TY - JOUR AU - Ali, Hazhmat AU - Traj, Péter AU - Szebeni, Gábor AU - Gémes, Nikolett AU - Resch, Vivien Erzsébet AU - Paragi, Gábor AU - Mernyák, Erzsébet AU - Minorics, Renáta AU - Zupkó, István TI - Investigation of the Antineoplastic Effects of 2-(4-Chlorophenyl)-13α-Estrone Sulfamate against the HPV16-Positive Human Invasive Cervical Carcinoma Cell Line SiHa JF - INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES J2 - INT J MOL SCI VL - 24 PY - 2023 IS - 7 PG - 17 SN - 1661-6596 DO - 10.3390/ijms24076625 UR - https://m2.mtmt.hu/api/publication/33727646 ID - 33727646 N1 - Funding Agency and Grant Number: Hungarian Research Foundation (NKFI) [K 143690, 142877 FK22, OTKA SNN 139323, 2020-1.1.6-JOEVO-2021-00003, TKP2021-EGA-32, TKP2021-EGA-17]; Ministry of Innovation and Technology of Hungary from the National Research, Development and Innovation Fund [TKP2021-EGA]; Nemzet Fiatal Tehetsegeiert OEsztoendij [NTP-NFTOE-21-B-0113]; New National Excellence Program of the Ministry for Innovation and Technology [UNKP-22-5-SZTE-535]; Janos Bolyai Research Scholarship of the Hungarian Academy of Sciences [BO/00582/22/8]; KDP-2021 Program of the Ministry for Innovation and Technology from the source of the National Research, Development and Innovation Fund [C1764415 KDP/2021] Funding text: This research was funded by Hungarian Research Foundation (NKFI), grant numbers K 143690, 142877 FK22, OTKA SNN 139323, and 2020-1.1.6-JOEVO-2021-00003. Projects no. TKP2021-EGA-32 and TKP2021-EGA-17 have been implemented with support provided by the Ministry of Innovation and Technology of Hungary from the National Research, Development and Innovation Fund, financed under the TKP2021-EGA funding scheme. The support provided by Nemzet Fiatal Tehetsegeiert OEsztoendij (NTP-NFTOE-21-B-0113) is also acknowledged. This work was supported by the UNKP-22-5-SZTE-535 New National Excellence Program of the Ministry for Innovation and Technology and by the Janos Bolyai Research Scholarship of the Hungarian Academy of Sciences BO/00582/22/8. Supported by the KDP-2021 Program of the Ministry for Innovation and Technology from the source of the National Research, Development and Innovation Fund for NG (C1764415 KDP/2021). AB - Cervical carcinoma is one of the most frequent malignant gynecological cancers in women of reproductive age. Because of the poor tolerability of currently available chemotherapeutic agents, efforts have been focused on developing innovative molecules, including steroids, that exert antineoplastic effects with a better safety profile. In addition to their endocrine properties, certain estrogens exhibit additional biological activities, such as antiangiogenic and anticancer effects. Based on previous studies, the antineoplastic properties of 13α-estrone sulfamate derivatives (13AES1-3) were investigated, and the mechanism of action for the most promising compound 13AES3 was explored. Based on their effects on the viability of different human adherent gynecological cancer cells, the SiHa cervical cell line was used for mechanistic experiments. The most active analog 13AES3 was shown to exert considerable proapoptotic effects, as evidenced by a colorimetric caspase-3 assay and fluorescent double staining. It also elicited antimigratory and anti-invasive effects in a concentration-dependent manner, as evidenced by wound healing and Boyden chamber assays, respectively. Regarding their mechanism of action, 13AES derivatives were shown to inhibit tubulin polymerization, and computer simulations provided a possible explanation for the importance of the presence of the chlorophenyl ring on the estrane skeleton. 13AES3 is considered to be the first 13α-estrone derivative with a significant antineoplastic potency against SiHa cancer cells. Therefore, it might serve as a valuable lead molecule for the design of anticancer agents targeting cervical carcinomas. LA - English DB - MTMT ER - TY - JOUR AU - Kovács, Édua AU - Ali, Hazhmat AU - Minorics, Renáta AU - Traj, Péter AU - Resch, Vivien Erzsébet AU - Paragi, Gábor AU - Bruszel, Bella AU - Zupkó, István AU - Mernyák, Erzsébet TI - Synthesis and Antiproliferative Activity of Steroidal Diaryl Ethers JF - MOLECULES J2 - MOLECULES VL - 28 PY - 2023 IS - 3 PG - 17 SN - 1420-3049 DO - 10.3390/molecules28031196 UR - https://m2.mtmt.hu/api/publication/33594496 ID - 33594496 N1 - Funding Agency and Grant Number: National Research, Development and Innovation Office-NKFIH [OTKA SNN 139323, TKP2021-EGA-17] Funding text: This work was supported by National Research, Development and Innovation Office-NKFIH through projects OTKA SNN 139323 and TKP2021-EGA-17. AB - Novel 13α-estrone derivatives have been synthesized via direct arylation of the phenolic hydroxy function. Chan–Lam couplings of arylboronic acids with 13α-estrone as a nucleophilic partner were carried out under copper catalysis. The antiproliferative activities of the newly synthesized diaryl ethers against a panel of human cancer cell lines (A2780, MCF-7, MDA-MB 231, HeLa, SiHa) were investigated by means of MTT assays. The quinoline derivative displayed substantial antiproliferative activity against MCF-7 and HeLa cell lines with low micromolar IC50 values. Disturbance of tubulin polymerization has been confirmed by microplate-based photometric assay. Computational calculations reveal significant interactions of the quinoline derivative with the taxoid binding site of tubulin. LA - English DB - MTMT ER - TY - CHAP AU - Ali, Hazhmat AU - Mernyák, Erzsébet AU - Traj, Péter AU - Gábor, J. Szebeni AU - Minorics, Renáta AU - Zupkó, István ED - Muszynska, Bozena TI - In Vitro Evaluation of Antiproliferative and Antimetastatic Activity of the Newly Synthesized 2-(4-Chlorophenyl)-13α-Estrone Sulfamate T2 - Natural vs. Artificial Networks: The Usefulness of the Concept in Health, Life, and Technical Sciences PB - Zakład Optymalizacji Zawodowej Ośrodek Umea Shinoda-Kuracejo CY - Martin CY - Krakow CY - Szeged SN - 9788395955457 PY - 2022 SP - 81 EP - 82 PG - 2 UR - https://m2.mtmt.hu/api/publication/33338885 ID - 33338885 LA - English DB - MTMT ER - TY - CONF AU - Ali, Hazhmat AU - Mernyák, Erzsébet AU - Traj, Péter AU - Szebeni, Gábor AU - Minorics, Renáta AU - Zupkó, István TI - Investigation of the anticancer potentials of the newly synthesized 13α- estrone derivatives T2 - 11th ISCTICO – HUPHAR – IUPHAR – CONFERENCE PY - 2021 SP - 76 EP - 76 PG - 1 UR - https://m2.mtmt.hu/api/publication/32585798 ID - 32585798 LA - English DB - MTMT ER - TY - JOUR AU - Traj, Péter AU - Ali, Hazhmat AU - Motzwickler-Németh, Anett AU - Dajcs, Sámuel Trisztán AU - Tömösi, Ferenc AU - Tea, Lanisnik-Rizner AU - Zupkó, István AU - Mernyák, Erzsébet TI - Transition metal-catalyzed A-ring C–H activations and C(sp2)–C(sp2) couplings in the 13α-estrone series and in vitro evaluation of antiproliferative properties JF - JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY J2 - J ENZYM INHIB MED CH VL - 36 PY - 2021 IS - 1 SP - 895 EP - 902 PG - 8 SN - 1475-6366 DO - 10.1080/14756366.2021.1900165 UR - https://m2.mtmt.hu/api/publication/31916683 ID - 31916683 LA - English DB - MTMT ER - TY - CHAP AU - Traj, Péter AU - Ali, Hazhmat AU - Anett, Németh AU - Sámuel, Trisztán Dajcs AU - Zupkó, István AU - Mernyák, Erzsébet ED - Alapi, Tünde ED - Berkecz, Róbert ED - Ilisz, István TI - Transition metal-catalyzed synthesis of 13α-estrone derivatives with potential anticancer properties T2 - Proceedings of the 26th International Symposium on Analytical and Environmental Problems PB - University of Szeged CY - Szeged SN - 9789633067710 PY - 2020 SP - 338 EP - 341 PG - 4 UR - https://m2.mtmt.hu/api/publication/32585831 ID - 32585831 LA - English DB - MTMT ER - TY - CHAP AU - Traj, Péter AU - Németh, Anett AU - Dajcs, Trisztán Sámuel AU - Mernyák, Erzsébet ED - Böszörményi, Éva ED - Kocsis, Marianna TI - Átmenetifém-katalizált keresztkapcsolási és C-H aktiválási reakciók a 13α-ösztron sorban T2 - XLIII. Kémiai Előadói Napok - Előadás összefoglalók PB - Szegedi Tudományegyetem (SZTE) CY - Szeged SN - 9786156018045 PY - 2020 SP - 69 EP - 75 PG - 7 UR - https://m2.mtmt.hu/api/publication/32582948 ID - 32582948 LA - Hungarian DB - MTMT ER - TY - JOUR AU - Szabados, Márton AU - Ádám, Anna Adél AU - Traj, Péter AU - Muráth, Szabolcs AU - Baán, Kornélia AU - Bélteky, Péter AU - Kónya, Zoltán AU - Kukovecz, Ákos AU - Sipos, Pál Miklós AU - Pálinkó, István TI - Mechanochemical and wet chemical syntheses of CaIn-layered double hydroxide and its performance in a transesterification reaction compared to those of other Ca2M(III) hydrocalumites (M: Al, Sc, V, Cr, Fe, Ga) and Mg(II)-, Ni(II)-, Co(II)- or Zn(II)-based hydrotalcites JF - JOURNAL OF CATALYSIS J2 - J CATAL VL - 391 PY - 2020 SP - 282 EP - 297 PG - 16 SN - 0021-9517 DO - 10.1016/j.jcat.2020.07.038 UR - https://m2.mtmt.hu/api/publication/31390677 ID - 31390677 LA - English DB - MTMT ER - TY - JOUR AU - Jójárt, Rebeka AU - Traj, Péter AU - Kovács, Édua AU - Horváth, Ágnes AU - Schneider, Gyula AU - Szécsi, Mihály AU - Pál, Attila AU - Paragi, Gábor AU - Mernyák, Erzsébet TI - Synthesis, Biological Evaluation and Docking Studies of 13-Epimeric 10-fluoro- and 10-Chloroestra-1,4-dien-3-ones as Potential Aromatase Inhibitors JF - MOLECULES J2 - MOLECULES VL - 24 PY - 2019 IS - 9 PG - 18 SN - 1420-3049 DO - 10.3390/molecules24091783 UR - https://m2.mtmt.hu/api/publication/30672179 ID - 30672179 N1 - WoS:hiba:000469518100142 2020-01-10 07:35 cikkazonosító nem egyezik LA - English DB - MTMT ER -