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.
SYNTHESIS OF A DICARBA- ANALOGUE OF OCTEOTRIDE KEEPING THE TYPE II BETA-TURN OF THE PHARMACOPHORE IN WATER SOLUTION / Carotenuto, A.; D'Addona, D.; Rivalta, E.; Chelli, M.; PAPINI ANNA MARIA, ; Rovero, Paolo; Ginanneschi, M.. - In: LETTERS IN ORGANIC CHEMISTRY. - ISSN 1570-1786. - STAMPA. - 2:(2005), pp. 274-279. [10.2174/1570178053765276]
SYNTHESIS OF A DICARBA- ANALOGUE OF OCTEOTRIDE KEEPING THE TYPE II BETA-TURN OF THE PHARMACOPHORE IN WATER SOLUTION
D. D'ADDONA;M. CHELLI;PAPINI ANNA MARIA;ROVERO, PAOLO;M. GINANNESCHI
2005
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.
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