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10.1021/ml300471d http://scihub22266oqcxt.onion/10.1021/ml300471d C4027490!4027490 !24900700     free     free     free Warning: file_get_contents(https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pubmed&id=24900700 &cmd=llinks): Failed to open stream: HTTP request failed! HTTP/1.1 429 Too Many Requests in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 215       ACS+Med+Chem+Lett 2013 ; 4 (6 ): 504-8 Nephropedia Template TP {{tp|p=24900700 |t=2013. Identification of New Nonsteroidal ROR? Ligands; Related Structure-Activity Relationships and Docking Studies |pdf=|usr=}}{{24900700 }} gab.com Text Identification of New Nonsteroidal ROR Ligands; Related Structure-Activity Relationships and Docking Studies JO: ACS Med Chem Lett http://www.kidney.de/pget.php?&tw=1&pmid=24900700 #FOAvip A high throughput screen was developed to identify novel, nonsteroidal ROR? agonists. Among the validated hit compounds, the 4-(4-(benzyloxy)phenyl)-5-carbonyl-2-oxo-1,2,3,4-tetrahydropyrimidine scaffold was the most prominent. Among the numerous analogues tested, compounds 8 and 9 showed the highest activity. Key structure-activity relationships (SAR) were established, where benzyl and urea moieties were both identified as very important elements to maintain the activity. Most notably, the SAR were consistent with the binding mode of the compound 8 (S-isomer) in the ROR? docking model that was developed in this program. As predicted by the model, the urea moiety is engaged in the formation of key hydrogen bonds with the backbone of Tyr380 and Asp382. The benzyl group is located in a wide hydrophobic pocket. The structural relationships reported in this letter will help in further optimization of this compound series and will provide novel synthetic probes helpful for elucidation of complex ROR? physiopathology. Twit Text FOAVip Identification of New Nonsteroidal ROR Ligands; Related Structure-Activity Relationships and Docking Studies ????ACS Med Chem Lett http://www.kidney.de/pget.php?&tw=1&pmid=24900700 #FOAvip Twit Text # Free Paper on # # # # # LINK http://www.kidney.de/pget.php?&tw=1&pmid=24900700 #FOAvip English Wikipedia <ref>{{Cite pmid|24900700 }}</ref> Identification of New Nonsteroidal ROR? Ligands; Related Structure-Activity Relationships and Docking Studies #MMPMID24900700 Dubernet M ; Duguet N ; Colliandre L ; Berini C ; Helleboid S ; Bourotte M ; Daillet M ; Maingot L ; Daix S ; Delhomel JF ; Morin-Allory L ; Routier S ; Walczak R ACS Med Chem Lett 2013[Jun]; 4 (6 ): 504-8 PMID24900700 show ga A high throughput screen was developed to identify novel, nonsteroidal ROR? agonists. Among the validated hit compounds, the 4-(4-(benzyloxy)phenyl)-5-carbonyl-2-oxo-1,2,3,4-tetrahydropyrimidine scaffold was the most prominent. Among the numerous analogues tested, compounds 8 and 9 showed the highest activity. Key structure-activity relationships (SAR) were established, where benzyl and urea moieties were both identified as very important elements to maintain the activity. Most notably, the SAR were consistent with the binding mode of the compound 8 (S-isomer) in the ROR? docking model that was developed in this program. As predicted by the model, the urea moiety is engaged in the formation of key hydrogen bonds with the backbone of Tyr380 and Asp382. The benzyl group is located in a wide hydrophobic pocket. The structural relationships reported in this letter will help in further optimization of this compound series and will provide novel synthetic probes helpful for elucidation of complex ROR? physiopathology. ?Identification of New Nonsteroidal ROR? Ligands; Related Structure-Act(epmc).pdf DeepDyve Pubget Overpricing