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Synthesis, characterization and biological evaluation of six highly cytotoxic ruthenium(ii) complexes with 4'-substituted-2,2':6',2''-terpyridine.


ABSTRACT: Herein, six ruthenium(ii) terpyridine complexes, i.e. [RuCl2(4-EtN-Phtpy)(DMSO)] (Ru1), [RuCl2(4-MeO-Phtpy)(DMSO)] (Ru2), [RuCl2(2-MeO-Phtpy)(DMSO)] (Ru3), [RuCl2(3-MeO-Phtpy)(DMSO)] (Ru4), [RuCl2(1-Bip-Phtpy)(DMSO)] (Ru5), and [RuCl2(1-Pyr-Phtpy)(DMSO)] (Ru6) with 4'-(4-diethylaminophenyl)-2,2':6',2''-terpyridine (4-EtN-Phtpy), 4'-(4-methoxyphenyl)-2,2':6',2''-terpyridine (4-MeO-Phtpy), 4'-(2-methoxyphenyl)-2,2':6',2''-terpyridine (2-MeO-Phtpy), 4'-(3-methoxyphenyl)-2,2':6',2''-terpyridine (3-MeO-Phtpy), 4'-(1-biphenylene)-2,2':6',2''-terpyridine (1-Bip-Phtpy), and 4'-(1-pyrene)-2,2':6',2''-terpyridine (1-Pyr-Phtpy), respectively, were synthesized and fully characterized. The MTT assay demonstrates that the in vitro anticancer activity of Ru1 is higher than that of Ru2-Ru6 and more selective for Hep-G2 cells than for normal HL-7702 cells. In addition, various biological assays show that Ru1 and Ru6, especially the Ru1 complex, are telomerase inhibitors targeting c-myc G4 DNA and also cause apoptosis of Hep-G2 cells. With the same Ru center, the in vitro antitumor activity and cellular uptake ability of the 4-EtN-Phtpy and 1-Bip-Phtpy ligands follow the order 4-EtN-Phtpy > 1-Bip-Phtpy.

SUBMITTER: Qin QP 

PROVIDER: S-EPMC6072480 | biostudies-literature | 2018 Mar

REPOSITORIES: biostudies-literature

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Synthesis, characterization and biological evaluation of six highly cytotoxic ruthenium(ii) complexes with 4'-substituted-2,2':6',2''-terpyridine.

Qin Qi-Pin QP   Meng Ting T   Tan Ming-Xiong MX   Liu Yan-Cheng YC   Wang Shu-Long SL   Zou Bi-Qun BQ   Liang Hong H  

MedChemComm 20180202 3


Herein, six ruthenium(ii) terpyridine complexes, <i>i.e.</i> [RuCl<sub>2</sub>(4-EtN-Phtpy)(DMSO)] (<b>Ru1</b>), [RuCl<sub>2</sub>(4-MeO-Phtpy)(DMSO)] (<b>Ru2</b>), [RuCl<sub>2</sub>(2-MeO-Phtpy)(DMSO)] (<b>Ru3</b>), [RuCl<sub>2</sub>(3-MeO-Phtpy)(DMSO)] (<b>Ru4</b>), [RuCl<sub>2</sub>(1-Bip-Phtpy)(DMSO)] (<b>Ru5</b>), and [RuCl<sub>2</sub>(1-Pyr-Phtpy)(DMSO)] (<b>Ru6</b>) with 4'-(4-diethylaminophenyl)-2,2':6',2''-terpyridine (4-EtN-Phtpy), 4'-(4-methoxyphenyl)-2,2':6',2''-terpyridine (4-MeO-Ph  ...[more]

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