TY - JOUR AU - Gajdács, Márió AU - Spengler, Gabriella AU - Sanmartin, C AU - Marc, MA AU - Handzlik, J AU - Dominguez-Alvarez, E TI - Selenoesters and selenoanhydrides as novel multidrug resistance reversing agents: A confirmation study in a colon cancer MDR cell line JF - BIOORGANIC & MEDICINAL CHEMISTRY LETTERS J2 - BIOORG MED CHEM LETT VL - 27 PY - 2017 IS - 4 SP - 797 EP - 802 PG - 6 SN - 0960-894X DO - 10.1016/j.bmcl.2017.01.033 UR - https://m2.mtmt.hu/api/publication/3179770 ID - 3179770 N1 - Megjegyzés-26430381 N1 Funding details: ESF, European Social Fund N1 Funding details: MTA, Magyar Tudományos Akadémia N1 Funding text: The authors are grateful to Mrs. Anikó Váradi Vigyikán for laboratory work and assistance; and to Prof. Dr. Juan Antonio Palop for his contribution and guidance in the design and structural characterization of the derivatives. This study was supported by the Szeged Foundation for Cancer Research, the European Union and the State of Hungary, co-financed by the European Social Fund in the framework of TÁMOP 4.2.4. A/2-11-1-2012-0001 ‘National Excellence Program’. This paper was also supported by the János Bolyai Research Scholarship of the Hungarian Academy of Sciences. Megjegyzés-26430390 N1 Funding details: ESF, European Social Fund N1 Funding details: MTA, Magyar Tudományos Akadémia N1 Funding text: The authors are grateful to Mrs. Anikó Váradi Vigyikán for laboratory work and assistance; and to Prof. Dr. Juan Antonio Palop for his contribution and guidance in the design and structural characterization of the derivatives. This study was supported by the Szeged Foundation for Cancer Research, the European Union and the State of Hungary, co-financed by the European Social Fund in the framework of TÁMOP 4.2.4. A/2-11-1-2012-0001 ‘National Excellence Program’. This paper was also supported by the János Bolyai Research Scholarship of the Hungarian Academy of Sciences. Funding Agency and Grant Number: Szeged Foundation for Cancer Research; European UnionEuropean Union (EU); State of Hungary; European Social FundEuropean Social Fund (ESF) [TAMOP 4.2.4. A/2-11-1-2012-0001]; Janos Bolyai Research Scholarship of the Hungarian Academy of SciencesHungarian Academy of Sciences Funding text: The authors are grateful to Mrs. Aniko Varadi Vigyikan for laboratory work and assistance; and to Prof. Dr. Juan Antonio Palop for his contribution and guidance in the design and structural characterization of the derivatives. This study was supported by the Szeged Foundation for Cancer Research, the European Union and the State of Hungary, co-financed by the European Social Fund in the framework of TAMOP 4.2.4. A/2-11-1-2012-0001 'National Excellence Program'. This paper was also supported by the Janos Bolyai Research Scholarship of the Hungarian Academy of Sciences. Department of Medical Microbiology and Immunobiology, Faculty of Medicine, University of Szeged, Dóm tér 10, Szeged, 6720, Hungary Department of Organic and Pharmaceutical Chemistry, School of Pharmacy, University of Navarra, Irunlarrea 1, Pamplona, 31010, Spain Department of Technology and Biotechnology of Drugs, Jagiellonian University Medical College, Medyczna 9, Kraków, 30-688, Poland Cited By :23 Export Date: 31 July 2020 CODEN: BMCLE Correspondence Address: Domínguez-Álvarez, E.; Department of Technology and Biotechnology of Drugs, Jagiellonian University Medical College, Medyczna 9, Poland; email: enriquedominguezalv@gmail.com Chemicals/CAS: dimethyl sulfoxide, 67-68-5; verapamil, 152-11-4, 52-53-9; multidrug resistance protein, 149200-37-3, 208997-77-7; ABCB1 protein, human; Anhydrides; Antineoplastic Agents; Esters; Organoselenium Compounds; P-Glycoproteins; Verapamil Funding details: European Social Fund, ESF, A/2-11-1-2012-0001 Funding details: European Commission, EC Funding details: Magyar Tudományos Akadémia, MTA Funding text 1: The authors are grateful to Mrs. Anik? V?radi Vigyik?n for laboratory work and assistance; and to Prof. Dr. Juan Antonio Palop for his contribution and guidance in the design and structural characterization of the derivatives. This study was supported by the Szeged Foundation for Cancer Research, the European Union and the State of Hungary, co-financed by the European Social Fund in the framework of T?MOP 4.2.4. A/2-11-1-2012-0001 ?National Excellence Program?. This paper was also supported by the J?nos Bolyai Research Scholarship of the Hungarian Academy of Sciences. Department of Medical Microbiology and Immunobiology, Faculty of Medicine, University of Szeged, Dóm tér 10, Szeged, 6720, Hungary Department of Organic and Pharmaceutical Chemistry, School of Pharmacy, University of Navarra, Irunlarrea 1, Pamplona, 31010, Spain Department of Technology and Biotechnology of Drugs, Jagiellonian University Medical College, Medyczna 9, Kraków, 30-688, Poland Cited By :30 Export Date: 18 January 2021 CODEN: BMCLE Correspondence Address: Domínguez-Álvarez, E.; Department of Technology and Biotechnology of Drugs, Jagiellonian University Medical College, Medyczna 9, Poland; email: enriquedominguezalv@gmail.com Chemicals/CAS: dimethyl sulfoxide, 67-68-5; verapamil, 152-11-4, 52-53-9; multidrug resistance protein, 149200-37-3, 208997-77-7; ABCB1 protein, human; Anhydrides; Antineoplastic Agents; Esters; Organoselenium Compounds; P-Glycoproteins; Verapamil Funding details: European Social Fund, ESF, A/2-11-1-2012-0001 Funding details: Magyar Tudományos Akadémia, MTA Funding details: European Commission, EC Funding text 1: The authors are grateful to Mrs. Anik? V?radi Vigyik?n for laboratory work and assistance; and to Prof. Dr. Juan Antonio Palop for his contribution and guidance in the design and structural characterization of the derivatives. This study was supported by the Szeged Foundation for Cancer Research, the European Union and the State of Hungary, co-financed by the European Social Fund in the framework of T?MOP 4.2.4. A/2-11-1-2012-0001 ?National Excellence Program?. This paper was also supported by the J?nos Bolyai Research Scholarship of the Hungarian Academy of Sciences. AB - 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. LA - English DB - MTMT ER - TY - JOUR AU - Takács, Daniella AU - Csonka, Ákos AU - Horváth, Ádám AU - Windt, Tímea AU - Gajdács, Márió AU - Riedl, Zsuzsanna AU - Hajós, György AU - Amaral, L AU - Molnár, József AU - Spengler, Gabriella TI - Reversal of ABCB1-related Multidrug Resistance of Colonic Adenocarcinoma Cells by Phenothiazines. JF - ANTICANCER RESEARCH J2 - ANTICANCER RES VL - 35 PY - 2015 IS - 6 SP - 3245 EP - 3251 PG - 7 SN - 0250-7005 UR - https://m2.mtmt.hu/api/publication/2901785 ID - 2901785 AB - 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. LA - English DB - MTMT ER -