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Antioxidant-inspired drug discovery: antitumor metabolite is formed in situ from a hydroxycinnamic acid derivative upon free radical scavenging.
dc.creator | Fási, Laura | |
dc.creator | Di Meo, Florent | |
dc.creator | Kuo, Ching-Ying | |
dc.creator | Stojković Burić, Sonja | |
dc.creator | Martins, Ana | |
dc.creator | Kúsz, Norbert | |
dc.creator | Béni, Zoltán | |
dc.creator | Dékány, Miklós | |
dc.creator | Balogh, György Tibor | |
dc.creator | Pešić, Milica | |
dc.creator | Wang, Hui-Chun | |
dc.creator | Trouillas, Patrick | |
dc.creator | Hunyadi, Attila | |
dc.date.accessioned | 2019-03-01T08:31:37Z | |
dc.date.available | 2019-03-01T08:31:37Z | |
dc.date.issued | 2019 | |
dc.identifier.issn | 0022-2623 | |
dc.identifier.uri | http://pubs.acs.org/doi/10.1021/acs.jmedchem.8b01994 | |
dc.identifier.uri | https://radar.ibiss.bg.ac.rs/handle/123456789/3278 | |
dc.description.abstract | Cancer cells generally possess higher levels of reactive oxygen species than normal cells, and this can serve as a possible therapeutic target. In this proof-of-concept study, an antioxidant-inspired drug discovery strategy was evaluated using a hydroxycinnamic acid derivative. The processing of oxidized mixtures of p-coumaric acid methyl ester (pcm) revealed a new antitumor lead, graviquinone. Graviquinone bypassed ABCB1-mediated resistance, induced DNA damage in lung carcinoma cells but exerted DNA protective activity in normal keratinocytes, and modulated DNA damage response in MCF-7 cells. The cytotoxic effect of pcm in MCF-7 cells was potentiated under H2O2-induced oxidative stress, and the formation of graviquinone was confirmed by Fenton's reaction on pcm. In silico DFT calculations suggested graviquinone as a kinetic product of pcm scavenging •OH radicals. Our results demonstrate the pharmacological value of an in situ-formed, oxidative stress-related metabolite of an antioxidant. This might be of particular importance for designing new strategies for antioxidant-based drug discovery. | en |
dc.relation | COST Action CM1407 | |
dc.relation | National Research, Developmentand Innovation Office, Hungary (NKFIH; K119770) | |
dc.relation | Ministryof Human Capacities, Hungary grant 20391-3/2018/FEKUS-TRAT | |
dc.relation | Czech ScienceFoundation (P208/12/G016 | |
dc.relation | National Program ofSustainability I from the Ministry-of-Youth, Education andSports of the Czech Republic (LO1305) | |
dc.relation | UNKP-18-4 New National Excellence Program of theMinistry of Human Capacitie | |
dc.relation | János Bolyaifellowship of the Hungarian Academy of Sciences | |
dc.relation | Kálmán Szász Prize | |
dc.relation | ungarian Academy ofSciences | |
dc.relation | Ministry of Science and Technology, Taiwan(MOST 107-2911-I-037-502) | |
dc.rights | restrictedAccess | |
dc.source | Journal of Medicinal Chemistry | |
dc.title | Antioxidant-inspired drug discovery: antitumor metabolite is formed in situ from a hydroxycinnamic acid derivative upon free radical scavenging. | en |
dc.type | article | en |
dc.rights.license | ARR | |
dcterms.abstract | Хунyади, Aттила; Пешић, Милица; Стојковић Бурић, Соња; Фáси, Лаура; Ди Мео, Флорент; Куо, Цхинг-Yинг; Мартинс, Aна; Кúсз, Норберт; Бéни, Золтáн; Дéкáнy, Миклóс; Балогх, Гyöргy Тибор; Wанг, Хуи-Цхун; Троуиллас, Патрицк; | |
dc.rights.holder | © 2019 American Chemical Society. | |
dc.citation.issue | 3 | |
dc.citation.volume | 62 | |
dc.identifier.doi | 10.1021/acs.jmedchem.8b01994 | |
dc.identifier.pmid | 30615450 | |
dc.identifier.scopus | 2-s2.0-85061622730 | |
dc.identifier.wos | 000459223600036 | |
dc.citation.apa | Fási, L., Di Meo, F., Kuo, C.-Y., Stojkovic Buric, S., Martins, A., Kúsz, N., … Hunyadi, A. (2019). Antioxidant-inspired drug discovery: antitumor metabolite is formed in situ from a hydroxycinnamic acid derivative upon free radical scavenging. Journal of Medicinal Chemistry, 62(3), 1657–1668. | |
dc.citation.vancouver | Fási L, Di Meo F, Kuo C-Y, Stojkovic Buric S, Martins A, Kúsz N, Béni Z, Dékány M, Balogh GT, Pesic M, Wang H-C, Trouillas P, Hunyadi A. Antioxidant-inspired drug discovery: antitumor metabolite is formed in situ from a hydroxycinnamic acid derivative upon free radical scavenging. J Med Chem. 2019;62(3):1657–68. | |
dc.citation.spage | 1657 | |
dc.citation.epage | 1668 | |
dc.type.version | publishedVersion | en |
dc.citation.rank | aM21 |
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