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Page 1
Discovery of highly selective and orally active lysophosphatidic acid receptor-1 antagonists with potent activity on human lung fibroblasts.
Qian Y, Hamilton M, Sidduri A, Gabriel S, Ren Y, Peng R, Kondru R, Narayanan A, Truitt T, Hamid R, Chen Y, Zhang L, Fretland AJ, Sanchez RA, Chang KC, Lucas M, Schoenfeld RC, Laine D, Fuentes ME, Stevenson CS, Budd DC. Qian Y, et al. Among authors: kondru r. J Med Chem. 2012 Sep 13;55(17):7920-39. doi: 10.1021/jm301022v. Epub 2012 Aug 29. J Med Chem. 2012. PMID: 22894757
Potent and highly selective benzimidazole inhibitors of PI3-kinase delta.
Murray JM, Sweeney ZK, Chan BK, Balazs M, Bradley E, Castanedo G, Chabot C, Chantry D, Flagella M, Goldstein DM, Kondru R, Lesnick J, Li J, Lucas MC, Nonomiya J, Pang J, Price S, Salphati L, Safina B, Savy PP, Seward EM, Ultsch M, Sutherlin DP. Murray JM, et al. Among authors: kondru r. J Med Chem. 2012 Sep 13;55(17):7686-95. doi: 10.1021/jm300717c. Epub 2012 Aug 21. J Med Chem. 2012. PMID: 22877085
Structure-based drug design of RN486, a potent and selective Bruton's tyrosine kinase (BTK) inhibitor, for the treatment of rheumatoid arthritis.
Lou Y, Han X, Kuglstatter A, Kondru RK, Sweeney ZK, Soth M, McIntosh J, Litman R, Suh J, Kocer B, Davis D, Park J, Frauchiger S, Dewdney N, Zecic H, Taygerly JP, Sarma K, Hong J, Hill RJ, Gabriel T, Goldstein DM, Owens TD. Lou Y, et al. Among authors: kondru rk. J Med Chem. 2015 Jan 8;58(1):512-6. doi: 10.1021/jm500305p. Epub 2014 Apr 16. J Med Chem. 2015. PMID: 24712864
Potent and selective inhibitors of PI3Kδ: obtaining isoform selectivity from the affinity pocket and tryptophan shelf.
Sutherlin DP, Baker S, Bisconte A, Blaney PM, Brown A, Chan BK, Chantry D, Castanedo G, DePledge P, Goldsmith P, Goldstein DM, Hancox T, Kaur J, Knowles D, Kondru R, Lesnick J, Lucas MC, Lewis C, Murray J, Nadin AJ, Nonomiya J, Pang J, Pegg N, Price S, Reif K, Safina BS, Salphati L, Staben S, Seward EM, Shuttleworth S, Sohal S, Sweeney ZK, Ultsch M, Waszkowycz B, Wei B. Sutherlin DP, et al. Among authors: kondru r. Bioorg Med Chem Lett. 2012 Jul 1;22(13):4296-302. doi: 10.1016/j.bmcl.2012.05.027. Epub 2012 May 17. Bioorg Med Chem Lett. 2012. PMID: 22672799
A Crowd-Based Process and Tool for HTS Hit Triage.
Peng Z, Gillespie P, Weisel M, So SS, So WV, Kondru R, Narayanan A, Hermann JC. Peng Z, et al. Among authors: kondru r. Mol Inform. 2013 Apr;32(4):337-45. doi: 10.1002/minf.201200154. Epub 2013 Apr 9. Mol Inform. 2013. PMID: 27481590 No abstract available.
Discovery of novel PI3-kinase δ specific inhibitors for the treatment of rheumatoid arthritis: taming CYP3A4 time-dependent inhibition.
Safina BS, Baker S, Baumgardner M, Blaney PM, Chan BK, Chen YH, Cartwright MW, Castanedo G, Chabot C, Cheguillaume AJ, Goldsmith P, Goldstein DM, Goyal B, Hancox T, Handa RK, Iyer PS, Kaur J, Kondru R, Kenny JR, Krintel SL, Li J, Lesnick J, Lucas MC, Lewis C, Mukadam S, Murray J, Nadin AJ, Nonomiya J, Padilla F, Palmer WS, Pang J, Pegg N, Price S, Reif K, Salphati L, Savy PA, Seward EM, Shuttleworth S, Sohal S, Sweeney ZK, Tay S, Tivitmahaisoon P, Waszkowycz B, Wei B, Yue Q, Zhang C, Sutherlin DP. Safina BS, et al. Among authors: kondru r. J Med Chem. 2012 Jun 28;55(12):5887-900. doi: 10.1021/jm3003747. Epub 2012 Jun 11. J Med Chem. 2012. PMID: 22626259
Finding the perfect spot for fluorine: improving potency up to 40-fold during a rational fluorine scan of a Bruton's Tyrosine Kinase (BTK) inhibitor scaffold.
Lou Y, Sweeney ZK, Kuglstatter A, Davis D, Goldstein DM, Han X, Hong J, Kocer B, Kondru RK, Litman R, McIntosh J, Sarma K, Suh J, Taygerly J, Owens TD. Lou Y, et al. Among authors: kondru rk. Bioorg Med Chem Lett. 2015 Jan 15;25(2):367-71. doi: 10.1016/j.bmcl.2014.11.030. Epub 2014 Nov 20. Bioorg Med Chem Lett. 2015. PMID: 25466710
Evaluation of amide replacements in CCR5 antagonists as a means to increase intrinsic permeability. Part 2: SAR optimization and pharmacokinetic profile of a homologous azacyle series.
Wanner J, Chen L, Lemoine RC, Kondru R, Jekle A, Heilek G, deRosier A, Ji C, Berry PW, Rotstein DM. Wanner J, et al. Among authors: kondru r. Bioorg Med Chem Lett. 2010 Nov 15;20(22):6802-7. doi: 10.1016/j.bmcl.2010.08.118. Epub 2010 Sep 18. Bioorg Med Chem Lett. 2010. PMID: 20855212
24 results