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Investigational New Drugs
Published in: Investigational New Drugs 4/2020

Open Access 01-08-2020 | Piperazine | PRECLINICAL STUDIES

Synthesis and cellular effects of novel 1,3,5-triazine derivatives in DLD and Ht-29 human colon cancer cell lines

Authors: Agnieszka Wróbel, Beata Kolesińska, Justyna Frączyk, Zbigniew J. Kamiński, Anna Tankiewicz-Kwedlo, Justyna Hermanowicz, Robert Czarnomysy, Dawid Maliszewski, Danuta Drozdowska

Published in: Investigational New Drugs | Issue 4/2020

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Summary

This study provides new information on the cellular effects of 1,3,5-triazine nitrogen mustards with different peptide groups in DLD and Ht-29 human colon cancer cell lines. A novel series of 2,4,6-trisubstituted 1,3,5-triazine derivatives bearing 2-chloroethyl and oligopeptide moieties was designed and synthesized. The most cytotoxic derivative was triazine with an Ala-Ala-OMe substituent on the ring (compound 7b). This compound induced time- and dose-dependent cytotoxicity in the DLD-1 and HT-29 colon cancer cell lines. The triazine derivative furthermore induced apoptosis through intracellular signaling pathway attenuation. Compound 7b may be a candidate for further evaluation as a chemotherapeutic agent against colorectal cancer.
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Metadata
Title
Synthesis and cellular effects of novel 1,3,5-triazine derivatives in DLD and Ht-29 human colon cancer cell lines
Authors
Agnieszka Wróbel
Beata Kolesińska
Justyna Frączyk
Zbigniew J. Kamiński
Anna Tankiewicz-Kwedlo
Justyna Hermanowicz
Robert Czarnomysy
Dawid Maliszewski
Danuta Drozdowska
Publication date
01-08-2020
Publisher
Springer US
Published in
Investigational New Drugs / Issue 4/2020
Print ISSN: 0167-6997
Electronic ISSN: 1573-0646
DOI
https://doi.org/10.1007/s10637-019-00838-9

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