6769-65-9Relevant articles and documents
Synthesis and structure-activity relationship of furoquinolinediones as inhibitors of Tyrosyl-DNA phosphodiesterase 2 (TDP2)
Yu, Le-Mao,Hu, Zhu,Chen, Yu,Ravji, Azhar,Lopez, Sophia,Plescia, Caroline B.,Yu, Qian,Yang, Hui,Abdelmalak, Monica,Saha, Sourav,Agama, Keli,Kiselev, Evgeny,Marchand, Christophe,Pommier, Yves,An, Lin-Kun
supporting information, p. 777 - 796 (2018/04/23)
Tyrosyl-DNA phosphodiesterase 2 (TDP2) is a recently discovered enzyme specifically repairing topoisomerase II (TOP2)-mediated DNA damage. It has been shown that inhibition of TDP2 synergize with TOP2 inhibitors. Herein, we report the discovery of the furoquinolinedione chemotype as a suitable skeleton for the development of selective TDP2 inhibitors. Compound 1 was identified as a TDP2 inhibitor as a result of screening our in-house compound library for compounds selective for TDP2 vs. TDP1. Further SAR studies provide several selective TDP2 inhibitors at low-micromolar range. The most potent compound 74 shows inhibitory activity with IC50 of 1.9 and 2.1 μM against recombinant TDP2 and TDP2 in whole cell extracts (WCE), respectively.
Design, synthesis, and biological evaluation of benzofuran derivatives as et receptor antagonists
Cai, Jin,Chen, Junqing,Cao, Meng,Wang, Peng,Feng, Chengliang,Ji, Min
, p. 5472 - 5480 (2013/12/04)
A series of novel benzofuran carboxylic acid derivatives have been designed and synthesized, with their antagonism effect screened on ET-1-induced contraction in the rat thoracic aortic ring. Some target compounds demonstrated significant inhibitory activ
Anti-allergic agents. I. 1,3-Bis-(2-carbethoxy-3-methylbenzofuranyl-4-oxy)-2-propanol and related derivatives
Sangwan,Rastogi,Kar
, p. 153 - 156 (2007/10/02)
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