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Synthesis, in vitro and in vivo activity of thiamine antagonist transketolase inhibitors.

• Allen Thomas, Yvan Le Huerou, +22 authors Guy P. A. Vigers
• Bioorganic & medicinal chemistry letters
• 2008

Tumor cells extensively utilize the pentose phosphate pathway for the synthesis of ribose. Transketolase is a key enzyme in this pathway and has been suggested as a target for inhibition in the… (More)

Identification and structure-activity studies of novel ultrashort-acting benzodiazepine receptor agonists.

• Jeffrey A Stafford, Gregory J Pacofsky, +9 authors Paul Feldman
• Bioorganic & medicinal chemistry letters
• 2002

The synthesis and evaluation of novel ultrashort-acting benzodiazepine (USA BZD) agonists is described. A BZD scaffold was modified by incorporation of amino acids and derivatives. The propionate… (More)

Design of non-nucleoside inhibitors of HIV-1 reverse transcriptase with improved drug resistance properties. 2.

• George A Freeman, C Webster Andrews Iii, +18 authors Joseph H Chan
• Journal of medicinal chemistry
• 2004

HIV-1 nonnucleoside reverse transcriptase inhibitors (NNRTIs) are part of the combination therapy currently used to treat HIV infection. The features of a new NNRTI drug for HIV treatment must… (More)

Discovery of Tumor-Specific Irreversible Inhibitors of Stearoyl CoA Desaturase

• Panayotis C Theodoropoulos, Stephen S Gonzales, +14 authors Deepak Nijhawan
• Nature chemical biology
• 2016

A hallmark of targeted cancer therapies is selective toxicity among cancer cell lines. We evaluated results from a viability screen of over 200,000 small molecules to identify two chemical series,… (More)

Functional Identification of Putrescine C- and N-Hydroxylases.

• Bin Li, Tiffany M. Lowe-Power, +5 authors Anthony Michael
• ACS chemical biology
• 2016

The small polyamine putrescine (1,4-diaminobutane) is ubiquitously and abundantly found in all three domains of life. It is a precursor, through N-aminopropylation or N-aminobutylation, for… (More)

Total Synthesis of (-)-Nodulisporic Acid D.

• Yike Zou, Jason E Melvin, Stephen S Gonzales, Matthew J Spafford, Amos B. Smith
• Journal of the American Chemical Society
• 2015

A convergent total synthesis of the architecturally complex indole diterpenoid (-)-nodulisporic acid D has been achieved. Key synthetic transformations include vicinal difunctionalization of an… (More)

Novel acyl coenzyme A (CoA): diacylglycerol acyltransferase-1 inhibitors: synthesis and biological activities of diacylethylenediamine derivatives.

• Yoshihisa Nakada, Thomas Aicher, +9 authors Shuji Kitamura
• Bioorganic & medicinal chemistry
• 2010

A series of diacylethylenediamine derivatives were synthesized and evaluated for their inhibitory activity against DGAT-1 and pharmacokinetic profile to discover new small molecule DGAT-1 inhibitors.… (More)

Relating the structure, activity, and physical properties of ultrashort-acting benzodiazepine receptor agonists.

• Gregory J Pacofsky, Jeffrey A Stafford, +12 authors Paul Feldman
• Bioorganic & medicinal chemistry letters
• 2002

The ultrashort-acting benzodiazepine (USA BZD) agonists reported previously have been structurally modified to improve aqueous solubility. Lactam-to-amidine modifications, replacement of the… (More)

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