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10.1021/ml200126j http://scihub22266oqcxt.onion/10.1021/ml200126j C4018126!4018126!24900269     free     free     free Deprecated: Implicit conversion from float 231.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 231.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 231.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 231.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 231.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534       ACS+Med+Chem+Lett 2011 ; 2 (11): 809-13 Nephropedia Template TP {{tp|p=24900269|t=2011. Highly Selective and Potent Thiophenes as PI3K Inhibitors with Oral Antitumor Activity |pdf=|usr=}}{{24900269}} gab.com Text Highly Selective and Potent Thiophenes as PI3K Inhibitors with Oral Antitumor Activity JO: ACS Med Chem Lett http://www.kidney.de/pget.php?&tw=1&pmid=24900269 #FOAvip Highly selective PI3K inhibitors with subnanomolar PI3K? potency and greater than 7000-fold selectivity against mTOR kinase were discovered through structure-based drug design (SBDD). These tetra-substituted thiophenes were also demonstrated to have good in vitro cellular potency and good in vivo oral antitumor activity in a mouse PI3K driven NCI-H1975 xenograft tumor model. Compounds with the desired human PK predictions and good in vitro ADMET properties were also identified. In this communication, we describe the rationale behind the installation of a critical triazole moiety to maintain the intricate H-bonding network within the PI3K receptor leading to both better potency and selectivity. Furthermore, optimization of the C-4 phenyl group was exploited to maximize the compounds mTOR selectivity. Twit Text FOAVip Highly Selective and Potent Thiophenes as PI3K Inhibitors with Oral Antitumor Activity ????ACS Med Chem Lett http://www.kidney.de/pget.php?&tw=1&pmid=24900269 #FOAvip Twit Text # Free Paper on # # # # # LINK http://www.kidney.de/pget.php?&tw=1&pmid=24900269 #FOAvip English Wikipedia <ref>{{Cite pmid|24900269}}</ref> Highly Selective and Potent Thiophenes as PI3K Inhibitors with Oral Antitumor Activity #MMPMID24900269 Liu KKC; Zhu J; Smith GL; Yin MJ; Bailey S; Chen JH; Hu Q; Huang Q; Li C; Li QJ; Marx MA; Paderes G; Richardson PF; Sach NW; Walls M; Wells PA; Zou A ACS Med Chem Lett 2011[Nov]; 2 (11): 809-13 PMID24900269show ga Highly selective PI3K inhibitors with subnanomolar PI3K? potency and greater than 7000-fold selectivity against mTOR kinase were discovered through structure-based drug design (SBDD). These tetra-substituted thiophenes were also demonstrated to have good in vitro cellular potency and good in vivo oral antitumor activity in a mouse PI3K driven NCI-H1975 xenograft tumor model. Compounds with the desired human PK predictions and good in vitro ADMET properties were also identified. In this communication, we describe the rationale behind the installation of a critical triazole moiety to maintain the intricate H-bonding network within the PI3K receptor leading to both better potency and selectivity. Furthermore, optimization of the C-4 phenyl group was exploited to maximize the compounds mTOR selectivity. äHighly Selective and Potent Thiophenes as PI3K Inhibitors with Oral An(epmc).pdf DeepDyve Pubget Overpricing