Henry H. Gu
Bristol-Myers Squibb
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Publication
Featured researches published by Henry H. Gu.
Bioorganic & Medicinal Chemistry Letters | 2002
William J. Pitts; Junqing Guo; T. G. Murali Dhar; Zhongqi Shen; Henry H. Gu; Scott H. Watterson; Mark S. Bednarz; Bang-Chi Chen; Joel C. Barrish; Donna A. Bassolino; Daniel L. Cheney; Catherine A. Fleener; Katherine A. Rouleau; Diane Hollenbaugh; Edwin J. Iwanowicz
A series of novel triazine-based small molecule inhibitors (IV) of inosine monophosphate dehydrogenase was prepared. The synthesis and the structure-activity relationships (SAR) derived from in vitro studies are described.
Bioorganic & Medicinal Chemistry Letters | 2003
Edwin J. Iwanowicz; Scott H. Watterson; Junqing Guo; William J. Pitts; T. G. Murali Dhar; Zhongqi Shen; Ping Chen; Henry H. Gu; Catherine A. Fleener; Katherine A. Rouleau; Daniel L. Cheney; Robert Townsend; Diane Hollenbaugh
The first reported structure-activity relationships (SARs) about the N-[3-methoxy-4-(5-oxazolyl)phenyl moiety for a series of recently disclosed inosine monophosphate dehydrogenase (IMPDH) inhibitors are described. The syntheses and in vitro inhibitory values for IMPDH II, and T-cell proliferation (for select analogues) are given.
Bioorganic & Medicinal Chemistry Letters | 2002
Ping Chen; Derek J. Norris; Edwin J. Iwanowicz; Steven H. Spergel; James Lin; Henry H. Gu; Zhongqi Shen; John Wityak; Tai-An Lin; Suhong Pang; Henry de Fex; Sidney Pitt; Ding Ren Shen; Arthur M. Doweyko; Donna A. Bassolino; Jacques Y. Roberge; Michael A. Poss; Bang-Chi Chen; Gary L. Schieven; Joel C. Barrish
We have identified a novel series of 1,5-imidazoquinoxalines as inhibitors of Lck with excellent potency (IC50s<5 nM) as well as good cellular activity against T-cell proliferation (IC50s<1 microM). Structure-activity studies demonstrate the requirement for the core heterocycle in addition to an optimal 2,6-disubstituted aniline group.
Bioorganic & Medicinal Chemistry Letters | 2003
T. G. Murali Dhar; Zhongqi Shen; Henry H. Gu; Ping Chen; Derek J. Norris; Scott H. Watterson; Shelley K. Ballentine; Catherine A. Fleener; Katherine A. Rouleau; Joel C. Barrish; Robert Townsend; Diane Hollenbaugh; Edwin J. Iwanowicz
A series of novel small molecule inhibitors of inosine monophosphate dehydrogenase (IMPDH), based upon a 3-cyanoindole core, were explored. IMPDH catalyzes the rate determining step in guanine nucleotide biosynthesis and is a target for anticancer, immunosuppressive and antiviral therapy. The synthesis and the structure-activity relationships (SAR), derived from in vitro studies, for this new series of inhibitors is given.
Bioorganic & Medicinal Chemistry Letters | 2002
Henry H. Gu; Edwin J. Iwanowicz; Junqing Guo; Scott H. Watterson; Zhongqi Shen; William J. Pitts; T. G. Murali Dhar; Catherine A. Fleener; Katherine A. Rouleau; N.Z. Sherbina; Mark R. Witmer; Jeffrey Tredup; Diane Hollenbaugh
A series of novel amide-based small molecule inhibitors of inosine monophosphate dehydrogenase is described. The synthesis and the structure-activity relationships (SARs) derived from in vitro studies are presented.
Bioorganic & Medicinal Chemistry Letters | 2002
Edwin J. Iwanowicz; Scott H. Watterson; Chunjian Liu; Henry H. Gu; Toomas Mitt; Katerina Leftheris; Joel C. Barrish; Catherine A. Fleener; Katherine A. Rouleau; N.Z. Sherbina; Diane Hollenbaugh
A series of novel guanidine-based small molecule inhibitors of inosine monophosphate dehydrogenase (IMPDH) was explored. IMPDH catalyzes the rate determining step in guanine nucleotide biosynthesis and is a target for anticancer, immunosuppressive and antiviral therapy. The synthesis and the structure-activity relationships (SARs), derived from in vitro studies, for this new series of inhibitors is given.
Bioorganic & Medicinal Chemistry Letters | 2002
Ping Chen; Edwin J. Iwanowicz; Derek J. Norris; Henry H. Gu; James Lin; Robert V. Moquin; Jagabandhu Das; John Wityak; Steven H. Spergel; Henry de Fex; Suhong Pang; Sydney Pitt; Ding Ren Shen; Gary L. Schieven; Joel C. Barrish
A series of anilino(imidazoquinoxaline) analogues bearing solubilizing side chains at the 6- and 7-positions of the fused phenyl ring has been prepared and evaluated for inhibition against Lck enzyme and of T-cell proliferation. Significant improvement of the cellular activity was achieved over the initial lead, compound 2.
Bioorganic & Medicinal Chemistry Letters | 2002
Scott H. Watterson; Chunjian Liu; T. G. Murali Dhar; Henry H. Gu; William J. Pitts; Joel C. Barrish; Catherine A. Fleener; Katherine A. Rouleau; N.Z. Sherbina; Diane Hollenbaugh; Edwin J. Iwanowicz
A series of novel amide-based small molecule inhibitors of inosine monophosphate dehydrogenase (IMPDH) was explored. The synthesis and the structure-activity relationships (SARs) derived from in vitro studies are described.
Bioorganic & Medicinal Chemistry Letters | 2003
T. G. Murali Dhar; Scott H. Watterson; Ping Chen; Zhongqi Shen; Henry H. Gu; Derek J. Norris; Marianne Carlsen; Kristin D. Haslow; William J. Pitts; Junqing Guo; John S. Chorba; Catherine A. Fleener; Katherine A. Rouleau; Robert Townsend; Diane Hollenbaugh; Edwin J. Iwanowicz
The synthesis and the structure-activity relationships (SAR) of analogues derived from the introduction of basic residues on ring D of quinolone-based inhibitors of IMPDH are described. This led to the identification of compound 27 as a potent inhibitor of IMPDH with significantly improved aqueous solubility over the lead compound 1.
Bioorganic & Medicinal Chemistry Letters | 2003
Scott H. Watterson; Marianne Carlsen; T. G. Murali Dhar; Zhongqi Shen; William J. Pitts; Junqing Guo; Henry H. Gu; Derek J. Norris; John S. Chorba; Ping Chen; Daniel L. Cheney; Mark R. Witmer; Catherine A. Fleener; Katherine A. Rouleau; Robert Townsend; Diane Hollenbaugh; Edwin J. Iwanowicz
A series of novel quinolone-based small molecule inhibitors of inosine monophosphate dehydrogenase (IMPDH) was explored. The synthesis and the structure-activity relationships (SARs) derived from in vitro studies are described.