Kania R - Search Results

1

Design strategies to target crystallographic waters applied to the Hsp90 molecular chaperone.

Kung PP, Sinnema PJ, Richardson P, Hickey MJ, Gajiwala KS, Wang F, Huang B, McClellan G, Wang J, Maegley K, Bergqvist S, Mehta PP, Kania R. Kung PP, et al. Among authors: kania r. Bioorg Med Chem Lett. 2011 Jun 15;21(12):3557-62. doi: 10.1016/j.bmcl.2011.04.130. Epub 2011 May 5. Bioorg Med Chem Lett. 2011. PMID: 21612924

2

Structure-based design and synthesis of (5-arylamino-2H-pyrazol-3-yl)-biphenyl-2',4'-diols as novel and potent human CHK1 inhibitors.

Teng M, Zhu J, Johnson MD, Chen P, Kornmann J, Chen E, Blasina A, Register J, Anderes K, Rogers C, Deng Y, Ninkovic S, Grant S, Hu Q, Lundgren K, Peng Z, Kania RS. Teng M, et al. J Med Chem. 2007 Nov 1;50(22):5253-6. doi: 10.1021/jm0704604. Epub 2007 Sep 21. J Med Chem. 2007. PMID: 17887663

3

Characterizing the effects of the juxtamembrane domain on vascular endothelial growth factor receptor-2 enzymatic activity, autophosphorylation, and inhibition by axitinib.

Solowiej J, Bergqvist S, McTigue MA, Marrone T, Quenzer T, Cobbs M, Ryan K, Kania RS, Diehl W, Murray BW. Solowiej J, et al. Biochemistry. 2009 Jul 28;48(29):7019-31. doi: 10.1021/bi900522y. Biochemistry. 2009. PMID: 19526984

4

Optimization of potent, selective, and orally bioavailable pyrrolodinopyrimidine-containing inhibitors of heat shock protein 90. Identification of development candidate 2-amino-4-{4-chloro-2-[2-(4-fluoro-1H-pyrazol-1-yl)ethoxy]-6-methylphenyl}-N-(2,2-difluoropropyl)-5,7-dihydro-6H-pyrrolo[3,4-d]pyrimidine-6-carboxamide.

Zehnder L, Bennett M, Meng J, Huang B, Ninkovic S, Wang F, Braganza J, Tatlock J, Jewell T, Zhou JZ, Burke B, Wang J, Maegley K, Mehta PP, Yin MJ, Gajiwala KS, Hickey MJ, Yamazaki S, Smith E, Kang P, Sistla A, Dovalsantos E, Gehring MR, Kania R, Wythes M, Kung PP. Zehnder L, et al. Among authors: kania r. J Med Chem. 2011 May 12;54(9):3368-85. doi: 10.1021/jm200128m. Epub 2011 Apr 20. J Med Chem. 2011. PMID: 21438541

5

Structure based drug design of crizotinib (PF-02341066), a potent and selective dual inhibitor of mesenchymal-epithelial transition factor (c-MET) kinase and anaplastic lymphoma kinase (ALK).

Cui JJ, Tran-Dubé M, Shen H, Nambu M, Kung PP, Pairish M, Jia L, Meng J, Funk L, Botrous I, McTigue M, Grodsky N, Ryan K, Padrique E, Alton G, Timofeevski S, Yamazaki S, Li Q, Zou H, Christensen J, Mroczkowski B, Bender S, Kania RS, Edwards MP. Cui JJ, et al. J Med Chem. 2011 Sep 22;54(18):6342-63. doi: 10.1021/jm2007613. Epub 2011 Aug 18. J Med Chem. 2011. PMID: 21812414

6

Discovery of pyrroloaminopyrazoles as novel PAK inhibitors.

Guo C, McAlpine I, Zhang J, Knighton DD, Kephart S, Johnson MC, Li H, Bouzida D, Yang A, Dong L, Marakovits J, Tikhe J, Richardson P, Guo LC, Kania R, Edwards MP, Kraynov E, Christensen J, Piraino J, Lee J, Dagostino E, Del-Carmen C, Deng YL, Smeal T, Murray BW. Guo C, et al. Among authors: kania r. J Med Chem. 2012 May 24;55(10):4728-39. doi: 10.1021/jm300204j. Epub 2012 May 14. J Med Chem. 2012. PMID: 22554206

7

Structural modifications of a 3-methoxy-2-aminopyridine compound to reduce potential for mutagenicity and time-dependent drug-drug interaction.

Palmer C, Pairish M, Kephart S, Bouzida D, Cui J, Deal J, Dong L, Gu D, Linton A, McAlpine I, Yamazaki S, Smith E, John-Baptiste A, Bagrodia S, Kania R, Guo C. Palmer C, et al. Among authors: kania r. Bioorg Med Chem Lett. 2012 Dec 15;22(24):7605-9. doi: 10.1016/j.bmcl.2012.10.011. Epub 2012 Oct 11. Bioorg Med Chem Lett. 2012. PMID: 23116892

8

Structure-based design, SAR analysis and antitumor activity of PI3K/mTOR dual inhibitors from 4-methylpyridopyrimidinone series.

Cheng H, Hoffman JE, Le PT, Pairish M, Kania R, Farrell W, Bagrodia S, Yuan J, Sun S, Zhang E, Xiang C, Dalvie D, Rahavendran SV. Cheng H, et al. Among authors: kania r. Bioorg Med Chem Lett. 2013 May 1;23(9):2787-92. doi: 10.1016/j.bmcl.2013.02.020. Epub 2013 Feb 13. Bioorg Med Chem Lett. 2013. PMID: 23506825

9

Design of potent and selective inhibitors to overcome clinical anaplastic lymphoma kinase mutations resistant to crizotinib.

Huang Q, Johnson TW, Bailey S, Brooun A, Bunker KD, Burke BJ, Collins MR, Cook AS, Cui JJ, Dack KN, Deal JG, Deng YL, Dinh D, Engstrom LD, He M, Hoffman J, Hoffman RL, Johnson PS, Kania RS, Lam H, Lam JL, Le PT, Li Q, Lingardo L, Liu W, Lu MW, McTigue M, Palmer CL, Richardson PF, Sach NW, Shen H, Smeal T, Smith GL, Stewart AE, Timofeevski S, Tsaparikos K, Wang H, Zhu H, Zhu J, Zou HY, Edwards MP. Huang Q, et al. Among authors: kania rs. J Med Chem. 2014 Feb 27;57(4):1170-87. doi: 10.1021/jm401805h. Epub 2014 Feb 6. J Med Chem. 2014. PMID: 24432909 Free article.

10

Discovery of (10R)-7-amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]-benzoxadiazacyclotetradecine-3-carbonitrile (PF-06463922), a macrocyclic inhibitor of anaplastic lymphoma kinase (ALK) and c-ros oncogene 1 (ROS1) with preclinical brain exposure and broad-spectrum potency against ALK-resistant mutations.

Johnson TW, Richardson PF, Bailey S, Brooun A, Burke BJ, Collins MR, Cui JJ, Deal JG, Deng YL, Dinh D, Engstrom LD, He M, Hoffman J, Hoffman RL, Huang Q, Kania RS, Kath JC, Lam H, Lam JL, Le PT, Lingardo L, Liu W, McTigue M, Palmer CL, Sach NW, Smeal T, Smith GL, Stewart AE, Timofeevski S, Zhu H, Zhu J, Zou HY, Edwards MP. Johnson TW, et al. Among authors: kania rs. J Med Chem. 2014 Jun 12;57(11):4720-44. doi: 10.1021/jm500261q. Epub 2014 Jun 3. J Med Chem. 2014. PMID: 24819116

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