Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 18, Issue 23, Pages 6199-6201Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2008.10.001
Keywords
Somatostatin analogue; Pyrazinone ring; Antiproliferative activity
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Funding
- KAKENHI [17790026]
- Kobe Gakuin University
- Hungarian Academy of Sciences [JAP-6/02, OTKA 49478, 60197, Ret-06/2006]
- Grants-in-Aid for Scientific Research [17790026] Funding Source: KAKEN
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Novel somatostatin analogues containing a pyrazinone ring, compounds 1 and 2, exhibited good antiproliferative activity on A431 tumor cells. To increase antitumor activity and binding affinity on somatostatin receptors (SSTRs), we substituted Tyr in the critical sequence, Tyr-D-Trp-Lys, with more hydrophobic aromatic residue. The substituted compounds dramatically lost antitumor activity, indicating that Tyr residue was an essential residue. (C) 2008 Elsevier Ltd. All rights reserved.
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