Synthesis of a Dicarba-Analog of Octreotide Keeping the Type II β -Turn of the Pharmacophore in Water Solution

Title: Synthesis of a Dicarba-Analog of Octreotide Keeping the Type II β -Turn of the Pharmacophore in Water Solution

Volume: 2 Issue: 3

Author(s): Alfonso Carotenuto, Debora D 'Addona, Eleonora Rivalta, Mario Chelli, Anna Maria Papini, Paolo Rovero and Mauro Ginanneschi

Affiliation:

Keywords: octreotide analog, solid-phase ring-closing metathesis, nmr conformational study

Abstract: The Z isomer of the new constrained analog of the anticancer drug octreotide,where L,L-cystine is replaced by 4,5-dehydro-L,L-diaminosuberic acid,was prepared by solid-phase ring-closing metathesis.NMR study ascertained that this molecule is conformationally very close to the parent octreotide and remains unaffected by the enzymatic pool of the human serum for more than 30 h.

Cite this article as:

Carotenuto Alfonso, D 'Addona Debora, Rivalta Eleonora, Chelli Mario, Papini Maria Anna, Rovero Paolo and Ginanneschi Mauro, Synthesis of a Dicarba-Analog of Octreotide Keeping the Type II β -Turn of the Pharmacophore in Water Solution, Letters in Organic Chemistry 2005; 2 (3) . https://dx.doi.org/10.2174/1570178053765276