92254-77-8Relevant academic research and scientific papers
Transition-Metal-Free Photoinduced Intramolecular Annulation of 2,3-Di(hetero)arylchromen-4-one
Han, Jie,Wang, Tao,Liang, Yong,Li, Ying,Li, Chenchen,Wang, Rui,Feng, Siqi,Zhang, Zunting
supporting information, p. 3552 - 3555 (2017/07/17)
An efficient transition-metal-free photoinduced intracyclization of 4H-chromen-4-ones in EtOH-H2O (7:1, v/v) at ambient temperature for the construction of complicated fused-ring heteroaromatics is established. The reaction proceeds smoothly without requiring any catalysts/additives.
Discovery of 3-(4-hydroxybenzyl)-1-(thiophen-2-yl)chromeno[2,3-c]pyrrol- 9(2H)-one as a phosphodiesterase-5 inhibitor and its complex crystal structure
Shang, Na-Na,Shao, Yong-Xian,Cai, Ying-Hong,Guan, Matthew,Huang, Manna,Cui, Wenjun,He, Lin,Yu, Yan-Jun,Huang, Lei,Li, Zhe,Bu, Xian-Zhang,Ke, Hengming,Luo, Hai-Bin
, p. 86 - 98 (2014/05/06)
Phosphodiesterase-5 (PDE5) inhibitors have been approved for the treatment of erectile dysfunction and pulmonary hypertension, but enthusiasm on discovery of PDE5 inhibitors continues for their potential new applications. Reported here is discovery of a series of new PDE5 inhibitors by structure-based design, molecular docking, chemical synthesis, and enzymatic characterization. The best compound, 3-(4-hydroxybenzyl)-1-(thiophen-2-yl)chromeno[2,3-c]pyrrol-9(2H)-one (57), has an IC50 of 17 nM against the PDE5 catalytic domain and good selectivity over other PDE families. The crystal structure of the PDE5 catalytic domain in complex with 57 was determined at 2 A resolution and showed that 57 occupies the same pocket as other PDE5 inhibitors, but has a different binding pattern in detail. On the basis of the binding pattern of 57, a novel scaffold can be proposed as a candidate of PDE inhibitors.
Synthesis of multi-functionalized chromeno[2, 3-c]pyrrol-9(2H)-ones: Investigation and application of Baker-Venkataraman rearrangement involved reactions catalyzed by 4-(Dimethylamino)pyridine
Yu, Yanjun,Hu, Yun,Shao, Weiyan,Huang, Jianing,Zuo, Yinglin,Huo, Yingpeng,An, Linkun,Du, Jun,Bu, Xianzhang
experimental part, p. 4551 - 4563 (2011/10/03)
An efficient one-pot synthesis of multi-functionalized chromeno[2, 3-c]pyrrol-9(2H)-ones from 1, 3-diaryl-1, 3-diket-ones and amino acids is described. The synthesis is based on the 4-(dimethylamino)pyridine-catalyzed Baker-Venkatara-man rearrangement and
