The growth of malignant tumors has been shown to be dependent on the evelopment of new blood vessels. Blocking tumor-induced angiogenesis is an efficiency strategy to prevent and cure cancer. It has been shown that the angiogenic process depends on vascular endothelial cell migration and invasion processes regulated by cell adhesion receptor. The integrin α vβ 3 is such a cell adhesion receptor. Recent studies show the integrin α vβ 3 and extracellular matrix can recognize each other through Arg-Gly-Asp(RGD) sequence, some peptides containing
RGD Sequence', 1, 1607947)"; href="/tags/rgd-sequence/">RGD sequence antagonists can inhibit embryonic neovascularization, tumor-induced angiogenesis, and tumor growth. According to the structure-activity relationships and
antiangiogenic mechanism of RGD sequence, we use
thalidomide as the leading structure to design and synthesize five 5-carboxy-1,3-dihydro-1,3-dioxo-2H-isoindole derivatives. All of them were first reported and their structures were confirmed by elementary analysis, IR and 1H NMR spectra. The results of preliminary antiangiogenic tests in vitro showed that most target compounds could inhibit ECV 304 proliferation. Moreover, it has been proved that the inhibition of endothelial cell proliferation was not the result of cytotoxic effect of target compounds.
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