Holland GW - Search Results

1

Discovery, structure-activity relationships, pharmacokinetics, and efficacy of glucokinase activator (2R)-3-cyclopentyl-2-(4-methanesulfonylphenyl)-N-thiazol-2-yl-propionamide (RO0281675).

Haynes NE, Corbett WL, Bizzarro FT, Guertin KR, Hilliard DW, Holland GW, Kester RF, Mahaney PE, Qi L, Spence CL, Tengi J, Dvorozniak MT, Railkar A, Matschinsky FM, Grippo JF, Grimsby J, Sarabu R. Haynes NE, et al. Among authors: holland gw. J Med Chem. 2010 May 13;53(9):3618-25. doi: 10.1021/jm100039a. J Med Chem. 2010. PMID: 20405948

2

Discovery, modeling, and human pharmacokinetics of N-(2-acetyl-4,6-dimethylphenyl)-3-(3,4-dimethylisoxazol-5-ylsulfamoyl)thiophene-2-carboxamide (TBC3711), a second generation, ETA selective, and orally bioavailable endothelin antagonist.

Wu C, Decker ER, Blok N, Bui H, You TJ, Wang J, Bourgoyne AR, Knowles V, Berens KL, Holland GW, Brock TA, Dixon RA. Wu C, et al. Among authors: holland gw. J Med Chem. 2004 Apr 8;47(8):1969-86. doi: 10.1021/jm030528p. J Med Chem. 2004. PMID: 15055997 Clinical Trial.

3

Acyl substitution at the ortho position of anilides enhances oral bioavailability of thiophene sulfonamides: TBC3214, an ETA selective endothelin antagonist.

Wu C, Decker ER, Blok N, Li J, Bourgoyne AR, Bui H, Keller KM, Knowles V, Li W, Stavros FD, Holland GW, Brock TA, Dixon RA. Wu C, et al. Among authors: holland gw. J Med Chem. 2001 Apr 12;44(8):1211-6. doi: 10.1021/jm000349x. J Med Chem. 2001. PMID: 11312921

4

Endothelin antagonists: substituted mesitylcarboxamides with high potency and selectivity for ET(A) receptors.

Wu C, Decker ER, Blok N, Bui H, Chen Q, Raju B, Bourgoyne AR, Knowles V, Biediger RJ, Market RV, Lin S, Dupré B, Kogan TP, Holland GW, Brock TA, Dixon RA. Wu C, et al. Among authors: holland gw. J Med Chem. 1999 Nov 4;42(22):4485-99. doi: 10.1021/jm9900063. J Med Chem. 1999. PMID: 10579813

5

Nonpeptide endothelin antagonists in clinical development.

Wu C, Decker ER, Holland GW, Brown PM, Stavros FD, Brock TA, Dixon RA. Wu C, et al. Among authors: holland gw. Drugs Today (Barc). 2001 Jul;37(7):441-453. doi: 10.1358/dot.2001.37.7.844187. Drugs Today (Barc). 2001. PMID: 12750762

6

Recently discovered sulfonamide-, acyl sulfonamide- and carboxylic acid-based endothelin antagonists.

Wu C, Holland GW, Brock TA, Dixon RA. Wu C, et al. Among authors: holland gw. IDrugs. 2003 Mar;6(3):232-9. IDrugs. 2003. PMID: 12789612 Review.

7

Development of cell adhesion molecule antagonists as therapeutics for asthma and COPD.

Vanderslice P, Biediger RJ, Woodside DG, Berens KL, Holland GW, Dixon RA. Vanderslice P, et al. Among authors: holland gw. Pulm Pharmacol Ther. 2004;17(1):1-10. doi: 10.1016/j.pupt.2003.10.004. Pulm Pharmacol Ther. 2004. PMID: 14643165 Review.

8

Genetic algorithm-optimized QSPR models for bioavailability, protein binding, and urinary excretion.

Wang J, Krudy G, Xie XQ, Wu C, Holland G. Wang J, et al. J Chem Inf Model. 2006 Nov-Dec;46(6):2674-83. doi: 10.1021/ci060087t. J Chem Inf Model. 2006. PMID: 17125207

9

A 3D structure model of integrin alpha 4 beta 1 complex: I. Construction of a homology model of beta 1 and ligand binding analysis.

You TJ, Maxwell DS, Kogan TP, Chen Q, Li J, Kassir J, Holland GW, Dixon RA. You TJ, et al. Among authors: holland gw. Biophys J. 2002 Jan;82(1 Pt 1):447-57. doi: 10.1016/S0006-3495(02)75409-X. Biophys J. 2002. PMID: 11751331 Free PMC article.

10

Development of reliable aqueous solubility models and their application in druglike analysis.

Wang J, Krudy G, Hou T, Zhang W, Holland G, Xu X. Wang J, et al. J Chem Inf Model. 2007 Jul-Aug;47(4):1395-404. doi: 10.1021/ci700096r. Epub 2007 Jun 15. J Chem Inf Model. 2007. PMID: 17569522

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