AI Article Synopsis
- Three new diterpenes, stellejasmins A and B, and 12--benzoylphorbol-13-heptanoate, were isolated from the roots of a plant and their structures determined using NMR and mass spectroscopy.
- The two diterpenes are notable for being the first in their family to possess a hydroxy group at C-2, with one compound containing a unique chlorine atom.
- Their potential as HIV inhibitors was tested alongside other diterpenes, revealing several with high potency, and marking the first structure-activity relationship study on natural daphnane and tigliane diterpenes.
Article Abstract
Three new diterpenes, stellejasmins A () and B () and 12--benzoylphorbol-13-heptanoate (), were isolated from the roots of L. The structures of - were elucidated by extensive NMR and mass spectroscopic analyses. Compounds and are the first derivatives containing a hydroxy group at C-2 in the family of daphnane and tigliane diterpenes. The presence of a chlorine atom in is unique in the plant metabolite. Compound has an odd-number acyl group, which is biosynthetically notable. Human immunodeficiency virus (HIV) LTR-driven transcription activity was tested with - and 17 known diterpenes isolated from L. and A.Gray. Among these, gnidimacrin (), stelleralide A (), and wikstroelide A () were highly potent, with EC values of 0.14, 0.33, and 0.39 nM, respectively. The structure-activity relationship (SAR) was investigated using 20 natural and eight synthetic diterpenes. This is the first SAR study on natural daphnane and tigliane diterpenes.
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| http://dx.doi.org/10.1021/acs.jmedchem.1c01973 | DOI Listing |
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