@article{MTMT:3179770, title = {Selenoesters and selenoanhydrides as novel multidrug resistance reversing agents: A confirmation study in a colon cancer MDR cell line}, url = {https://m2.mtmt.hu/api/publication/3179770}, author = {Gajdács, Márió and Spengler, Gabriella and Sanmartin, C and Marc, MA and Handzlik, J and Dominguez-Alvarez, E}, doi = {10.1016/j.bmcl.2017.01.033}, journal-iso = {BIOORG MED CHEM LETT}, journal = {BIOORGANIC & MEDICINAL CHEMISTRY LETTERS}, volume = {27}, unique-id = {3179770}, issn = {0960-894X}, abstract = {Taking into account that multidrug resistance (MDR) is the main cause for chemotherapeutic failure in cancer treatment and as a continuation of our efforts to overcome this problem we report the evaluation of one cyclic selenoanhydride (1) and ten selenoesters (2-11) in MDR human colon adenocarcinoma Colo 320 cell line. The most potent derivatives (1, 9-11) inhibited the ABCB1 efflux pump much stronger than the reference compound verapamil. Particularly, the best one (9) was 4-fold more potent than verapamil at a 10-fold lower concentration. Furthermore, the evaluated derivatives exerted a potent and selective cytotoxic activity. In addition, they were strong apoptosis inducers as the four derivatives triggered apoptotic events in a 64-72% of the examined MDR Colo 320 human adenocarcinoma cells.}, year = {2017}, eissn = {1464-3405}, pages = {797-802}, orcid-numbers = {Gajdács, Márió/0000-0003-1270-0365; Spengler, Gabriella/0000-0001-8085-0950} } @article{MTMT:2901785, title = {Reversal of ABCB1-related Multidrug Resistance of Colonic Adenocarcinoma Cells by Phenothiazines.}, url = {https://m2.mtmt.hu/api/publication/2901785}, author = {Takács, Daniella and Csonka, Ákos and Horváth, Ádám and Windt, Tímea and Gajdács, Márió and Riedl, Zsuzsanna and Hajós, György and Amaral, L and Molnár, József and Spengler, Gabriella}, journal-iso = {ANTICANCER RES}, journal = {ANTICANCER RESEARCH}, volume = {35}, unique-id = {2901785}, issn = {0250-7005}, abstract = {BACKGROUND: The most common mechanism that reduces the efficacy of anticancer agents is overexpression of ATP-binding cassette (ABC) drug transporters. Phenothiazines and structurally-related compounds can sensitize multidrug-resistant (MDR) cells to chemotherapeutics. MATERIALS AND METHODS: Phenothiazine derivatives were investigated regarding their anticancer and MDR-reversing effect on colonic adenocarcinoma cells. The anti-proliferative and cytotoxic effects of the derivatives were assessed by the thiazolyl blue tetrazolium bromide (MTT) method, the modulation of the ABCB1 activity was measured by rhodamine 123 accumulation assay using flow cytometry. RESULTS: All phenothiazines exhibited potent cytotoxic effect on the sensitive and MDR colon adenocarcinoma cell lines. The inhibition of the ABCB1 transporter was greater in the presence of the phenothiazine derivatives than for the known ABCB1 inhibitor verapamil. CONCLUSION: It can be concluded that these derivatives show synergism in the presence of doxorubicin and could have potential as ABCB1 inhibitors.}, year = {2015}, eissn = {1791-7530}, pages = {3245-3251}, orcid-numbers = {Windt, Tímea/0000-0001-9913-3337; Gajdács, Márió/0000-0003-1270-0365; Spengler, Gabriella/0000-0001-8085-0950} }