Pilon, Adhan and Avecilla, Fernando and Rácz, Bálint and Gátszegi, Gerda T. and Spengler, Gabriella (2023) Iron(II)-cyclopentadienyl compounds are cytotoxic against colon adenocarcinoma cell lines: Ethylenebis(diphenylphosphane) vs. triphenylphosphane. JOURNAL OF INORGANIC BIOCHEMISTRY, 249. ISSN 0162-0134
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Abstract
Structure-activity studies aiming to understand the role of each coligand in the formulation of new metallodrugs is an important subject. In that frame, six new compounds with general formula [Fe(η5-C5H5)(dppe)(L)][CF3SO3] with L = benzonitriles (1–4) or carbon monoxide (5) and compound [Fe(η5 -C5H5)(CO)(PPh3)2][CF3SO3] (6) were synthesized and compared with three other previously reported compounds [Fe(η5-C5H5)(CO)(L)(PPh3)][CF3SO3]. We were particularly interested in assessing the effect of dppe vs. (PPh3 + CO) for this set of compounds. For that, all compounds were tested against two human colon adenocarcinoma cell lines, Colo205 and the refractile Colo320 (expressing ABCB1, an efflux pump causing multidrug resistance), showing IC50 values in the micromolar range. The presence of dppe in the compound’s coordination sphere over (PPh3 + CO) allows for more redox stable compounds showing higher cytotoxicity and selectivity, with improved cytotoxicity towards resistant cells that is not related to the inhibition of ABCB1. Further studies with GSH and H2O2 for selected compounds indicated that their antioxidant ability is not probably the main responsible for their cytotoxicity.
Item Type: | Article |
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Additional Information: | This work was funded by Fundação para a Ciência e a Tecnologia (FCT), I.P./MCTES through national funds (PIDDAC) - UIDB/00100/2020, UIDP/00100/2020 and LA/P/0056/2020. Andreia Valente acknowledges CEECIND 2017 (CEECIND/01974/2017; acknowledging FCT, as well as POPH and FSE—European Social Fund). A. P. thank FCT for his Ph.D. Grant (SFRH/BD/139412/2018 and COVID/BD/153267/2023). B.R. was supported by the Szeged Foundation for Cancer Research (Szegedi Rákkutatásért Alapítvány). G.S. was supported by the János Bolyai Research Scholarship (BO/00158/22/5) of the Hungarian Academy of Sciences and by the ÚNKP-22-5-SZTE-588 New National Excellence Program of the Ministry for Culture and Innovation from the source of the National Research, Development and Innovation Fund. |
Subjects: | Q Science / természettudomány > QD Chemistry / kémia > QD03 Inorganic chemistry / szervetlen kémia Q Science / természettudomány > QH Natural history / természetrajz > QH301 Biology / biológia > QH3011 Biochemistry / biokémia |
SWORD Depositor: | MTMT SWORD |
Depositing User: | MTMT SWORD |
Date Deposited: | 13 Oct 2023 07:47 |
Last Modified: | 13 Oct 2023 07:47 |
URI: | http://real.mtak.hu/id/eprint/176668 |
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