A series of pyridine chalcone derivatives were designed and synthesized. The structures were confirmed by 1 H NMR, 13 C NMR and HRMS. In vitro biological activity evaluation results showed that five of the compounds exhibited good biological activity against gram positive bacteria staphylococcus aureus (ATCC 29213). Further antibiotic activity of these five compounds against 11 clinical isolated methicillin-resistant staphylococcus aureus (MRSA) were evaluated. The results showed that four of the compounds exhibited good antibacterial activity against MRSA. (E)-2-Bromo-N-{4-[3-(pyridin-2-yl)acryloyl]phenyl}acetamide (5k) showed the most effective activity (minimum inhibitory concentration, MIC=4 μg/mL). In terms of hemolytic activity evaluation, compound 5k showed virtually no toxicity even in 1000 μg/mL concentration. To sum up, pyridine chalcone 5k was potential for further antibiotic study as anti-MRSA agent.
Jaspine B is a natural product with significant antitumor activity, which was isolated from the marine sponge Pachastrissa sp. In order to find new antitumor compounds with high efficiency and succinct synthetic methods, a series of 3-epi-jaspine B analogues were designed and synthesized. 16 compounds were synthesized and all of them were unknown in the literature. Their structures were determined by 1 H NMR, 13 C NMR and HRMS. The antitumor activity of these compounds against four tumor cell lines B16-F10, A-549, MCF-7 and PC-3 was assayed using thiazolyl blue (MTT) assay, and some compounds showed potent inhibitory effect on tumor cells. Compounds 8f and 11 were more potent against A-549 with IC 50 of (9.646±0.984) and (7.144±0.854) μg/mL.
scite is a Brooklyn-based organization that helps researchers better discover and understand research articles through Smart Citations–citations that display the context of the citation and describe whether the article provides supporting or contrasting evidence. scite is used by students and researchers from around the world and is funded in part by the National Science Foundation and the National Institute on Drug Abuse of the National Institutes of Health.