Screening of peptidomimetic libraries for antitumor activity

Bökönyi, Györgyi, Horváth, Anikó, Örfi, Lászó, Szabó, Edit Z., Houghten, Richard A., Ostresh, John M., Idei, Miklós, Hollósy, Ferenc, Szende, Béla, Teplán, István and Kéri, György (2000) Screening of peptidomimetic libraries for antitumor activity. Journal of Peptide Science, 6 Supp. 1: 192-192. doi:10.1002/psc.21


Author Bökönyi, Györgyi
Horváth, Anikó
Örfi, Lászó
Szabó, Edit Z.
Houghten, Richard A.
Ostresh, John M.
Idei, Miklós
Hollósy, Ferenc
Szende, Béla
Teplán, István
Kéri, György
Title Screening of peptidomimetic libraries for antitumor activity
Journal name Journal of Peptide Science   Check publisher's open access policy
ISSN 1075-2617
1099-1387
Publication date 2000
Sub-type Other
DOI 10.1002/psc.21
Volume 6
Issue Supp. 1
Start page 192
End page 192
Total pages 1
Place of publication Chichester, West Sussex, U.K .
Publisher John Wiley
Collection year 2000
Language eng
Subject C4
320501 Pharmaceutical Sciences and Pharmacy
670400 Human Pharmaceutical Products
Formatted abstract
The aim of our work was to screen peptidomimetic tyrosine kinase inhibitory libraries for antiproliferative and apoptotic or necrotic effect. We also wanted to distinguish between cytostatic and cytotoxic activities.

4-Benzylaminoquinasolines can be potent reversible inhibitors of Epidermal Growth Factor Receptor (EGFR) Tyrosine Kinase. It is known that after the benzylic methylation the biological activity depends on the chirality of the carbon atom, therefore we synthesized 4-amino acid quinasoline derivatives varying the nature and the configuration of the amino acid and/or the substituent of the benzyl ring (R2). A similar library was developed when we substituted quinasolone derivatives in position 2 with different amino acid derivatives. The synthesis of these libraries resulted in more then 100 compounds of each library. We systematically tested the above libraries using three different biological
assays.
1. MTT test: fast screening of big number of compounds for the inhibition of human carcinoma cell proliferation.
2. Counting of the cells: screening of the compounds which showed some biological activity in the previous assay.
3. Tyrosine kinase assay.
The results of the above assays will be discussed.
Q-Index Code C4
Additional Notes Special Issue Supplement: "26th European Peptide Society Meeting". Presented as Poster P368 at the above conference, "PEPTIDES 2000" held at Montpellier, France, September 10-15, 2000.

Document type: Journal Article
Sub-type: Other
Collection: School of Pharmacy Publications
 
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Created: Tue, 10 Jun 2008, 12:50:52 EST