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In vitro and in vivo antiproliferative activity of organo-nickel SCS-pincer complexes on estrogen responsive MCF7 and MC4L2 breast cancer cells. Effect of amine fragments substitutions on the BSA binding and cytotoxicity

Abstract

A family of organonickel complexes has been prepared, fully characterized, and tested for their antiproliferative activity against estrogen-responsive human breast cancer cells (MCF7). The three SCS-type pincer ligands HL1, HL2, and HL3 and their corresponding Ni(II) complexes NiL1, NiL2, and NiL3 have been synthesized and fully characterized, including by single crystal diffraction studies for the complexes. The complexes possess square planar geometry with two symmetrical 5-membered nicekllacycles. Fluorescence spectroscopy, circular dichroism measurements, and molecular modeling studies were used to evaluate the protein binding and antiproliferative activities of these organometallic complexes both in vitro and in vivo. Fluorescence quenching was used to investigate Bovine serum albumin (BSA) interaction at different temperatures (293, 303 and 313 K), and the results were analyzed using classical Stern-Volmer equation, allowing us to propose a dynamic quenching mechanism. Studies in vitro on the antiproliferative activity of the three organonickel complexes against estrogen-responsive human breast cancer cells (MCF7) showed promising antitumor activity for NiL1 containing pyrrolidine fragments. In vivo administration of this compound significantly inhibits tumor growth in estrogen-dependent MC4L2 cancer cells in female BALB/c mice.

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Publication details

The article was received on 27 Jul 2018, accepted on 25 Oct 2018 and first published on 25 Oct 2018


Article type: Paper
DOI: 10.1039/C8DT03079K
Citation: Dalton Trans., 2018, Accepted Manuscript
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    In vitro and in vivo antiproliferative activity of organo-nickel SCS-pincer complexes on estrogen responsive MCF7 and MC4L2 breast cancer cells. Effect of amine fragments substitutions on the BSA binding and cytotoxicity

    M. Hosseini-Kharat, D. Zargarian, A. M. Alizadeh, K. Karami, M. Saeidifar, S. Khalighfard, L. Dubrulle, M. Zakariazadeh, J. Cloutier and Z. Sohrabijam, Dalton Trans., 2018, Accepted Manuscript , DOI: 10.1039/C8DT03079K

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