Nitrogen-containing polyhydroxylated aromatics as HIV-1 integrase inhibitors: synthesis, structure-activity relationship analysis, and biological activity
…, P Wang, T Sanchez, F Christ, Z Debyser…
Index: Yu, Shenghui; Zhang, Linna; Yan, Shifeng; Wang, Peng; Sanchez, Tino; Christ, Frauke; Debyser, Zeger; Neamati, Nouri; Zhao, Guisen Journal of Enzyme Inhibition and Medicinal Chemistry, 2012 , vol. 27, # 5 p. 628 - 640
Full Text: HTML
Citation Number: 5
Abstract
Four series of forty-five nitrogen-containing polyhydroxylated aromatics based on caffeic acid phenethyl ester were designed and synthesized as HIV-1 integrase (IN) inhibitors. Most of these compounds inhibited IN catalytic activities in low micromolar range. Among these new analogues, compounds 9e and 9f were the most potent IN inhibitors with IC50 value of 0.7 μM against strand transfer reaction. Their key structure-activity relationships were also ...
Related Articles:
Structure-guided design of potent diazobenzene inhibitors for the BET bromodomains
[Zhang, Guangtao; Plotnikov, Alexander N.; Rusinova, Elena; Shen, Tong; Morohashi, Keita; Joshua, Jennifer; Zeng, Lei; Mujtaba, Shiraz; Ohlmeyer, Michael; Zhou, Ming-Ming Journal of Medicinal Chemistry, 2013 , vol. 56, # 22 p. 9251 - 9264]
Some Fluorine and Chlorine Derivatives of Sulfanilamidobenzenesulfonic Acids
[Suter; Weston Journal of the American Chemical Society, 1940 , vol. 62, p. 604]
[Marwaha, Sania; Uvell, Hanna; Salin, Olli; Lindgren, Anders E. G.; Silver, Jim; Elofsson, Mikael; Gylfe, Asa Antimicrobial Agents and Chemotherapy, 2014 , vol. 58, # 5 p. 2968 - 2971]