Sugar amino acid containing somatostatin analogues that induce apoptosis in both drug-sensitive and multidrug-resistant tumor cells.
[carbohydrate structure--see text] 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 IC(50) values in the low microM range, making them promising leads for chemotherapeutic drugs against multidrug-resistant carcinoma.
Gruner
S A
SA
Novaspin Biotech GmbH and Institut für Organische Chemie und Biochemie, Technische Universität München, Lichtenbergstr. 4, D-85747 Garching, Germany.
Kéri
G
G
Schwab
R
R
Venetianer
A
A
Kessler
H
H
D000465:Algorithms; D000596:Amino Acids / Q000737:chemistry*; D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000494:pharmacology*; D017209:Apoptosis; D019008:Drug Resistance, Neoplasm; D004354:Drug Screening Assays, Antitumor; D006727:Hormone Antagonists / Q000138:chemical synthesis / Q000494:pharmacology*; D051381:Rats; D013004:Somatostatin / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D013400:Sugar Acids / Q000737:chemistry*; D014407:Tumor Cells, Cultured
D000596:Amino Acids; D000970:Antineoplastic Agents; D006727:Hormone Antagonists; D013400:Sugar Acids; D013004:Somatostatin