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

ABSTRACT: Two 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.

SUBMITTER: Carvalho DEL 

PROVIDER: S-EPMC6963899 | biostudies-literature | 2020 Jan

REPOSITORIES: biostudies-literature

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

Carvalho Diogo E L DEL   Oliveira Katia M KM   Bomfim Larissa M LM   Soares Milena B P MBP   Bezerra Daniel P DP   Batista Alzir A AA   Correa Rodrigo S RS  

ACS omega 20200103 1

Two new Ru(II)-based complexes containing 2-thiouracil derivatives, known as 2-thiouracil (2TU) and 6-methyl-2-thiouracil (6m2TU), were synthesized using <i>cis,trans-</i>[RuCl<sub>2</sub>(PPh<sub>3</sub>)<sub>2</sub>(bipy)] as a precursor. The obtained compounds with a general formula <i>trans-</i>[Ru(2TU)(PPh<sub>3</sub>)<sub>2</sub>(bipy)]PF<sub>6</sub> (<b>1</b>) and <i>trans-</i>[Ru(6m2TU)(PPh<sub>3</sub>)<sub>2</sub>(bipy)]PF<sub>6</sub> (<b>2</b>) were characterized by analytical techniqu  ...[more]

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