One of the fundamental objectives of organic and medicinal chemistry is the design, synthesis,
and production of molecules having value as human therapeutic agents. Until 1920-1940, …

Apoptosis resistance commonly occurs in cancers, preventing activation of Caspase family
cell death proteases. XIAP is an endogenous inhibitor of Caspases overexpressed in many …

Serine-, threonine-, and cysteine-derived cyclic building blocks (pseudo-prolines, ΨPro)
serve as reversible protecting groups for Ser, Thr, and Cys and prove to be versatile tools for …

In the 15 years since their first description, the conceptual and technical approaches that
encompass combinatorial chemistry have gained wide acceptance across virtually all scientific …

Virtual screening is increasingly being used in drug discovery programs with a growing number
of successful applications. Experimental methodologies developed to speed up the drug …

Heterocyclic chemistry constitutes an essential branch of organic chemistry and heterocycles
are widely known to display an array of biological properties. Pyrazoles represent key …

… 1 , Clemencia Pinilla, Marc A Giulianotti, Jon R Appel, Colette T Dooley, Adel Nefzi, John
M Ostresh, Yongping Yu, Gerald M Maggiora, Jose L Medina-Franco, Daniela Brunner, Jeff …

We tested the effects of small-molecule XIAP antagonists based on a polyphenylurea
pharmacophore on cultured acute myelogenous leukemia (AML) cell lines and primary patient …

Mixture based synthetic combinatorial libraries offer a tremendous enhancement for the rate
of drug discovery, allowing the activity of millions of compounds to be assessed through the …

The rapid rise in antibiotic-resistant Gram-positive bacterial infections prompted us to explore
the development of novel strategies for synthesis of large chemical libraries amenable to …