On January 1, 2010, Wang, Haofan; Byun, Youngjoo; Barinka, Cyril; Pullambhatla, Mrudula; Bhang, Hyo-eun C.; Fox, James J.; Lubkowski, Jacek; Mease, Ronnie C.; Pomper, Martin G. published an article.Synthetic Route of 32462-30-9 The title of the article was Bioisosterism of urea-based GCPII inhibitors: Synthesis and structure-activity relationship studies. And the article contained the following:
We report a strategy based on bioisosterism to improve the physicochem. properties of existing hydrophilic, urea-based GCPII inhibitors. Comprehensive structure-activity relation studies of the P1′ site of ZJ-43- and DCIBzL-based compounds identified several glutamate-free inhibitors with Ki values below 20 nM. Among them, compound 32d (Ki = 11 nM) exhibited selective uptake in GCPII-expressing tumors by SPECT-CT imaging in mice. A novel conformational change of amino acids in the S1′ pharmacophore pocket was observed in the x-ray crystal structure of GCPII complexed with 32d. The experimental process involved the reaction of H-Phg(4-OH)-OH(cas: 32462-30-9).Synthetic Route of 32462-30-9
The Article related to gcpii inhibitor urea derivative bioisosterism preparation structure activity, Pharmacology: Structure-Activity and other aspects.Synthetic Route of 32462-30-9
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