299165-10-9Relevant academic research and scientific papers
Synthesis of Novel Trifluoromethyl Group Containing Pyrido Furo/Thieno Pyrimidinone Derivatives and Their Anticancer Activity
Racha, Hanumandlu,Vadla, Balakishan,Peddolla, Kavitha,Betala, Sailu
supporting information, p. 1844 - 1849 (2019/05/21)
A series of novel trifluoromethyl group containing pyridofuro/thieno pyrimidinone derivatives 5a–p were prepared starting from 2-oxo/thioxo-6-phenyl/thien-2-yl-4-(trifluoromethyl)-1,2-dihydropyridine-3-carbonitrile 1 compound on reaction with bromoethylac
Synthesis of Novel Alkyl Amide Functionalized Trifluoromethyl Substituted Furo/thieno Pyridine Derivatives: Their Anticancer Activity and CoMFA and CoMSIA Studies
Bhoomandla, Srinu,Gunda, Shravan Kumar,Kotoori, Srawanthi,Kanuparthy, Phani Raja
supporting information, (2019/06/27)
A series of novel alkyl amide functionalized trifluoromethyl substituted furo/thieno pyridine derivatives 4a–h, 5a–d, and 6a–h were prepared starting from 2-oxo/thioxo-6-phenyl/thien-2-yl-4-(trifluoromethyl)-1,2-dihydropyridine-3-carbonitrile 1 on reactio
2-oxadiazole-3-aminothiophene thieno-[2,3-b] pyridine derivative and preparing method and application thereof
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Paragraph 0114-0116, (2017/09/01)
The invention belongs to the field of chemical pharmaceuticals, and particularly relates to a 2-oxadiazole-3-aminothiophene thieno-[2,3-b] pyridine derivative and a preparing method and application thereof. The structure of the 2-oxadiazole-3-aminothiophene thieno-[2,3-b] pyridine derivative is shown in the formula I. A compound of the 2-oxadiazole-3-aminothiophene thieno-[2,3-b] pyridine derivative has the good HCV inhibitory effect, and meanwhile shows the low cytotoxicity, and a new method is provided for development of an anti-HCV inhibitor. The general formula is defined in the description.
A new series of HCV inhibitors based on a 2-(thieno[2,3B]pyridin-2-yl)-1,3,4-oxadiazole scaffold
Zuo, Wei-Qiong,Wang, Ning-Yu,Zhu, Yong-Xia,Liu, Li,Xiao, Kun-Jie,Zhang, Li-Dan,Gao, Chao,Liu, Zhi-Hao,You, Xin-Yu,Shi, Yao-Jie,Peng, Cui-Ting,Ran, Kai,Tang, Hong,Yu, Luo-Ting
, p. 40277 - 40286 (2016/05/24)
A new series of HCV inhibitors based on a 2-(thieno[2,3-b]pyridin-2-yl)-1,3,4-oxadiazole scaffold was developed. Detailed SAR investigations revealed the HCV inhibitory activity was sensitive to the size of C5, the C6-fused ring, and the size and flexibility of C5′ cycloalkane, which led to the identification of several compounds with potent inhibitory activity against HCV genotype 1b replicon. The most potent compound 10d showed ～100-fold improvement in potency compared with compound 1, with an EC50 of 0.039 μM, but without obvious cytotoxicity in vitro.
Discovery and structure-activity relationships study of novel thieno[2,3-b]pyridine analogues as hepatitis C virus inhibitors
Wang, Ning-Yu,Zuo, Wei-Qiong,Xu, Ying,Gao, Chao,Zeng, Xiu-Xiu,Zhang, Li-Dan,You, Xin-Yu,Peng, Cui-Ting,Shen, Yang,Yang, Sheng-Yong,Wei, Yu-Quan,Yu, Luo-Ting
, p. 1581 - 1588 (2014/03/21)
Current treatment for hepatitis C is barely satisfactory, there is an urgent need to develop novel agents for combating hepatitis C virus infection. This study discovered a new class of thieno[2,3-b]pyridine derivatives as HCV inhibitors. First, a hit compound characterized by a thienopyridine core was identified in a cell-based screening of our privileged small molecule library. And then, structure activity relationship study of the hit compound led to the discovery of several potent compounds without obvious cytotoxicity in vitro (12c, EC50 = 3.3 μM, SI >30.3, 12b, EC50 = 3.5 μM, SI >28.6, 10l, EC50 = 3.9 μM, SI >25.6, 12o, EC 50 = 4.5 μM, SI >22.2, respectively). Although the mechanism of them had not been clearly elucidated, our preliminary optimization of this class of compounds had provided us a start point to develop new anti-HCV agents.
