1270046-46-2Relevant academic research and scientific papers
Benzouracil-coumarin-arene conjugates as inhibiting agents for chikungunya virus
Hwu, Jih Ru,Kapoor, Mohit,Tsay, Shwu-Chen,Lin, Chun-Cheng,Hwang, Kuo Chu,Horng, Jia-Cherng,Chen, I-Chia,Shieh, Fa-Kuen,Leyssen, Pieter,Neyts, Johan
, p. 103 - 109 (2015)
Chikungunya virus (CHIKV) is an arbovirus that was first recognized in an epidemic form in East Africa in 1952-1953. The virus is primarily transmitted through mosquitoes and the resulting disease, chikungunya fever, is found in nearly 40 countries. Neith
Design, synthesis, and biological evaluation of imidazolyl derivatives of 4,7-disubstituted coumarins as aromatase inhibitors selective over 17-α-hydroxylase/C17-20 lyase
Stefanachi, Angela,Favia, Angelo D.,Nicolotti, Orazio,Leonetti, Francesco,Pisani, Leonardo,Catto, Marco,Zimmer, Christina,Hartmann, Rolf W.,Carotti, Angelo
experimental part, p. 1613 - 1625 (2011/06/19)
The design, synthesis, and biological evaluation of a series of new aromatase (AR, CYP19) inhibitors bearing an imidazole ring linked to a 7-substituted coumarin scaffold at position 4 (or 3) are reported. Many compounds exhibited an aromatase inhibitory potency in the nanomolar range along with a high selectivity over 17-α-hydroxylase/C17-20 lyase (CYP17). The most potent AR inhibitor was the 7-(3,4-difluorophenoxy)-4-imidazolylmethyl coumarin 24 endowed with an IC50 = 47 nM. Docking simulations on a selected number of coumarin derivatives allowed the identification of the most important interactions driving the binding and clearly indicated the allowed and disallowed regions for appropriate structural modifications of coumarins and closely related heterocyclic molecular scaffolds.
