Synthesis and cytotoxic activity of Boc-protected pentapeptide amide analogs of somatostatin

• Published in: Russian chemical bulletin Vol. 65; no. 11; pp. 2766 - 2769
• Main Authors: Balaev, A. N., Osipov, V. N., Okhmanovich, K. A., Ruchko, E. A., Kolotaev, A. V., Khachatryan, D. S.
• Format: Journal Article
• Language: English
• Published: New York Springer US 01-11-2016; Springer Nature B.V
• Subjects: Amides; Analogs; Brief Communications; Chemistry; Chemistry and Materials Science; Chemistry/Food Science; Inorganic Chemistry; Organic Chemistry; liquid-phase peptide synthesis; cytotoxic activity; somatostatin analogs; pentapeptide amides
• ISSN: 1066-5285; 1573-9171
• DOI: 10.1007/s11172-016-1651-1

New Boc-protected pentapeptide amides of the general formula Boc—Cys(Boc)—Phe—
d
-Trp—Lys(Boc)—Thr—NHR, which are analogs of the natural hormone somatostatin, were synthesized. The cytotoxic activity of the new compounds was evaluated against the cancer cell lines MCF-7, PC 3, and HCT-116 by the MTT test, and some of these compounds were found to exhibit activity at micromolar concentrations.