Design, synthesis and biological evaluation of novel HIV-1 protease inhibitors with pentacyclic triterpenoids as P2-ligands. Issue 3 (1st February 2019)

• Record Type: Journal Article
• Authors: Zhu, Mei; Du, Xiao-Nan; Li, Yun-Ge; Zhang, Guo-Ning; Wang, Ju-Xian; Wang, Yu-Cheng
• Is Part Of: Bioorganic & medicinal chemistry letters. Volume 29:Issue 3(2019)
• Page Start: 357
• Page End: 361
• Publication Date: 2019-02-01
• Subjects: HIV-1 protease inhibitors -- P2 ligand -- Pentacyclic triterpenoids; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1016/j.bmcl.2018.12.040
• Languages: English
• ISSNs: 0960-894X

Abstract

Graphical abstract: Abstract: The design, synthesis and SAR study of a new series of HIV-1 protease inhibitors with pentacyclic triterpenoids as P2 ligands and phenylsulfonamide as P2′ ligands were discussed. These compounds exhibited micromolar inhibitory potency, among which compound T1c displayed HIV-1 protease inhibition with IC50 values of 0.12 μM, which was 67 times the inhibitory activity of its raw material Ursolic acid (8.0 μM).