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- W2127377844 abstract "2,3-Seco-dioic acids derived from four different triterpene skeletons were prepared and evaluated for their anti-HIV-1 protease activity. Two A-seco derivatives showed potent inhibitory activity against HIV-1 protease (3c and 3e, IC50 5.7 and 3.9 μM, respectively), while four other derivatives showed moderate to weak inhibition (3a, 3b, 3d and 3f, IC50 15.7–88.1 μM). The combination of a 2,3-seco-2,3-dioic acid functional group in ring A and a free acid group at C-28 or C-30 significantly enhanced HIV-1 protease inhibitory activity (3a, 3c–3e, IC50 3.9–17.6 μM). On the other hand, all A-seco derivatives were found to be very weak inhibitors of HCV, renin and trypsin proteases (IC50 > 80 μM). These findings indicate that A-seco triterpenes with a carboxyl group at C-28 or C-30 are novel and highly selective HIV-1 protease inhibitors." @default.
- W2127377844 created "2016-06-24" @default.
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- W2127377844 date "2009-10-01" @default.
- W2127377844 modified "2023-10-14" @default.
- W2127377844 title "Synthesis and evaluation of A-seco type triterpenoids for anti-HIV-1protease activity" @default.
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- W2127377844 doi "https://doi.org/10.1016/j.ejmech.2009.05.002" @default.
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