Research Topics
Genomes and Genes | Gary T WangSummaryAffiliation: Abbott Laboratories Country: USA Publications
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Publications
Synthesis and activity of 1-aryl-1'-imidazolyl methyl ethers as non-thiol farnesyltransferase inhibitorsQun Li
Cancer Research, GPRD, Abbott Laboratories, Abbott Park, IL 60064 6101, USA
Bioorg Med Chem Lett 14:5371-6. 2004..The compounds are characterized as being simple, easier to make, and possess no chiral center involved...
Design, synthesis, and structural analysis of influenza neuraminidase inhibitors containing pyrrolidine coresG T Wang
Pharmaceutical Product Division, Abbott Laboratories, Abbott Park, Illinois 60064, USA
J Med Chem 44:1192-201. 2001....
Lead optimization of methionine aminopeptidase-2 (MetAP2) inhibitors containing sulfonamides of 5,6-disubstituted anthranilic acidsGary T Wang
Cancer Research, Global Pharmaceutical Research and Development, Abbott Laboratories, Abbott Park, IL 60064, USA
Bioorg Med Chem Lett 17:2817-22. 2007..Introduction of a tertiary amino moiety at the ortho-position of the sulfonyl phenyl ring gave reduced protein binding and improved cellular activity, but led to lower oral bioavailability...
1-(5-Chloro-2-alkoxyphenyl)-3-(5-cyanopyrazin-2-yl)ureas [correction of cyanopyrazi] as potent and selective inhibitors of Chk1 kinase: synthesis, preliminary SAR, and biological activitiesGary T Wang
Cancer Research, Global Pharmaceutical R and D, Abbott Laboratories, Abbott Park, Illinois 60064, USA
J Med Chem 48:3118-21. 2005..Flow cytometry (FACS) analysis confirmed that 2e abrogated G2 checkpoint arrest of H1299 cells caused by doxorubicin and S checkpoint arrest caused by camptothecin...
Amino-substituted heterocycles as isosteres of trans-cinnamides: design and synthesis of heterocyclic biaryl sulfides as potent antagonists of LFA-1/ICAM-1 bindingGary T Wang
Global Pharmaceutical Research and Development, Abbott Laboratories, Abbott Park Road, Abbott Park, IL 60064, USA
Bioorg Med Chem Lett 15:195-201. 2005..Applying this isosterism to previously reported p-arylthio cinnamides resulted in the identification of 4-amino-6-(p-arylthio)phenyl-pyrimidines and 2-amino-4-(p-arylthio)phenyl-pyridines as potent antagonists of LFA-1/ICAM-1 binding...
Design and synthesis of o-trifluoromethylbiphenyl substituted 2-amino-nicotinonitriles as inhibitors of farnesyltransferaseGary T Wang
Global Pharmaceutical Research and Development, Abbott Laboratories, Abbott Park, IL 60064, USA
Bioorg Med Chem Lett 15:153-8. 2005..Optimization of this lead resulted in compounds 2e and 2g, with FT IC(50) values of 1.3 and 1.8 nM, GGT IC(50) of 1400 nM, and EC(50) (Ras processing) values of 13 and 11 nM, respectively...
Design, synthesis, and structural analysis of inhibitors of influenza neuraminidase containing a 2,3-disubstituted tetrahydrofuran-5-carboxylic acid coreGary T Wang
Global Pharmaceutical Research and Development, Abbott Laboratories, Abbott Park, IL 60064, USA
Bioorg Med Chem Lett 15:125-8. 2005..Both compounds 9 and 14 inhibit influenza NA A with an IC(50) of about 0.5 microM and NA B with an IC(50) of 1.0 microM...
Substituted 4-amino-1H-pyrazolo[3,4-d]pyrimidines as multi-targeted inhibitors of insulin-like growth factor-1 receptor (IGF1R) and members of ErbB-family receptor kinasesGary T Wang
Global Pharmaceutical Research and Development, Abbott Laboratories, Abbott Park, IL 60064, USA
Bioorg Med Chem Lett 20:6067-71. 2010....
Synthesis and biological evaluation of 1-(2,4,5-trisubstituted phenyl)-3-(5-cyanopyrazin-2-yl)ureas as potent Chk1 kinase inhibitorsGaoquan Li
Cancer Research, Global Pharmaceutical Research and Development, Abbott Laboratories, Abbott Park, IL 60064, USA
Bioorg Med Chem Lett 16:2293-8. 2006..7 microM) and enhanced doxorubicin cytotoxicity (IC50=0.44 microM) while displaying no single agent activity...
Discovery and optimization of anthranilic acid sulfonamides as inhibitors of methionine aminopeptidase-2: a structural basis for the reduction of albumin bindingGeorge S Sheppard
Cancer Research, Global Pharmaceutical Research and Development, Abbott Laboratories, Department R47A, 100 Abbott Park Road, Abbott Park, Illinois 60064, USA
J Med Chem 49:3832-49. 2006....
Synthesis and biological evaluation of 1-benzyl-5-(3-biphenyl-2-yl-propyl)-1H-imidazole as novel farnesyltransferase inhibitorNan horng Lin
Cancer Research, R 47B, Global Pharmaceutical Products Division, Abbott Laboratories, 100 Abbott Park Road, Abbott Park, IL 60064 3500, USA
Bioorg Med Chem Lett 14:5057-62. 2004..The most promising compound identified from this series is analog 29 that possesses potent enzymatic and cellular activities...
Design, synthesis, and biological activity of 4-[(4-cyano-2-arylbenzyloxy)-(3-methyl-3H-imidazol-4-yl)methyl]benzonitriles as potent and selective farnesyltransferase inhibitorsLe Wang
Globe Pharmaceutical R and Abbott Laboratories, 100 Abbott Park Road, Abbott Park, Illinois 60064 6101, USA
J Med Chem 47:612-26. 2004..Medicinal chemistry efforts led to the discovery of compound 64 with potent cellular activity (EC(50) = 3.5 nM) and outstanding pharmacokinetic profiles in dog (96% bioavailable, 18.4 h oral t(1/2), and 0.19 L/(h x kg) plasma clearance)...
Insulin-like growth factor-1 receptor and ErbB kinase inhibitor combinations block proliferation and induce apoptosis through cyclin D1 reduction and Bax activationJulie L Wilsbacher
Cancer Research, Global Pharmaceutical Research and Development, Abbott Laboratories, Abbott Park, IL 60064, USA
J Biol Chem 283:23721-30. 2008..Thus, targeting both IGF-1R and ErbB receptors simultaneously results in cell cycle arrest and apoptosis through combined effects on Akt, cyclin D1, and Bax activation...
Imidazo[2,1-b]thiazoles: multitargeted inhibitors of both the insulin-like growth factor receptor and members of the epidermal growth factor family of receptor tyrosine kinasesSteve D Fidanze
Global Pharmaceutical Research and Development, Abbott Laboratories, Abbott Park, IL 60064, USA
Bioorg Med Chem Lett 20:2452-5. 2010..The design and enzyme activities of a novel class of imidazo[2,1-b]thiazoles is presented...
