Abstract
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.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Amino Acid Sequence
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Antineoplastic Agents / chemical synthesis*
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Antineoplastic Agents / chemistry
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Antineoplastic Agents / pharmacology*
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Drug Screening Assays, Antitumor
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Humans
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Pyrazines / chemical synthesis*
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Pyrazines / chemistry
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Pyrazines / pharmacology*
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Receptors, Somatostatin / drug effects*
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Somatostatin / analogs & derivatives
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Somatostatin / chemical synthesis
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Somatostatin / chemistry
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Somatostatin / pharmacology
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Stereoisomerism
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Structure-Activity Relationship
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Tyrosine / chemistry
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Tyrosine / pharmacology*
Substances
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Antineoplastic Agents
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Pyrazines
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Receptors, Somatostatin
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Tyrosine
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Somatostatin