94739-93-2Relevant academic research and scientific papers
Synthesis, computational studies and assessment of in vitro inhibitory activity of umbelliferon-based compounds against tumour-associated carbonic anhydrase isoforms IX and XII
Angeli, Andrea,Capasso, Clemente,De Luca, Laura,Del Prete, Sonia,Gitto, Rosaria,Mancuso, Francesca,Supuran, Claudiu T.
, p. 1442 - 1449 (2020/07/13)
Coumarins are widely diffused secondary metabolites possessing a plethora of biological activities. It has been established that coumarins represent a peculiar class of human carbonic anhydrase (hCA) inhibitors having a distinct mechanism of action involv
Anti-influenza drug discovery: Structure-activity relationship and mechanistic insight into novel angelicin derivatives
Yeh, Jiann-Yih,Coumar, Mohane Selvaraj,Horng, Jim-Tong,Shiao, Hui-Yi,Kuo, Fu-Ming,Lee, Hui-Ling,Chen, In-Chun,Chang, Chun-Wei,Tang, Wen-Fang,Tseng, Sung-Nain,Chen, Chi-Jene,Shih, Shin-Ru,Hsu, John T.-A.,Liao, Chun-Chen,Chao, Yu-Sheng,Hsieh, Hsing-Pang
experimental part, p. 1519 - 1533 (2010/08/20)
By using a cell-based high throughput screening campaign, a novel angelicin derivative 6a was identified to inhibit influenza A. (H1N1) virus induced cytopathic effect in Madin-Darby canine kidney cell culture in low micromolar range. Detailed structure-activity relationship studies of 6a revealed that the angelicin scaffold is essential for activity in pharmacophore B, while meta-substituted phenyl/2-thiophene rings are optimal in pharmacophore A and C. The optimized lead 4-methyl-9-phenyl-8-(thiophene-2-carbonyl)-furo[2,3-h] chromen-2-one (8g, IC50 = 70 nM) showed 64-fold enhanced activity compared to the high throughput screening (HTS) hit 6a. Also, 8g was found effective in case of influenza A (H3N2) and influenza B virus strains similar to approved anti-influenza drug zanamivir (4). Preliminary mechanistic studies suggest that these compounds act as anti-influenza agents by inhibiting ribonucleoprotein (RNP) complex associated activity and have the potential to be developed further, which could form the basis for developing additional defense against influenza pandemics.
