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Discovery and Optimization of Quinazolinone-pyrrolopyrrolones as Potent and Orally Bioavailable Pan-Pim Kinase Inhibitors.
Pettus LH, Andrews KL, Booker SK, Chen J, Cee VJ, Chavez F Jr, Chen Y, Eastwood H, Guerrero N, Herberich B, Hickman D, Lanman BA, Laszlo J 3rd, Lee MR, Lipford JR, Mattson B, Mohr C, Nguyen Y, Norman MH, Powers D, Reed AB, Rex K, Sastri C, Tamayo N, Wang P, Winston JT, Wu B, Wu T, Wurz RP, Xu Y, Zhou Y, Tasker AS, Wang HL. Pettus LH, et al. Among authors: eastwood h. J Med Chem. 2016 Jul 14;59(13):6407-30. doi: 10.1021/acs.jmedchem.6b00610. Epub 2016 Jun 22. J Med Chem. 2016. PMID: 27285051
Discovery of ( R)-8-(6-Methyl-4-oxo-1,4,5,6-tetrahydropyrrolo[3,4- b]pyrrol-2-yl)-3-(1-methylcyclopropyl)-2-((1-methylcyclopropyl)amino)quinazolin-4(3 H)-one, a Potent and Selective Pim-1/2 Kinase Inhibitor for Hematological Malignancies.
Wang HL, Andrews KL, Booker SK, Canon J, Cee VJ, Chavez F Jr, Chen Y, Eastwood H, Guerrero N, Herberich B, Hickman D, Lanman BA, Laszlo J 3rd, Lee MR, Lipford JR, Mattson B, Mohr C, Nguyen Y, Norman MH, Pettus LH, Powers D, Reed AB, Rex K, Sastri C, Tamayo N, Wang P, Winston JT, Wu B, Wu Q, Wu T, Wurz RP, Xu Y, Zhou Y, Tasker AS. Wang HL, et al. Among authors: eastwood h. J Med Chem. 2019 Feb 14;62(3):1523-1540. doi: 10.1021/acs.jmedchem.8b01733. Epub 2019 Jan 17. J Med Chem. 2019. PMID: 30624936
Synthesis and preliminary biological evaluation of potent and selective 2-(3-alkoxy-1-azetidinyl) quinolines as novel PDE10A inhibitors with improved solubility.
Rzasa RM, Frohn MJ, Andrews KL, Chmait S, Chen N, Clarine JG, Davis C, Eastwood HA, Horne DB, Hu E, Jones AD, Kaller MR, Kunz RK, Miller S, Monenschein H, Nguyen T, Pickrell AJ, Porter A, Reichelt A, Zhao X, Treanor JJS, Allen JR. Rzasa RM, et al. Among authors: eastwood ha. Bioorg Med Chem. 2014 Dec 1;22(23):6570-6585. doi: 10.1016/j.bmc.2014.10.013. Bioorg Med Chem. 2014. PMID: 25456383
95 results