Nucleobase Derivatives as Building Blocks to Form Ru(II)-Based Complexes with High Cytotoxicity

dc.creatorCarvalho, Diogo E. L.
dc.creatorOliveira, Katia M.
dc.creatorBomfim, Larissa Mendes
dc.creatorSoares, Milena Botelho Pereira
dc.creatorBezerra, Daniel Pereira
dc.creatorBatista, Alzir A.
dc.creatorCorrea, Rodrigo S.
dc.date2020-04-07T17:19:25Z
dc.date2020-04-07T17:19:25Z
dc.date2020
dc.date.accessioned2023-09-26T21:00:52Z
dc.date.available2023-09-26T21:00:52Z
dc.identifierCARVALHO, Diogo E L et al. Derivatives as Building Blocks to Form Ru(II)-Based Complexes with High Cytotoxicity. ACS Omega, v. 5, p. 122-130, 2020.
dc.identifier2470-1343
dc.identifierhttps://www.arca.fiocruz.br/handle/icict/40670
dc.identifier10.1021/acsomega.9b01921
dc.identifier.urihttps://repositorioslatinoamericanos.uchile.cl/handle/2250/8867740
dc.descriptionBrazilian Research Agencies: FAPEMIG, FAPESB, FAPESP, CNPq and CAPES. D.E.L.C. thanks FAPEMIG for a fellowship, and K.M.O. is supported by a postdoctoral fellowship grant from CAPES (PNPD program). Also, R.S.C. would like to thank the financial support provided by PROPP/ UFOP, FAPEMIG (APQ-01674-18), and CNPq (grants 403588/2016-2 and 308370/2017-1). The authors thank the IFSC-USP (E.E. Castellano and J.A. Ellena) for X-ray crystallography measurements and the “Laboratório Multiusuário de Caracterização de Moléculas”/UFOP for the NMR facilities.
dc.descriptionTwo new Ru(II)-based complexes containing 2-thiouracil derivatives, known as 2-thiouracil (2TU) and 6-methyl-2-thiouracil (6m2TU), were synthesized using cis,trans-[RuCl2(PPh3)2(bipy)] as a precursor. The obtained compounds with a general formula trans-[Ru(2TU)(PPh3)2(bipy)]PF6 (1) and trans-[Ru(6m2TU)(PPh3)2(bipy)]PF6 (2) were characterized by analytical techniques such as NMR, UV-vis, and IR spectroscopies, elementary analysis, mass spectrometry, and single-crystal X-ray diffraction. Moreover, the investigation of the complexes-DNA interaction were carried out using spectrophotometric titrations and showed that the complexes present a weak interaction with this biomolecule. The compounds were evaluated against HL-60, K-562, HepG2, and B16-F10 cancer cells and against noncancer cells (PBMCs). The results of the biological assay revealed that complex 2 is more promising than complex 1. Finally, the present study suggests that complexes 1 and 2 causes cell death by apoptosis, significantly increasing the percentage of apoptotic HL-60 cells, in which the compounds altered the cell cycle, reducing the cells in G1/G0, G2/M, and S phases.
dc.formatapplication/pdf
dc.languagepor
dc.publisherAmerican Chemical Society:
dc.rightsopen access
dc.subjectProteínas Transportadoras de Nucleobases
dc.subjectCitotoxicidade Imunológica
dc.subjectPirimidinas
dc.subjectTratamento Farmacológico
dc.subjectNucleobase Transport Proteins
dc.subjectCytotoxicity, Immunologic
dc.subjectPyrimidines
dc.subjectDrug Therapy
dc.titleNucleobase Derivatives as Building Blocks to Form Ru(II)-Based Complexes with High Cytotoxicity
dc.typeArticle


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