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Discovery of a Covalent Inhibitor of KRASG12C (AMG 510) for the Treatment of Solid Tumors.
Lanman BA, Allen JR, Allen JG, Amegadzie AK, Ashton KS, Booker SK, Chen JJ, Chen N, Frohn MJ, Goodman G, Kopecky DJ, Liu L, Lopez P, Low JD, Ma V, Minatti AE, Nguyen TT, Nishimura N, Pickrell AJ, Reed AB, Shin Y, Siegmund AC, Tamayo NA, Tegley CM, Walton MC, Wang HL, Wurz RP, Xue M, Yang KC, Achanta P, Bartberger MD, Canon J, Hollis LS, McCarter JD, Mohr C, Rex K, Saiki AY, San Miguel T, Volak LP, Wang KH, Whittington DA, Zech SG, Lipford JR, Cee VJ. Lanman BA, et al. Among authors: wurz rp. J Med Chem. 2020 Jan 9;63(1):52-65. doi: 10.1021/acs.jmedchem.9b01180. Epub 2019 Dec 24. J Med Chem. 2020. PMID: 31820981
Discovery of N-(1-Acryloylazetidin-3-yl)-2-(1H-indol-1-yl)acetamides as Covalent Inhibitors of KRASG12C.
Shin Y, Jeong JW, Wurz RP, Achanta P, Arvedson T, Bartberger MD, Campuzano IDG, Fucini R, Hansen SK, Ingersoll J, Iwig JS, Lipford JR, Ma V, Kopecky DJ, McCarter J, San Miguel T, Mohr C, Sabet S, Saiki AY, Sawayama A, Sethofer S, Tegley CM, Volak LP, Yang K, Lanman BA, Erlanson DA, Cee VJ. Shin Y, et al. Among authors: wurz rp. ACS Med Chem Lett. 2019 Aug 20;10(9):1302-1308. doi: 10.1021/acsmedchemlett.9b00258. eCollection 2019 Sep 12. ACS Med Chem Lett. 2019. PMID: 31531201 Free PMC article.
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: wurz rp. 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
Discovery of imidazopyridazines as potent Pim-1/2 kinase inhibitors.
Wurz RP, Sastri C, D'Amico DC, Herberich B, Jackson CLM, Pettus LH, Tasker AS, Wu B, Guerrero N, Lipford JR, Winston JT, Yang Y, Wang P, Nguyen Y, Andrews KL, Huang X, Lee MR, Mohr C, Zhang JD, Reid DL, Xu Y, Zhou Y, Wang HL. Wurz RP, et al. Bioorg Med Chem Lett. 2016 Nov 15;26(22):5580-5590. doi: 10.1016/j.bmcl.2016.09.067. Epub 2016 Oct 1. Bioorg Med Chem Lett. 2016. PMID: 27769621
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: wurz rp. 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 and Optimization of Macrocyclic Quinoxaline-pyrrolo-dihydropiperidinones as Potent Pim-1/2 Kinase Inhibitors.
Cee VJ, Chavez F Jr, Herberich B, Lanman BA, Pettus LH, Reed AB, Wu B, Wurz RP, Andrews KL, Chen J, Hickman D, Laszlo J 3rd, Lee MR, Guerrero N, Mattson BK, Nguyen Y, Mohr C, Rex K, Sastri CE, Wang P, Wu Q, Wu T, Xu Y, Zhou Y, Winston JT, Lipford JR, Tasker AS, Wang HL. Cee VJ, et al. Among authors: wurz rp. ACS Med Chem Lett. 2016 Feb 12;7(4):408-12. doi: 10.1021/acsmedchemlett.5b00403. eCollection 2016 Apr 14. ACS Med Chem Lett. 2016. PMID: 27096050 Free PMC article.
34 results