George Boykow
Overview
Explore the profile of George Boykow including associated specialties, affiliations and a list of published articles.
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14
Citations
154
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Recent Articles
1.
Chen X, Stout S, Mueller U, Boykow G, Visconti R, Siliphaivanh P, et al.
SLAS Discov
. 2017 Aug;
22(9):1131-1141.
PMID: 28763622
We have developed and validated label-free, liquid chromatography-mass spectrometry (LC-MS)-based equilibrium direct and competition binding assays to quantitate small-molecule antagonist binding to recombinant human and mouse BLT1 receptors expressed in...
2.
McKittrick B, Caldwell J, Bara T, Boykow G, Chintala M, Clader J, et al.
Bioorg Med Chem Lett
. 2015 Mar;
25(7):1592-6.
PMID: 25728416
The development of renin inhibitors with favorable oral pharmacokinetic profiles has been a longstanding challenge for the pharmaceutical industry. As part of our work to identify inhibitors of BACE1, we...
3.
Chelliah M, Eagen K, Guo Z, Chackalamannil S, Xia Y, Tsai H, et al.
ACS Med Chem Lett
. 2014 Jun;
5(5):561-5.
PMID: 24900880
We have synthesized several C7-spirocyclic analogues of vorapaxar and evaluated their in vitro activities against PAR-1 receptor. Some of these analogues showed activities and rat plasma levels comparable to vorapaxar....
4.
Chelliah M, Chackalamannil S, Xia Y, Greenlee W, Ahn H, Kurowski S, et al.
ACS Med Chem Lett
. 2014 Jun;
5(2):183-7.
PMID: 24900795
We have synthesized several C7-aminomethyl analogues of vorapaxar that are potent PAR-1 antagonists. Many of these analogues showed excellent in vitro binding affinity and pharmacokinetics profile in rats. Compound 6a...
5.
Smith K, Browne S, Jayaraman S, Bleickardt C, Hodge L, Lis E, et al.
Eur J Pharmacol
. 2014 Feb;
728:31-8.
PMID: 24486705
Adenosine A2A receptors are predominantly localized on striatopallidal gamma-aminobutyric acid (GABA) neurons, where they are colocalized with dopamine D2 receptors and are involved in the regulation of movement. Adenosine A2A...
6.
Chelliah M, Chackalamannil S, Xia Y, Eagen K, Greenlee W, Ahn H, et al.
Bioorg Med Chem Lett
. 2012 Mar;
22(7):2544-9.
PMID: 22405832
Discovery of a novel nor-seco himbacine analog as potent thrombin receptor (PAR-1) antagonist is described. Despite low plasma level, these new analogs showed excellent ex vivo efficacy in the monkey...
7.
Xia Y, Chackalamannil S, Greenlee W, Wang Y, Hu Z, Root Y, et al.
Bioorg Med Chem Lett
. 2010 Oct;
20(22):6676-9.
PMID: 20888225
An analog of the thrombin receptor antagonist vorapaxar (SCH 530348) with increased aqueous solubility, compound 9c (SCH 602539), was discovered through incorporation of polar substituents on the pyridine ring of...
8.
Chackalamannil S, Wang Y, Greenlee W, Hu Z, Xia Y, Ahn H, et al.
J Med Chem
. 2008 May;
51(11):3061-4.
PMID: 18447380
The discovery of an exceptionally potent series of thrombin receptor (PAR-1) antagonists based on the natural product himbacine is described. Optimization of this series has led to the discovery of...
9.
Chelliah M, Chackalamannil S, Xia Y, Eagen K, Clasby M, Gao X, et al.
J Med Chem
. 2007 Sep;
50(21):5147-60.
PMID: 17854166
Pursuing our earlier efforts in the himbacine-based thrombin receptor antagonist area, we have synthesized a series of compounds that incorporate heteroatoms in the C-ring of the tricyclic motif. This effort...
10.
Clasby M, Chackalamannil S, Czarniecki M, Doller D, Eagen K, Greenlee W, et al.
Bioorg Med Chem Lett
. 2007 May;
17(13):3647-51.
PMID: 17490877
The synthesis and biological activity of a novel series of thrombin receptor antagonists is described. This series of compounds showed excellent in vitro and in vivo potency. The most potent...