Synthesis and biological evaluation of selective CXCR4 antagonists containing alkene dipeptide isosteres.
نویسندگان
چکیده
A set of cyclic peptide analogues of a selective CXCR4 antagonist FC131 [cyclo(-d-Tyr-Arg-Arg-Nal-Gly-)] were synthesized and bioevaluated. Using (E)-alkene and (Z)-fluoroalkene dipeptide isosteres for Arg-Arg and Arg-Nal substructures, indispensable or the partial contribution of the two peptide bonds to the CXCR4 antagonism and anti-HIV activity was demonstrated. FC131 and the analogues were shown to selectively inhibit SDF-1 binding to CXCR4, whereas no inhibition of binding of SDF-1 to CXCR7 was observed.
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ورودعنوان ژورنال:
- Organic & biomolecular chemistry
دوره 8 3 شماره
صفحات -
تاریخ انتشار 2010