Synthesis, anticancer activities and experimental-theoretical DNA interaction studies of 2-amino-4-phenyl-4H-benzo[h]chromene-3-carbonitrile

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dc.creatorBraga, Taniris Cafiero
dc.creatorSilva, Marina de Magalhães
dc.creatorNascimento, Eduarda O. O.
dc.creatorSilva, Edjan Carlos Dantas da
dc.creatorRego, Yuri de Freitas
dc.creatorMandal, Mullicka
dc.creatorSouza, Zaqueu Alves de
dc.creatorRuiz, Ana Lúcia Tasca Gois
dc.creatorCarvalho, João Ernesto de
dc.creatorMartins, Felipe Terra
dc.date.accessioned2023-12-06T11:48:59Z
dc.date.available2023-12-06T11:48:59Z
dc.date.issued2022
dc.description.abstractTwenty chromenes were synthesized with good to excellent yields (70–96%). From the series of chromenes herein tested, compounds 14, 12, 15, 16, 17, 18, and 20 were the most potent throughout the cancer human cell lines tested. In general, the para-position electron-withdrawing substituents on the phenyl ring are favored towards potency and selectivity for cancer cells. Biophysical studies were performed with eight chromene derivatives (13-20) and ctDNA to evaluate possible biological targets. The molecular fluorescence verified that compound 16 presented a higher binding constant (Kb) with the ctDNA, agreeing with in vitro biological results and that evaluated chromenes derivatives interact preferentially via intercalation. Finally, an inverse linear correlation (logKb vs. GI50) was observed for six human carcinogenic cell lines; hence, the mechanism of action of these compounds may be related to DNA interaction.
dc.identifier.citationBRAGA, Taniris Cafiero et al. Synthesis, anticancer activities and experimental-theoretical DNA interaction studies of 2-amino-4-phenyl-4H-benzo[h]chromene-3-carbonitrile. European Journal of Medicinal Chemistry Reports, Amsterdam, v. 4, e100030, 2022. DOI: 10.1016/j.ejmcr.2022.100030. Disponível em: https://www.sciencedirect.com/science/article/pii/S2772417422000024?via%3Dihub. Acesso em: 30 nov. 2023.
dc.identifier.doi10.1016/j.ejmcr.2022.100030
dc.identifier.issne- 2772-4174
dc.identifier.urihttp://repositorio.bc.ufg.br//handle/ri/23911
dc.language.isoeng
dc.publisher.countryHolanda
dc.publisher.departmentInstituto de Química - IQ (RMG)
dc.rightsAcesso Aberto
dc.rights.urihttp://creativecommons.org/licenses/by-nc-nd/4.0/
dc.subjectChromene
dc.subjectAntiproliferative activity
dc.subjectBioanalytical correlation
dc.subjectDNA interaction
dc.subjectIntercalation
dc.titleSynthesis, anticancer activities and experimental-theoretical DNA interaction studies of 2-amino-4-phenyl-4H-benzo[h]chromene-3-carbonitrile
dc.typeArtigo

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