George L Trainor
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Explore the profile of George L Trainor including associated specialties, affiliations and a list of published articles.
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39
Citations
454
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Recent Articles
1.
Li G, Meanwell N, Krystal M, Langley D, Naidu B, Sivaprakasam P, et al.
J Med Chem
. 2020 Feb;
63(5):2620-2637.
PMID: 32081010
The standard of care for HIV-1 infection, highly active antiretroviral therapy (HAART), combines two or more drugs from at least two classes. Even with the success of HAART, new drugs...
2.
Huang A, Jayaraman L, Fura A, Vite G, Trainor G, Gottardis M, et al.
ACS Med Chem Lett
. 2016 Jan;
7(1):40-5.
PMID: 26819663
Efforts to identify a potent, reversible, nonsteroidal CYP17A1 lyase inhibitor with good selectivity over CYP17A1 hydroxylase and CYPs 11B1 and 21A2 for the treatment of castration-resistant prostate cancer (CRPC) culminated...
3.
Wan H, Schroeder G, Hart A, Inghrim J, Grebinski J, Tokarski J, et al.
ACS Med Chem Lett
. 2015 Aug;
6(8):850-5.
PMID: 26288683
JAK2 kinase inhibitors are a promising new class of agents for the treatment of myeloproliferative neoplasms and have potential for the treatment of other diseases possessing a deregulated JAK2-STAT pathway....
4.
Hart A, Schroeder G, Wan H, Grebinski J, Inghrim J, Kempson J, et al.
ACS Med Chem Lett
. 2015 Aug;
6(8):845-9.
PMID: 26288682
Early hit to lead work on a pyrrolopyridine chemotype provided access to compounds with biochemical and cellular potency against Janus kinase 2 (JAK2). Structure-based drug design along the extended hinge...
5.
Zimmermann K, Sang X, Mastalerz H, Johnson W, Zhang G, Liu Q, et al.
Bioorg Med Chem Lett
. 2015 May;
25(14):2809-12.
PMID: 25987372
The discovery, synthesis, and characterization of 9H-carbazole-1-carboxamides as potent and selective ATP-competitive inhibitors of Janus kinase 2 (JAK2) are discussed. Optimization for JAK family selectivity led to compounds 14 and...
6.
Trainor G
Expert Opin Drug Discov
. 2013 Mar;
2(1):51-64.
PMID: 23496037
Plasma protein binding of drugs is a well-recognised phenomena, but it is only recently that the implications for drug action in vivo have been fully appreciated. Plasma proteins, by virtue...
7.
He L, Seitz S, Trainor G, Tortolani D, Vaccaro W, Poss M, et al.
Bioorg Med Chem Lett
. 2012 Aug;
22(18):5995-8.
PMID: 22902653
A series of aminothiazoles that are potent inhibitors of LIM kinases 1 and 2 is described. Appropriate choice of substituents led to molecules with good selectivity for either enzyme. An...
8.
Dzierba C, Sielecki T, Arvanitis A, Galka A, Johnson T, Takvorian A, et al.
Bioorg Med Chem Lett
. 2012 Jul;
22(15):4986-9.
PMID: 22749422
Pyrido[3,2-b]pyrazin-3(4H)-ones and pteridin-7(8H)-ones were evaluated as corticotropin-releasing factor-1 receptor antagonists. The synthesis, SAR studies and pharmacokinetic evaluation of these analogs are described herein.
9.
Harikrishnan L, Srivastava N, Kayser L, Nirschl D, Kumaragurubaran K, Roy A, et al.
Bioorg Med Chem Lett
. 2012 Feb;
22(6):2287-90.
PMID: 22365758
Identification, synthesis and structure-activity relationship of small-molecule VIPR1 antagonists encompassing two chemical series are described.
10.
Thompson L, Shi J, Decicco C, Tebben A, Olson R, Boy K, et al.
Bioorg Med Chem Lett
. 2011 Oct;
21(22):6909-15.
PMID: 21974952
The synthesis, evaluation, and structure-activity relationships of a set of related constrained diaminopropane inhibitors of BACE-1 are described. The full in vivo profile of an optimized inhibitor in both normal...