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Preparation and improved stability of N-Boc-alpha-amino-5-acyl Meldrum's acids, a versatile class of building blocks for combinatorial chemistry.
The preparation of novel N-Boc-alpha-amino-5-acyl Meldrum's acids is described. The synthetic inaccessibility and instability of several of these products have led to the development of a protocolExpand
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α,α-Difluoro-β-ketophosphonates as potent inhibitors of protein tyrosine phosphatase 1B
Abstract A novel series of inhibitors that contain an aryl α,α-difluoro-β-ketophosphonate group has been synthesized and evaluated against protein tyrosine phosphatase 1B. These compounds exhibitExpand
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Discovery and structure-activity relationships of novel sulfonamides as potent PTP1B inhibitors.
A series of novel sulfonamides containing a single difluoromethylene-phosphonate group were discovered to be potent inhibitors of protein tyrosine phosphatase 1B. Structure-activity relationshipsExpand
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Novel, selective EPO receptor ligands lacking erythropoietic activity reduce infarct size in acute myocardial infarction in rats.
Erythropoietin (EPO) has been shown to protect the heart against acute myocardial infarction in pre-clinical studies, however, EPO failed to reduce infarct size in clinical trials and showedExpand
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Exploring structure-activity relationships around the phosphomannose isomerase inhibitor AF14049 via combinatorial synthesis.
Phosphomannose Isomerase (PMI) has been shown by genetic methods to be an essential enzyme in fungal cell wall biosynthesis. The PMI inhibitor AF14049 was discovered as an unanticipated side productExpand
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Discovery and Characterization of a Potent Interleukin-6 Binding Peptide with Neutralizing Activity In Vivo
Interleukin-6 (IL-6) is an important member of the cytokine superfamily, exerting pleiotropic actions on many physiological processes. Over-production of IL-6 is a hallmark of immune-mediatedExpand
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Studies on cyclodepsipeptides - part II : The total synthesis of jaspamide and geodiamolide-D
The total synthesis of cyclodepsipeptides jaspamide and geodiamolide D have been presented.
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Studies on cyclodepsipeptides - Part I : A stereoselective synthesis of C12 polyketide unit (C1–C8) present in Jaspamide and Geodiamolide A–F
An innovative synthetic protocol to obtain the polyketide C12 chain in an enantiomerically pure form has been developed.
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Discovery and optimization of a TRAIL R2 agonist for cancer therapy.
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