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Chrysin, a natural flavonoid, has been investigated for its anticancer biological properties. Antifungal and anticancer properties of hydrazone derivatives have been proven. In this study, eight compounds of substituted Chrysin hydrazine derivatives have been designed, synthesized, and screened against cancerous cell lines, including MCF-7 and HepG-2. All products are reported for the first time. Most compounds exhibited significant cytotoxic activity against selected cell lines. The chemical structures of all compounds were confirmed by spectroscopic methods and elemental analyzes. In vitro evaluation of these synthesized compounds showed most of them have potential antiproliferative activity. Compounds 3e and 3f have shown significant anti-proliferative activity against MCF-7 and HepG-2 cell lines, respectively, compared to Chrysin (P < 0.05). The IC50 values of compounds 3e and 3f were 101.44 and 166.19 µM after 48 h, respectively. Moreover, the compounds 3e and 3f induced significant apoptosis more than Chrysin (P < 0.05). The Results of this research might help the design and synthesis of novel drugs toward developing new antitumor agents for cancer treatment. [ABSTRACT FROM AUTHOR]

A series of novel tetrahydropyrimidin-4-yl)pyridine derivatives 6(a–h) have been designed and synthesized as inhibitors of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE). The chemical structures of all newly synthesized compounds were characterized by spectroscopic methods (IR, 1H NMR, 13C NMR) and elemental analyzes. The in vitro studies showed that all the synthesized derivatives showed significant BChE inhibitory activity more potent than donepezil as the standard (IC50 values less than 0.1 µM). All the target compounds demonstrated good AChE inhibitory effects comparable with donepezil as the reference drug with IC50 values ranging from 0.08 to 0.1 µM. The best results were obtained by 4-methyl substituted derivative 6d with IC50 value of 0.082 µM which was comparable with AChE inhibitory effects of donepezil (IC50 = 0.079 µM). [ABSTRACT FROM AUTHOR]