136850-48-1Relevant articles and documents
Studies on synthesis and biological activity of oxidative aglafolin derivatives
Wang, Xianyou,Xie, Zhuoqun,Fu, Bin,Li, Nan,Wang, Mingan,Ma, Yongqiang,Du, Fengpei,Xu, Yanjun,Qin, Zhaohai
, p. 1430 - 1434 (2015)
The synthesis of the key intermediate of rocaglamide, oxidative aglafolin, was studied, and its diastereoisomers were obtained. The amination of oxidative aglafolin was also investigated, affording amino derivatives. The preliminary bioassay results indic
COMPOSITIONS AND METHODS FOR INHIBITING VIRAL INFECTION
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Paragraph 0507-0508, (2020/05/06)
Described herein are compounds, agents, compositions, and methods related to the treatment of a viral infection (e.g., Hepatitis C viral infection). In particular, the compounds, agents, compositions, and methods described herein inhibit viral entry into a target cell.
Chemical Synthesis Enables Structural Reengineering of Aglaroxin C Leading to Inhibition Bias for Hepatitis C Viral Infection
Zhang, Wenhan,Liu, Shufeng,Maiga, Rayelle I.,Pelletier, Jerry,Brown, Lauren E.,Wang, Tony T.,Porco, John A.
, p. 1312 - 1323 (2019/01/21)
As a unique rocaglate (flavagline) natural product, aglaroxin C displays intriguing biological activity by inhibiting hepatitis C viral entry. To further elucidate structure-activity relationships and diversify the pyrimidinone scaffold, we report a concise synthesis of aglaroxin C utilizing a highly regioselective pyrimidinone condensation. We have prepared more than 40 aglaroxin C analogues utilizing various amidine condensation partners. Through biological evaluation of analogues, we have discovered two lead compounds, CMLD012043 and CMLD012044, which show preferential bias for the inhibition of hepatitis C viral entry vs translation inhibition. Overall, the study demonstrates the power of chemical synthesis to produce natural product variants with both target inhibition bias and improved therapeutic indexes.
