Discovery of Potent Nonpeptide Vitronectin Receptor (αVβ3) Antagonists

  title={Discovery of Potent Nonpeptide Vitronectin Receptor ($\alpha$V$\beta$3) Antagonists},
  author={Richard M. Keenan and H MillerWilliam and Chet Kwon and Fadia E. Ali and James Francis Callahan and Raul R. Calvo and Hwang Sm and Kenneth D. Kopple and Catherine E. Peishoff and James M. Samanen and Angela S. Wong and C K Yuan and William F. Huffman},
  journal={Journal of Medicinal Chemistry},
Combretastatin-Inspired Heterocycles as Antitubulin Anticancer Agents
The results revealed the importance of the 2-aminoimidazole-carbonyl motif as a double bond replacement in combretastatin and indicated a pharmacodynamically interesting pattern of H-bond acceptors/donors and requisite syn-templated aryls.
Direct and Regioselective Introduction of Acetals into Imidazoles at the 2-Position by an Iridium-Catalyzed Reaction with Formates in the Presence of Hydrosilanes
The iridium-catalyzed reaction of imidazoles with formates in the presence of hydrosilanes as co-reactants, leading to the production of 2-[(alkoxy)(siloxy)methyl]imidazoles, is described. Dimethyl
Synthesis of Polysubstituted 2-Aminoimidazoles via Alkene-Diamination of Guanidine with Conjugated α-Bromoalkenones.
A step-economical access to polysubstituted aminoimidazoles has been accomplished via alkene vicinal C-N bonds formation of 2-bromo-2-alkenones with guanidine avoiding its
αvβ3- or α5β1-Integrin-Selective Peptidomimetics for Surface Coating.
The aim of this Review is to illustrate the evolution of surface-coating molecules in this field: from peptides and proteins with relatively low integrin-binding activity and receptor selectivity to highly active and selective peptidomimetic ligands.
Role of Side‐Chain Bioisosteres in Determining the Binding Affinity of Click Chemistry Derived RGD Peptidomimetics to αvβ3 Integrin
Triazole-containing Arg-Gly-Asp (RGD) peptidomimetics capable of interacting with αvβ3 integrin were developed through click chemistry and molecular modelling calculations of a hit compound showed that the triazole and 2-aminopyridine rings were involved in important π-stacking interactions with Tyr178.
Integrin Antagonists and Angiogenesis
The rationale for the development of various therapeutic and diagnostic candidate anti-integrin agents is reviewed here, as are nanoparticle delivery systems directed at specific sites on integrins.