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Pharmacological characterization of CP-547,632, a novel vascular endothelial growth factor receptor-2 tyrosine kinase inhibitor for cancer therapy.
Signaling through vascular endothelial growth factor (VEGF) receptors (VEGFRs) is a key pathway initiating endothelial cell proliferation and migration resulting in angiogenesis, a requirement forExpand
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Linezolid, the first oxazolidinone antibacterial agent.
Linezolid (Zyvox) is the first member of an entirely new class of antibiotics to reach the market in over 35 years; it was approved for use in 2000. A member of the oxazolidinone class ofExpand
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Delineating the role of cooperativity in the design of potent PROTACs for BTK
Significance Proteolysis targeting chimera (PROTAC)-based protein degradation is an emerging field that holds significant promise for targeting the “undruggable” proteome: the vast majority of theExpand
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Count of benign melanocytic nevi as a major indicator of risk for nonfamilial nodular and superficial spreading melanoma
A study of 207 consecutive white patients older than 18 years of age with nonfamilial nodular and superficial spreading melanoma and 295 controls was conducted in southeast France. Controls wereExpand
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Potent inhibitors of LpxC for the treatment of Gram-negative infections.
In this paper, we present the synthesis and SAR as well as selectivity, pharmacokinetic, and infection model data for representative analogues of a novel series of potent antibacterial LpxCExpand
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Discovery of Dap-3 polymyxin analogues for the treatment of multidrug-resistant Gram-negative nosocomial infections.
We report novel polymyxin analogues with improved antibacterial in vitro potency against polymyxin resistant recent clinical isolates of Acinetobacter baumannii and Pseudomonas aeruginosa . InExpand
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Pyridone methylsulfone hydroxamate LpxC inhibitors for the treatment of serious gram-negative infections.
The synthesis and biological activity of a new series of LpxC inhibitors represented by pyridone methylsulfone hydroxamate 2a is presented. Members of this series have improved solubility and freeExpand
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Discovery of 3,3-dimethyl-5-hydroxypipecolic hydroxamate-based inhibitors of aggrecanase and MMP-13.
A series of pipecolic hydroxamate inhibitors of MMP-13 and aggrecanase was discovered based on screening known inhibitors of TNF-alpha converting enzyme (TACE). Potency versus aggrecanase wasExpand
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Pyridone-conjugated monobactam antibiotics with gram-negative activity.
Herein we describe the structure-aided design and synthesis of a series of pyridone-conjugated monobactam analogues with in vitro antibacterial activity against clinically relevant Gram-negativeExpand
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