Wang, Shengzheng published the artcileScaffold diversity inspired by the natural product evodiamine: discovery of highly potent and multitargeting antitumor agents, Recommanded Product: 2-Hydroxy-4-(trifluoromethyl)benzoic acid, the publication is Journal of Medicinal Chemistry (2015), 58(16), 6678-6696, database is CAplus and MEDLINE.
A critical question in natural product-based drug discovery is how to translate the product into drug-like mols. with optimal pharmacol. properties. The generation of natural product-inspired scaffold diversity is an effective but challenging strategy to investigate the broader chem. space and identify promising drug leads. Extending the efforts to the natural product evodiamine, a diverse library containing 11 evodiamine-inspired novel scaffolds and their derivatives were designed and synthesized. Most of them showed good to excellent antitumor activity against various human cancer cell lines. In particular, 3-chloro-10-hydroxyl thio-evodiamine I showed excellent in vitro and in vivo antitumor efficacy with good tolerability and low toxicity. Antitumor mechanism and target profiling studies indicate that compound I is the first-in-class triple topoisomerase I/topoisomerase II/tubulin inhibitor. Overall, this study provided an effective strategy for natural product-based drug discovery.
Journal of Medicinal Chemistry published new progress about 328-90-5. 328-90-5 belongs to alcohols-buliding-blocks, auxiliary class Trifluoromethyl,Fluoride,Carboxylic acid,Benzene,Phenol, name is 2-Hydroxy-4-(trifluoromethyl)benzoic acid, and the molecular formula is C14H17BFNO2, Recommanded Product: 2-Hydroxy-4-(trifluoromethyl)benzoic acid.
Referemce:
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