method, in order to imidazo [1, 2 - a] pyridine compound as raw material, with the bromine second grade nitrile or [...] and under the action of the photocatalysis reaction, is obtained. Compared with the prior art, the method of the invention avoids the use of potassium cyanide or sodium cyanide and two connecting, iodomethane, and in the preparation of imidazo [1, 2 - a] pyridine compound of the cyanogen methylation product in the process, the chemical conversion from the original threestep shortened to step. The invention short preparation route, the preparation method is simple, the production cost is low, and the yield is high, have reduced the solvent to use and at the time of blowdown to the environment caused by pollution, easy to implement, easy to realize industrial. (by machine translation)
