Perspectives in Cancer Chemotherapy, in vitro and in vivo Experiments

Autor: Helga Engi
Rok vydání: 2008
Předmět:
Zdroj: Hungarian Medical Journal. 2:279-291
ISSN: 1789-0403
1788-6139
DOI: 10.1556/hmj.2.2008.2.28358
Popis: The development of pharmacological agents able to counteract the mechanisms of multidrug resistance (MDR) in oncology has remained a major goal for the past ten years. Several mechanisms are thought to be involved in drug resistance, including those associated with drug transport, detoxification and apoptosis. The first part of this thesis was focused on the inhibition of MDR through inhibition of the MDR P-glycoprotein (P-gp) in various cell lines. Six groups of compounds were involved in the P-gp efflux pump inhibitory studies: cinnamylidene ketones; 1,4-dihydropyridines derivatives; phenothiazines; HSP90 inhibitor peptide derivatives; Tylosin Betti base derivative and Euphorbia diterpenes. The majority of the tested compounds were able to increase the R123 accumulation in cancer cell lines. Generally, the newly identified MDR modifiers were able to enhance the antiproliferative activity of selected anticancer drugs in a synergistic or additive way in vitro on MDR cells. The in vitro activity of TBN was...
Databáze: OpenAIRE