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Discovery and SAR of PF-4693627, a potent, selective and orally bioavailable mPGES-1 inhibitor for the potential treatment of inflammation.
TLDR
A novel series of orally active, selective benzoxazole piperidinecarboxamides as mPGES-1 inhibitors is discovered, including 23, 26, and 29, which were effective in a carrageenan-stimulated guinea pig air pouch model of inflammation. Expand
Design, parallel synthesis, and crystal structures of pyrazinone antithrombotics as selective inhibitors of the tissue factor VIIa complex.
TLDR
This study ultimately led to the synthesis of compound 34, which exhibited 16 nM activity on TF/VIIa with >6250 x selectivity vs Factor Xa and thrombin and was chosen for preclinical, intravenous proof-of-concept studies to demonstrate the separation between antithrombotic efficacy and bleeding side effects in a nonhuman primate model of electrolytic-induced arterial thrombosis. Expand
Selective small molecule PARG inhibitor causes replication fork stalling and cancer cell death
TLDR
It is found that PARG expression is upregulated in many cancers and structural and biological insight is provided with small molecule PARG inhibitors and it is shown thatPARG inhibition sensitizes cells to ionizing radiation and kills cancer cells through replication fork defects. Expand
Structure-based drug design of pyrazinone antithrombotics as selective inhibitors of the tissue factor VIIa complex.
TLDR
Structure-based drug design coupled with polymer-assisted solution-phase library synthesis was utilized to develop a series of pyrazinone inhibitors of the tissue factor/Factor VIIa complex to demonstrate the separation between antithrombotic efficacy and bleeding side effects in a primate model of thrombosis. Expand
Fourier Transform Infrared (FTIR) Spectroscopy
Infrared (IR) spectroscopy has always been a powerful tool for the identification of organic materials. However, with the development of Fourier transform infrared (FTIR) spectroscopy, it has becomeExpand
Inhibitors of HGFA, Matriptase, and Hepsin Serine Proteases: A Nonkinase Strategy to Block Cell Signaling in Cancer.
TLDR
This preliminary investigation provides evidence that HGFA is a promising therapeutic target in breast cancer and other tumor types driven by c-MET and RON. Expand
Structure-based discovery of small molecule hepsin and HGFA protease inhibitors: Evaluation of potency and selectivity derived from distinct binding pockets.
TLDR
The first reported non-peptide small molecule inhibitors of both HGFA and hepsin are discovered, which have differential potency and selectivity towards all three proteases. Expand
Chiral cations in 4+3 cycloadditions
Abstract The reaction of the chiral acetal 4 with furan and cyclopentadiene in the presence of a Lewis acid gives 4+3 cycloadducts in very good yields. Diastereoselectivity in the case of furan isExpand
Structure-activity relationships among DNA ligase inhibitors: Characterization of a selective uncompetitive DNA ligase I inhibitor.
TLDR
Together, the results demonstrate that L82-G17 is a LigI-selective inhibitor with utility as a probe of the catalytic activity and cellular functions of LIGI and provide a framework for the future design of DNA ligase inhibitors. Expand
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