Synthesis and Biological Evaluation of Novel Betulin Derivatives with Aromatic Hydrazone Side Chain as Potential Anticancer Agents

Abstract

A series of novel betulin-28-hydrazone derivatives (7a-7o) were synthesized. All compounds were evaluated for their in vitro cytotoxicities in four human carcinoma cells (HepG2, MCF-7, HCT-116 and A549). Among them, compound 7l displayed the most potent cytotoxicity with an IC50 (concentration of the tested compound that inhibits 50% of cell growth) value of 7.37 ± 0.38 μM against MCF-7 cells. The preliminary cellular mechanism studies indicated that compound 7l could induce MCF-7 cells apoptosis. The above findings indicated that compound 7l may be used as a lead compound for antitumor agents with improved efficacy.

Chemical Characterization, Phenolic Compounds Quantification, and Assessment of Antioxidant and Anti‐Acetylcholinesterase Activities of Byrsonima sericea DC fruits

“…Betulin belongs to the lupane class and is widespread in nature, especially found in the bark of the species Betula pendula Roth. It has broad biological activities including anti‐inflammatory, antitumor and antibacterial [22,23] …”

“…It has broad biological activities including antiinflammatory, antitumor and antibacterial. [22,23] α-Amyrin is an ursane-class triterpene, while β-amyrin is an olean-class isomer. They are found especially in species of the genus Protium.…”