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Page 1
Inhibition of RAF Isoforms and Active Dimers by LY3009120 Leads to Anti-tumor Activities in RAS or BRAF Mutant Cancers.
Peng SB, Henry JR, Kaufman MD, Lu WP, Smith BD, Vogeti S, Rutkoski TJ, Wise S, Chun L, Zhang Y, Van Horn RD, Yin T, Zhang X, Yadav V, Chen SH, Gong X, Ma X, Webster Y, Buchanan S, Mochalkin I, Huber L, Kays L, Donoho GP, Walgren J, McCann D, Patel P, Conti I, Plowman GD, Starling JJ, Flynn DL. Peng SB, et al. Among authors: mochalkin i. Cancer Cell. 2015 Sep 14;28(3):384-98. doi: 10.1016/j.ccell.2015.08.002. Epub 2015 Sep 3. Cancer Cell. 2015. PMID: 26343583 Free article.
Identification of Clinical Candidate M2698, a Dual p70S6K and Akt Inhibitor, for Treatment of PAM Pathway-Altered Cancers.
DeSelm L, Huck B, Lan R, Neagu C, Potnick J, Xiao Y, Chen X, Jones R, Richardson TE, Heasley BH, Haxell T, Moore J, Tian H, Georgi K, Rohdich F, Sutton A, Johnson T, Mochalkin I, Jackson J, Lin J, Crowley L, Machl A, Clark A, Wilker E, Sherer B, Goutopoulos A. DeSelm L, et al. Among authors: mochalkin i. J Med Chem. 2021 Oct 14;64(19):14603-14619. doi: 10.1021/acs.jmedchem.1c01087. Epub 2021 Oct 1. J Med Chem. 2021. PMID: 34596404
Discovery of 4-aminopyrimidine analogs as highly potent dual P70S6K/Akt inhibitors.
Xiao Y, Huck BR, Lan R, DeSelm L, Chen X, Qiu H, Neagu C, Johnson T, Mochalkin I, Gardberg A, Jiang X, Tian H, Dutt V, Santos D, Head J, Jackson J, Syed S, Lin J, Wilker E, Ma J, Clark A, Machl A, Bankston D, Jones CCV, Goutopoulos A, Sherer B. Xiao Y, et al. Among authors: mochalkin i. Bioorg Med Chem Lett. 2021 Oct 15;50:128352. doi: 10.1016/j.bmcl.2021.128352. Epub 2021 Sep 2. Bioorg Med Chem Lett. 2021. PMID: 34481987
Discovery of 6-ethyl-2,4-diaminopyrimidine-based small molecule renin inhibitors.
Holsworth DD, Jalaie M, Belliotti T, Cai C, Collard W, Ferreira S, Powell NA, Stier M, Zhang E, McConnell P, Mochalkin I, Ryan MJ, Bryant J, Li T, Kasani A, Subedi R, Maiti SN, Edmunds JJ. Holsworth DD, et al. Among authors: mochalkin i. Bioorg Med Chem Lett. 2007 Jul 1;17(13):3575-80. doi: 10.1016/j.bmcl.2007.04.052. Epub 2007 Apr 25. Bioorg Med Chem Lett. 2007. PMID: 17482464
Rational design of 6-(2,4-diaminopyrimidinyl)-1,4-benzoxazin-3-ones as small molecule renin inhibitors.
Powell NA, Ciske FL, Cai C, Holsworth DD, Mennen K, Van Huis CA, Jalaie M, Day J, Mastronardi M, McConnell P, Mochalkin I, Zhang E, Ryan MJ, Bryant J, Collard W, Ferreira S, Gu C, Collins R, Edmunds JJ. Powell NA, et al. Among authors: mochalkin i. Bioorg Med Chem. 2007 Sep 1;15(17):5912-49. doi: 10.1016/j.bmc.2007.05.069. Epub 2007 Jun 2. Bioorg Med Chem. 2007. PMID: 17574423
Structure based design of an in vivo active hydroxamic acid inhibitor of P. aeruginosa LpxC.
Warmus JS, Quinn CL, Taylor C, Murphy ST, Johnson TA, Limberakis C, Ortwine D, Bronstein J, Pagano P, Knafels JD, Lightle S, Mochalkin I, Brideau R, Podoll T. Warmus JS, et al. Among authors: mochalkin i. Bioorg Med Chem Lett. 2012 Apr 1;22(7):2536-43. doi: 10.1016/j.bmcl.2012.01.140. Epub 2012 Feb 16. Bioorg Med Chem Lett. 2012. PMID: 22401863
Discovery of Evobrutinib: An Oral, Potent, and Highly Selective, Covalent Bruton's Tyrosine Kinase (BTK) Inhibitor for the Treatment of Immunological Diseases.
Caldwell RD, Qiu H, Askew BC, Bender AT, Brugger N, Camps M, Dhanabal M, Dutt V, Eichhorn T, Gardberg AS, Goutopoulos A, Grenningloh R, Head J, Healey B, Hodous BL, Huck BR, Johnson TL, Jones C, Jones RC, Mochalkin I, Morandi F, Nguyen N, Meyring M, Potnick JR, Santos DC, Schmidt R, Sherer B, Shutes A, Urbahns K, Follis AV, Wegener AA, Zimmerli SC, Liu-Bujalski L. Caldwell RD, et al. Among authors: mochalkin i. J Med Chem. 2019 Sep 12;62(17):7643-7655. doi: 10.1021/acs.jmedchem.9b00794. Epub 2019 Aug 15. J Med Chem. 2019. PMID: 31368705
Corrigendum to "Discovery of 4-aminopyrimidine analogs as highly potent dual P70S6K/Akt inhibitors" [Bioorgan. Med. Chem. Lett. 50 (2021) 128352].
Xiao Y, Huck BR, Lan R, DeSelm L, Chen X, Qiu H, Neagu C, Johnson T, Mochalkin I, Gardberg A, Jiang X, Tian H, Dutt V, Santos D, Head J, Jackson J, Syed S, Lin J, Wilker E, Ma J, Clark A, Machl A, Bankston D, Jones CCV, Goutopoulos A, Sherer B. Xiao Y, et al. Among authors: mochalkin i. Bioorg Med Chem Lett. 2022 Jul 1;67:128758. doi: 10.1016/j.bmcl.2022.128758. Epub 2022 Apr 25. Bioorg Med Chem Lett. 2022. PMID: 35484006 No abstract available.
32 results