Miyakoshi, Hitoshi published the artcile1,2,3-Triazole-Containing Uracil Derivatives with Excellent Pharmacokinetics as a Novel Class of Potent Human Deoxyuridine Triphosphatase Inhibitors, Recommanded Product: 2-(3-(Benzyloxy)phenyl)acetic acid, the publication is Journal of Medicinal Chemistry (2012), 55(14), 6427-6437, database is CAplus and MEDLINE.
Deoxyuridine triphosphatase (dUTPase) has emerged as a potential target for drug development as a 5-fluorouracil-based combination chemotherapy. The design and synthesis of a novel class of human dUTPase inhibitors, 1,2,3-triazole-containing uracil derivatives, is described. Compound I, which possesses 1,5-disubstituted 1,2,3-triazole moiety that mimics the amide bond of tert-amide-containing inhibitor II locked in a cis conformation showed potent inhibitory activity, and its structure-activity relationship studies led us to the discovery of highly potent inhibitors III and IV (IC50 = ?0.029 ¦ÌM). These derivatives dramatically enhanced the growth inhibition activity of 5-fluoro-2′-deoxyuridine against HeLa S3 cells in vitro (EC50 = ?0.05 ¦ÌM). In addition, compound IV exhibited a markedly improved pharmacokinetic profile as a result of the introduction of a benzylic hydroxy group and significantly enhanced the antitumor activity of 5-fluorouracil against human breast cancer MX-1 xenograft model in mice. These data indicate that IV is a promising candidate for combination cancer chemotherapies with TS inhibitors.
Journal of Medicinal Chemistry published new progress about 1860-58-8. 1860-58-8 belongs to catalysis-chemistry, auxiliary class Carboxylic acid,Benzene,Ether, name is 2-(3-(Benzyloxy)phenyl)acetic acid, and the molecular formula is C15H14O3, Recommanded Product: 2-(3-(Benzyloxy)phenyl)acetic acid.
Referemce:
https://courses.lumenlearning.com/boundless-chemistry/chapter/catalysis/,
Catalysis – Wikipedia