903905-67-9Relevant academic research and scientific papers
Structure-activity studies on a library of potent calix[4]arene-based PDGF antagonists that inhibit PDGF-stimulated PDGFR tyrosine phosphorylation
Zhou, Huchen,Wang, De-An,Baldini, Laura,Ennis, Eileen,Jain, Rishi,Carie, Adam,Sebti, Said M.,Hamilton, Andrew D.
, p. 2376 - 2386 (2008/09/19)
Platelet-derived growth factor (PDGF) and its receptor PDGFR are required for tumor growth and angiogenesis, so disruption of the PDGF-PDGFR interaction should lead to starvation of tumors and reduction of tumor growth. Potent PDGF antagonists have been discovered through the synthesis of a series of calix[4]arene-based compounds that are designed to bind to the three-loop region of PDGF. The effect of lower-rim alkylation, linker and number of interacting head groups on the calix[4]arene scaffold on PDGF affinity and cellular activity has been investigated. The Royal Society of Chemistry 2006.
