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Page 1
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: bellamacina c. 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
Design, synthesis and structure activity relationship of potent pan-PIM kinase inhibitors derived from the pyridyl carboxamide scaffold.
Nishiguchi GA, Burger MT, Han W, Lan J, Atallah G, Tamez V, Lindvall M, Bellamacina C, Garcia P, Feucht P, Zavorotinskaya T, Dai Y, Wong K. Nishiguchi GA, et al. Among authors: bellamacina c. Bioorg Med Chem Lett. 2016 May 1;26(9):2328-32. doi: 10.1016/j.bmcl.2016.03.037. Epub 2016 Mar 11. Bioorg Med Chem Lett. 2016. PMID: 26995528
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. Among authors: bellamacina c. 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. Among authors: bellamacina c. 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
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: bellamacina c. 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.
Optimization of a Dibenzodiazepine Hit to a Potent and Selective Allosteric PAK1 Inhibitor.
Karpov AS, Amiri P, Bellamacina C, Bellance MH, Breitenstein W, Daniel D, Denay R, Fabbro D, Fernandez C, Galuba I, Guerro-Lagasse S, Gutmann S, Hinh L, Jahnke W, Klopp J, Lai A, Lindvall MK, Ma S, Möbitz H, Pecchi S, Rummel G, Shoemaker K, Trappe J, Voliva C, Cowan-Jacob SW, Marzinzik AL. Karpov AS, et al. Among authors: bellamacina c. ACS Med Chem Lett. 2015 May 22;6(7):776-81. doi: 10.1021/acsmedchemlett.5b00102. eCollection 2015 Jul 9. ACS Med Chem Lett. 2015. PMID: 26191365 Free PMC article.
Design, structure-activity relationship, and in vivo characterization of the development candidate NVP-HSP990.
McBride CM, Levine B, Xia Y, Bellamacina C, Machajewski T, Gao Z, Renhowe P, Antonios-McCrea W, Barsanti P, Brinner K, Costales A, Doughan B, Lin X, Louie A, McKenna M, Mendenhall K, Poon D, Rico A, Wang M, Williams TE, Abrams T, Fong S, Hendrickson T, Lei D, Lin J, Menezes D, Pryer N, Taverna P, Xu Y, Zhou Y, Shafer CM. McBride CM, et al. Among authors: bellamacina c. J Med Chem. 2014 Nov 13;57(21):9124-9. doi: 10.1021/jm501107q. Epub 2014 Nov 4. J Med Chem. 2014. PMID: 25368984
19 results