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Dive into the research topics where Thomas G. Gant is active.

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Featured researches published by Thomas G. Gant.


Bioorganic & Medicinal Chemistry Letters | 2009

Potent and cellularly active 4-aminoimidazole inhibitors of cyclin-dependent kinase 5/p25 for the treatment of Alzheimer's disease.

Christopher John Helal; Zhijun Kang; John C. Lucas; Thomas G. Gant; Michael K. Ahlijanian; Joel B. Schachter; Karl E.G. Richter; James M. Cook; Frank S. Menniti; Kristin Kelly; Scot Mente; Jay Pandit; Natalie Hosea

Utilizing structure-based drug design, a 4-aminoimidazole heterocyclic core was synthesized as a replacement for a 2-aminothiazole due to potential metabolically mediated toxicity. The synthetic route utilized allowed for ready synthesis of 1-substituted-4-aminoimidazoles. SAR exploration resulted in the identification of a novel cis-substituted cyclobutyl group that gave improved enzyme and cellular potency against cdk5/p25 with up to 30-fold selectivity over cdk2/cyclin E.


Bioorganic & Medicinal Chemistry Letters | 2004

Discovery and SAR of 2-aminothiazole inhibitors of cyclin-dependent kinase 5/p25 as a potential treatment for Alzheimer's disease.

Christopher John Helal; Mark A. Sanner; Christopher B. Cooper; Thomas G. Gant; Mavis Diane Adam; John C. Lucas; Zhijun Kang; Stanley William Kupchinsky; Michael K. Ahlijanian; Bonnie Frances Tate; Frank S. Menniti; Kristin Kelly; Marcia Peterson


Archive | 2000

Heterocyclic derivatives useful as anticancer agents

Thomas G. Gant; Mark C. Noe


Bioorganic & Medicinal Chemistry Letters | 2006

Discovery of novel isothiazole inhibitors of the TrkA kinase: structure-activity relationship, computer modeling, optimization, and identification of highly potent antagonists.

Blaise Lippa; Joel Morris; Matthew Corbett; Tricia Kwan; Mark C. Noe; Sheri L. Snow; Thomas G. Gant; Melchiorra Mangiaracina; Heather Anne Coffey; Barbara Foster; Elisabeth Knauth; Matthew D. Wessel


Archive | 2001

Salts of a isothiazole-4-carboxamide and their use as anti-hyperproliferation agents

Thomas G. Gant; Glenn Robert Williams


Archive | 2005

Benzonitrile derivatives to treat musculoskeletal frailty

Thomas G. Gant; Roger J. Hill; Hua Zhu Ke; Bruce Allen Lefker; James Paul O'malley


Archive | 1999

Optically pure androgen mediator

Thomas G. Gant


Archive | 2001

Salt forms of 3-(4-bromo-2,6-difluoro-benzyloxy)-5-[3-(4-pyrrolidin-1-yl-butyl)-ureido]-isothiazole-4-carboxylic acid amide and method of production

Thomas G. Gant; Glenn Robert Williams


Archive | 2007

Salts of isothiazole-4-carboxamide and use of the same as anti-hyperproliferation agents

Thomas G. Gant; Glenn Robert Williams; ロバート ウィリアムズ,グレン; ジー. ガント,トーマス


Archive | 2005

FORMES DE SELS D'AMIDE D'ACIDE 3-(4-BROMO-2,6-DIFLUORO-BENZYLOXY) - 5 [3 - (4 - PYRROLIDINE - 1 - YL - BUTYL) UREIDO] ISOTHIAZOLE - 4 - CARBOXYLIQUE, ET PROCEDE POUR LEUR PRODUCTION.

Thomas G. Gant; Glenn Robert Williams

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