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Structure Guided Optimization, in Vitro Activity, and in Vivo Activity of Pan-PIM Kinase Inhibitors.
Burger MT, Han W, Lan J, Nishiguchi G, Bellamacina C, Lindval M, Atallah G, Ding Y, Mathur M, McBride C, Beans EL, Muller K, Tamez V, Zhang Y, Huh K, Feucht P, Zavorotinskaya T, Dai Y, Holash J, Castillo J, Langowski J, Wang Y, Chen MY, Garcia PD. Burger MT, et al. Among authors: garcia pd. ACS Med Chem Lett. 2013 Oct 15;4(12):1193-7. doi: 10.1021/ml400307j. eCollection 2013 Dec 12. ACS Med Chem Lett. 2013. PMID: 24900629 Free PMC article.
Synthesis and Structure-Activity Relationship of Tetra-Substituted Cyclohexyl Diol Inhibitors of Proviral Insertion of Moloney Virus (PIM) Kinases.
Han W, Ding Y, Chen Z, Langowski JL, Bellamacina C, Rico A, Nishiguchi GA, Lan J, Atallah G, Lindvall M, Lin S, Zang R, Feucht P, Zavorotinskaya T, Dai Y, Garcia P, Burger MT. Han W, et al. J Med Chem. 2020 Dec 10;63(23):14885-14904. doi: 10.1021/acs.jmedchem.0c01279. Epub 2020 Dec 1. J Med Chem. 2020. PMID: 33258605
Pan-PIM kinase inhibition provides a novel therapy for treating hematologic cancers.
Garcia PD, Langowski JL, Wang Y, Chen M, Castillo J, Fanton C, Ison M, Zavorotinskaya T, Dai Y, Lu J, Niu XH, Basham S, Chan J, Yu J, Doyle M, Feucht P, Warne R, Narberes J, Tsang T, Fritsch C, Kauffmann A, Pfister E, Drueckes P, Trappe J, Wilson C, Han W, Lan J, Nishiguchi G, Lindvall M, Bellamacina C, Aycinena JA, Zang R, Holash J, Burger MT. Garcia PD, et al. Clin Cancer Res. 2014 Apr 1;20(7):1834-45. doi: 10.1158/1078-0432.CCR-13-2062. Epub 2014 Jan 28. Clin Cancer Res. 2014. PMID: 24474669
Identification of N-(4-((1R,3S,5S)-3-Amino-5-methylcyclohexyl)pyridin-3-yl)-6-(2,6-difluorophenyl)-5-fluoropicolinamide (PIM447), a Potent and Selective Proviral Insertion Site of Moloney Murine Leukemia (PIM) 1, 2, and 3 Kinase Inhibitor in Clinical Trials for Hematological Malignancies.
Burger MT, Nishiguchi G, Han W, Lan J, Simmons R, Atallah G, Ding Y, Tamez V, Zhang Y, Mathur M, Muller K, Bellamacina C, Lindvall MK, Zang R, Huh K, Feucht P, Zavorotinskaya T, Dai Y, Basham S, Chan J, Ginn E, Aycinena A, Holash J, Castillo J, Langowski JL, Wang Y, Chen MY, Lambert A, Fritsch C, Kauffmann A, Pfister E, Vanasse KG, Garcia PD. Burger MT, et al. Among authors: garcia pd. J Med Chem. 2015 Nov 12;58(21):8373-86. doi: 10.1021/acs.jmedchem.5b01275. Epub 2015 Oct 27. J Med Chem. 2015. PMID: 26505898
Discovery of chiral dihydropyridopyrimidinones as potent, selective and orally bioavailable inhibitors of AKT.
Parthasarathy S, Henry K, Pei H, Clayton J, Rempala M, Johns D, De Frutos O, Garcia P, Mateos C, Pleite S, Wang Y, Stout S, Condon B, Ashok S, Lu Z, Ehlhardt W, Raub T, Lai M, Geeganage S, Burkholder TP. Parthasarathy S, et al. Bioorg Med Chem Lett. 2018 Jun 1;28(10):1887-1891. doi: 10.1016/j.bmcl.2018.03.092. Epub 2018 Apr 2. Bioorg Med Chem Lett. 2018. PMID: 29655979
Cyclin A/B RxL Macrocyclic Inhibitors to Treat Cancers with High E2F Activity.
Singh S, Gleason CE, Fang M, Laimon YN, Khivansara V, Xie S, Durmaz YT, Sarkar A, Ngo K, Savla V, Li Y, Abu-Remaileh M, Li X, Tuladhar B, Odeh R, Hamkins-Indik F, He D, Membreno MW, Nosrati M, Gushwa NN, Leung SSF, Fraga-Walton B, Hernandez L, Baldomero MP, Lent BM, Spellmeyer D, Luna JF, Hoang D, Gritsenko Y, Chand M, DeMart MK, Metobo S, Bhatt C, Shapiro JA, Yang K, Dupper NJ, Bockus AT, Doench JG, Aggen JB, Liu LF, Levin B, Wang EW, Vendrell I, Fischer R, Kessler B, Gokhale PC, Signoretti S, Spektor A, Kreatsoulas C, Singh R, Earp DJ, Garcia PD, Nijhawan D, Oser MG. Singh S, et al. Among authors: garcia pd. bioRxiv [Preprint]. 2024 Aug 1:2024.08.01.605889. doi: 10.1101/2024.08.01.605889. bioRxiv. 2024. PMID: 39211113 Free PMC article. Preprint.
83 results