Rapid synthesis of RGD mimetics with isoxazoline scaffolds on solid phase: identification of alphavbeta3 antagonists lead compounds

A L Rockwell; M Rafalski; W J Pitts; D G Batt; J J Petraitis; W F DeGrado; S Mousa; P K Jadhav

doi:10.1016/s0960-894x(99)00114-6

Rapid synthesis of RGD mimetics with isoxazoline scaffolds on solid phase: identification of alphavbeta3 antagonists lead compounds

Bioorg Med Chem Lett. 1999 Apr 5;9(7):937-42. doi: 10.1016/s0960-894x(99)00114-6.

Authors

A L Rockwell¹, M Rafalski, W J Pitts, D G Batt, J J Petraitis, W F DeGrado, S Mousa, P K Jadhav

Affiliation

¹ Du Pont Pharmaceuticals Company, Chemical and Physical Sciences Department, Experimental Station, Wilmington, DE 19880-0500, USA.

PMID: 10230615
DOI: 10.1016/s0960-894x(99)00114-6

Abstract

Isoxazoline containing RGD mimetics were rapidly synthesized on a solid phase to optimize linkers, regioisomers of isoxazoline scaffolds, and exosite binding groups to yield lead alphavbeta3 antagonists.

MeSH terms

Isoxazoles / chemistry*
Molecular Mimicry*
Oligopeptides / chemical synthesis
Oligopeptides / chemistry*
Oligopeptides / pharmacology
Receptors, Vitronectin / antagonists & inhibitors*

Substances

Isoxazoles
Oligopeptides
Receptors, Vitronectin
arginyl-glycyl-aspartic acid