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Discovery of 1-arylcarbonyl-6,7-dimethoxyisoquinoline derivatives as glutamine fructose-6-phosphate amidotransferase (GFAT) inhibitors.

• Yimin Qian, Mushtaq Ahmad, +11 authors D Bolin
• Bioorganic & medicinal chemistry letters
• 2011

Through high throughput screening and subsequent hit identification and optimization, we synthesized a series of 1-arylcarbonyl-6,7-dimethoxyisoquinoline derivatives as the first reported potent and… (More)

Cell-based screening approach for antitumor drug leads which exploits sensitivity differences between normal and cancer cells: identification of two novel cell-cycle inhibitors.

• Lyubomir T. Vassilev, Sonja Kazmer, +5 authors Steven J. Berthel
• Anti-cancer drug design
• 2001

A cell-based in vitro screening approach for identification of antitumor drug leads that exploits the differential sensitivity between normal and cancer cells was developed. It is a three-step,… (More)

Optimization of benzodiazepinones as selective inhibitors of the X-linked inhibitor of apoptosis protein (XIAP) second baculovirus IAP repeat (BIR2) domain.

• Robert F Kester, Andrew F Donnell, +29 authors Barry Goggin
• Journal of medicinal chemistry
• 2013

The IAPs are key regulators of the apoptotic pathways and are commonly overexpressed in many cancer cells. IAPs contain one to three BIR domains that are crucial for their inhibitory function. The… (More)

Benzazepinones and benzoxazepinones as antagonists of inhibitor of apoptosis proteins (IAPs) selective for the second baculovirus IAP repeat (BIR2) domain.

• Andrew F Donnell, Christophe Michoud, +26 authors Stacy W Remiszewski
• Journal of medicinal chemistry
• 2013

XIAP is a key regulator of apoptosis, and its overexpression in cancer cells may contribute to their survival. The antiapoptotic function of XIAP derives from its BIR domains, which bind to and… (More)

Identification of phenyl-pyridine-2-carboxylic acid derivatives as novel cell cycle inhibitors with increased selectivity for cancer cells.

• Steven J. Berthel, Ian M Marks, +5 authors Lyubomir T. Vassilev
• Anti-cancer drugs
• 2002

Ro 41-4439, a phenyl-pyridine-2-carboxylic acid derivative, was identified by a cell-based screening approach that exploits the differences between normal and cancer cells in their sensitivity to… (More)

Potent, selective MCH-1 receptor antagonists.

• Shawn D Erickson, Bruce Banner, +18 authors Hong Bing Wang
• Bioorganic & medicinal chemistry letters
• 2008

This paper describes the lead optimization of a new series of potent, selective, orally bioavailable, brain-penetrant MCH-1 receptor antagonists. A major focus of the work was to achieve a… (More)

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