Discovery of N-hydroxy-3-alkoxybenzamides as direct acid sphingomyelinase inhibitors using a ligand-based pharmacophore model.

Acid sphingomyelinase (ASM) has been shown to be involved in many physiological processes, emerging to be a promising drug target. In this study, we constructed a ligand-based pharmacophore model of ASM inhibitors and applied this model to optimize the lead compound α-mangostin, a known inhibitor of ASM. 23 compounds were designed and evaluated in vitro for ASM inhibition, of these, 10 compounds were found to be more potent than α-mangostin.

Synthesis and biological evaluation of novel tanshinone IIA derivatives for treating pain.

Due to ineffectiveness and side effects of existing analgesics, chronic pain has become one of the most complex and difficult problems in the clinic. Monoacylglycerol lipase (MAGL) is an essential hydrolase in the endocannabinoid system and has been identified as a potential target for the treatment of pain. In the present study, we designed and synthesized twelve tanshinone IIA analogs and screened their activity against MAGL.

I-Catalyzed cross dehydrogenative coupling: rapid access to benzoxazinones and quinazolinones.

An efficient and applicable I-catalyzed intramolecular dehydrogenative C-O/C-N coupling reaction via activating the C-H bond adjacent to the N atom has been developed to provide dozens of substituted benzoxazinones (31 examples) and quinazolinones (5 examples) in good to excellent yields (up to 98%). This one-pot methodology has significant advantages, including a metal-free process, broad substrate scope, high atom economy, and simple operation. This strategy goes through an iminium intermediate followed by nucleophilic attack to provide the desired products.

Synthesis and biological evaluation of tanshinone IIA derivatives as novel endothelial protective agents.

Aim: Oxidative stress-induced endothelial injury is a main risk factor in the pathogenesis of cardiovascular diseases. Tanshinone IIA (Tan IIA) exerts protective functions on endothelial cells in response to oxidative stress. To exploit new bioactive compounds from this natural product, 12 derivatives were first synthesized and evaluated for endothelial protective activities.

Pharmacology of mangostins and their derivatives: A comprehensive review.

Mangosteen (Garcinia mangostana Linn.) is a well-known tropical tree indigenous to Southeast Asia. Its fruit's pericarp abounds with a class of isoprenylated xanthones which are referred as mangostins.

Anticarcinogenic Effects of α-Mangostin: A Review.

Cancer chemoprevention is a promising strategy taken to block, reverse, or retard carcinogenesis. -Mangostin, a natural xanthone isolated from the pericarps of mangosteen, represents one of the most studied chemopreventive agents. This compound has been reported to interfere with all the major stages of carcinogenesis: initiation, promotion, and progression.