Scott K Thompson
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Explore the profile of Scott K Thompson including associated specialties, affiliations and a list of published articles.
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Articles
21
Citations
363
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Recent Articles
1.
Ramachandran R, Thompson S, Malkmus S, Mieda T, Lin J, Gupta S, et al.
J Pharmacol Exp Ther
. 2020 Jul;
374(3):521-528.
PMID: 32616515
The sensation of pruritus, or itch, is associated with a variety of skin and medical disorders. Itch is transmitted through afferent C-fibers, and sodium channels play a key role in...
2.
Kallander L, Washburn D, Hoang T, Frazee J, Stoy P, Johnson L, et al.
Bioorg Med Chem Lett
. 2009 Nov;
20(1):371-4.
PMID: 19926282
The previously reported pyrrolidine class of progesterone receptor partial agonists demonstrated excellent potency but suffered from serious liabilities including hERG blockade and high volume of distribution in the rat. The...
3.
Marino Jr J, Kallander L, Ma C, Oh H, Lee D, Gaitanopoulos D, et al.
Bioorg Med Chem Lett
. 2009 Sep;
19(19):5617-21.
PMID: 19717304
The liver X receptors (LXR) play a key role in cholesterol homeostasis and lipid metabolism. SAR studies around tertiary-amine lead molecule 2, an LXR full agonist, revealed that steric and...
4.
Wang Y, Duraiswami C, Madauss K, Tran T, Williams S, Deng S, et al.
Bioorg Med Chem Lett
. 2009 Aug;
19(17):4916-9.
PMID: 19664922
High throughput screening of the corporate compound collection led to the identification of a novel series of 2-amino-9-aryl-3-cyano-4-methyl-7-oxo-6,7,8,9-tetrahydropyrido[2',3':4,5]thieno[2,3-b]pyridine derivatives as selective PR agonists. Initial SAR exploration leading to potent and...
5.
Washburn D, Hoang T, Frazee J, Johnson L, Hammond M, Manns S, et al.
Bioorg Med Chem Lett
. 2009 Jul;
19(16):4664-8.
PMID: 19616429
We have designed and synthesized a novel series of pyrrolidinones as progesterone receptor partial agonists. Compounds from this series had improved AR selectivity, rat pharmacokinetic properties, and in vivo potency...
6.
Thompson S, Washburn D, Frazee J, Madauss K, Hoang T, Lapinski L, et al.
Bioorg Med Chem Lett
. 2009 Jul;
19(16):4777-80.
PMID: 19595590
Using the X-ray crystal structure of an amide-based progesterone receptor (PR) partial agonist bound to the PR ligand binding domain, a novel PR partial agonist class containing a pyrrolidine ring...
7.
Hammond M, Washburn D, Hoang H, Manns S, Frazee J, Nakamura H, et al.
Bioorg Med Chem Lett
. 2009 Jun;
19(15):4441-5.
PMID: 19497745
The lead serum and glucocorticoid-related kinase 1 (SGK1) inhibitors 4-(5-phenyl-1H-pyrrolo[2,3-b]pyridin-3-yl)benzoic acid (1) and {4-[5-(2-naphthalenyl)-1H-pyrrolo[2,3-b]pyridin-3-yl]phenyl}acetic acid (2) suffer from low DNAUC values in rat, due in part to formation and excretion...
8.
Synthesis and SAR of amino acid-derived heterocyclic progesterone receptor full and partial agonists
Hammond M, Patterson J, Manns S, Hoang T, Washburn D, Trizna W, et al.
Bioorg Med Chem Lett
. 2009 Apr;
19(10):2637-41.
PMID: 19376703
Two classes of amino acid-derived heterocyclic progesterone receptor ligands were developed to address the metabolic issues posed by the dimethyl amide functionality of the lead compound (1). The tetrazole-derived ligands...
9.
Washburn D, Hoang T, Campobasso N, Smallwood A, Parks D, Webb C, et al.
Bioorg Med Chem Lett
. 2009 Jan;
19(4):1097-100.
PMID: 19167885
A novel series of 1H-indol-1-yl tertiary amine LXR agonists has been designed. Compounds from this series were potent agonists with good rat pharmacokinetic parameters. In addition, the crystal structure of...
10.
Sherk A, Frigo D, Schnackenberg C, Bray J, Laping N, Trizna W, et al.
Cancer Res
. 2008 Sep;
68(18):7475-83.
PMID: 18794135
Androgens, through their actions on the androgen receptor (AR), are required for the development of the prostate and contribute to the pathologic growth dysregulation observed in prostate cancers. Consequently, androgen...