Abstract:
:Four types of piscidinol A derivatives were synthesized and evaluated their ability to inhibit HIV-1 protease to understand their structure-activity relationships. Of these tirucallane-type triterpene derivatives, an A-seco derivative (1b) moderately inhibited human immunodeficiency virus (HIV) protease (IC50 38.2 μM). The 2,2-dimethyl succinic acid (DMS) acylated tirucallane derivatives (4b, 6a, and 7b, 50 < IC50 < 100 μM) were more inhibitory against HIV-1 PR than the others (PA, 2a, 4a, 4c-4d, 5a, 6b-6d, and 7a, IC50 > 100 μM). These findings indicated that the 2,3-seco-2,3-dioic acid (1b) and DMS-acylated tirucallane-type derivatives preferably inhibited HIV viral protease.
journal_name
J Asian Nat Prod Resjournal_title
Journal of Asian natural products researchauthors
Wei Y,Ma CM,Jiang TB,Du J,Zhou X,Liu GQ,Hattori Mdoi
10.1080/10286020.2015.1084505subject
Has Abstractpub_date
2015-01-01 00:00:00pages
1079-90issue
11eissn
1028-6020issn
1477-2213journal_volume
17pub_type
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