Sugar Amino Acid Containing Somatostatin Analogues that Induce Apoptosis in Both Drug-Sensitive and Multidrug-Resistant Tumor Cells

Resistance to chemotherapy has become a major problem in cancer therapy. The new sugar amino acid (SAA) containing somatostatin analogues presented possess antiproliferative and apoptotic activity against both multidrug-resistant and drug-sensitive hepatoma carcinoma cells. Synthesis, design, and bi...

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Bibliographic Details
Published in:Organic letters 2001-11, Vol.3 (23), p.3723-3725
Main Authors: Gruner, Sibylle A. W, Kéri, Gyorgy, Schwab, Richard, Venetianer, Aniko, Kessler, Horst
Format: Article
Language:English
Subjects:
Algorithms
Amino Acids - chemistry
Animals
Antineoplastic Agents - chemical synthesis
Antineoplastic Agents - pharmacology
Apoptosis
Drug Resistance, Neoplasm
Drug Screening Assays, Antitumor
Hormone Antagonists - chemical synthesis
Hormone Antagonists - pharmacology
Rats
Somatostatin - analogs & derivatives
Somatostatin - chemical synthesis
Somatostatin - pharmacology
Structure-Activity Relationship
Sugar Acids - chemistry
Tumor Cells, Cultured
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Summary:Resistance to chemotherapy has become a major problem in cancer therapy. The new sugar amino acid (SAA) containing somatostatin analogues presented possess antiproliferative and apoptotic activity against both multidrug-resistant and drug-sensitive hepatoma carcinoma cells. Synthesis, design, and biological evaluation of the cyclic analogues and of the furanoid SAA used will be discussed. Four analogues have IC50 values in the low μM range, making them promising leads for chemotherapeutic drugs against multidrug-resistant carcinoma.
ISSN:1523-7060
1523-7052
DOI:10.1021/ol0166698