1571-90-0Relevant articles and documents
Fragment-based lead discovery of a novel class of small molecule antagonists of neuropeptide B/W receptor subtype 1 (GPR7)
Moningka, Remond,Romero, F. Anthony,Hastings, Nicholas B.,Guo, Zhiqiang,Wang, Ming,Di Salvo, Jerry,Li, Ying,Trusca, Dorina,Deng, Qiaoling,Tong, Vincent,Terebetski, Jenna L.,Ball, Richard G.,Ujjainwalla, Feroze
, (2020/10/02)
Here, we report the discovery of a new class of NPBWR1 antagonists identified from a fragment-based screen. Compound 1 (cAMP IC50 = 250 μM; LE = 0.29) emerged as an initial hit. Further optimization of 1 by SAR-by-catalogue and chemical modification produced 21a (cAMP IC50 = 30 nM; LE = 0.39) with a 6700-fold increase in potency from fragment 1. Somewhat surprisingly, Schild analysis of compound 21a suggested that in vitro inhibition of NPW-mediated effects on upon cAMP accumulation were saturable, and that compound 21a dose-dependently increased [125I]-hNPW23 dissociation rate constants from NPBWR1 in kinetic binding studies. Collectively, these data are inconsistent with a classic surmountable, orthosteric mechanism of inhibition. The benzimidazole inhibitors reported herein may therefore represent a mechanistically differentiated class of compounds with which to form a better appreciation of the pharmacology and physiological roles of this central neuropeptide system.
A nanoscopic icosahedral {Mo72Fe30} cluster catalyzes the aerobic synthesis of benzimidazoles
Garazhian, Zohreh,Rezaeifard, Abdolreza,Jafarpour, Maasoumeh
, p. 34854 - 34861 (2019/11/14)
In this study, the catalytic efficiency of amorphous {Mo72Fe30} nanocapsules as a safe Keplerate polyoxometalate in organic synthesis was exploited. The easy-made solid catalyst exhibited high efficiency using a very low dosage (0.02
Design, synthesis and in vitro evaluation of 6-amide-2-aryl benzoxazole/benzimidazole derivatives against tumor cells by inhibiting VEGFR-2 kinase
Yuan, Xu,Yang, Qingyi,Liu, Tongyan,Li, Ke,Liu, Yuwen,Zhu, Changcheng,Zhang, Zhiyun,Li, Linghua,Zhang, Conghai,Xie, Mingjin,Lin, Jun,Zhang, Jihong,Jin, Yi
, p. 147 - 165 (2019/06/27)
Herein, we have carried out a structural optimization campaign to discover the novel anti-tumor agents with our previously screened YQY-26 as the hit compound. A library of thirty-seven 6-amide-2-aryl benzoxazole/benzimidazole derivatives has been designe
