87980-68-5Relevant articles and documents
Identification, structural modification, and dichotomous effects on human immunodeficiency virus type 1 (HIV-1) replication of ingenane esters from Euphorbia kansui
Liu, Qingbo,Li, Wei,Huang, Li,Asada, Yoshihisa,Morris-Natschke, Susan L.,Chen, Chin-Ho,Lee, Kuo-Hsiung,Koike, Kazuo
supporting information, p. 618 - 627 (2018/07/29)
Euphorbia kansui showed potent anti-HIV-1 activity during screening of a library composed of plant extracts from Euphorbiaceae and Thymelaeaceae families. Bioassay-guided isolation led to identification of ingenane esters as the active compounds. Further chemical modification resulted in 3-(2-naphthoyl)ingenol (23), which exhibited the most potent anti-HIV-1 activity. Compound 23 also acted as an HIV-1-latency-reversing agent on activation of HIV-1 replication in a latently infected U1 cell model and a T cell latent HIV-1 model JLat-A2.
Semisynthesis of ingenol 3-angelate (PEP005): Efficient stereoconservative angeloylation of alcohols
Liang, Xifu,Grue-Sorensen, Gunnar,Petersen, Anders Klarskov,H?gberg, Thomas
, p. 2647 - 2652 (2013/01/15)
A high-yielding method was developed for the preparation of ingenol 3-angelate (PEP005, ingenol mebutate) via the corresponding 5,20-acetonide without concomitant isomerization of the angelate (Z-form) to the corresponding tiglate (E-form). The general sc
INGENOL-3-ACYLATES I
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Page/Page column 37-38, (2012/07/13)
The invention relates to compounds of general formula (I) wherein R is (C1-C7)alkyl, (C2-C7)alkenyl or (C2-C7)alkynyl; wherein R is substituted with R1; and pharmaceutically acceptable salt