Vol.:(0123456789) 1 3 Molecular Diversity https://doi.org/10.1007/s11030-019-10014-z ORIGINAL ARTICLE Antiproliferative activity and apoptosis induction, of organo‑antimony(III)–copper(I) conjugates, against human breast cancer cells C. N. Banti 1  · V. Tsiatouras 1  · K. Karanicolas 1  · N. Panagiotou 2  · A. J. Tasiopoulos 2  · N. Kourkoumelis 3  · S. K. Hadjikakou 1 Received: 25 September 2019 / Accepted: 2 November 2019 © Springer Nature Switzerland AG 2019 Abstract Three known organo-antimony(III)–copper(I), mixed-metal small bioactive molecules (SBAMs) of formula [Cu(tpSb) 3 Cl] (1), [Cu 2 (tpSb) 4 Br 2 ] (2) and [Cu 2 (tpSb) 4 I 2 ] (3) (tpSb = triphenylstibine) were used for the clarifcation of their antiproliferative activity against human breast cancer cells: MCF-7 (hormone-dependent cells) and MDA-MB-231 (hormone-independent cells). The in vitro toxicity of 1–3 was studied against normal human foetal lung fbroblast cells (MRC-5). The genotoxicity of 1–3 was determined by the presence of micronucleus. The type of the cell death caused by 1–3 was determined using cell cycle arrest. The molecular mechanism of action of 1–3 was defned by their binding afnity towards CT-DNA (calf thymus DNA) using UV spectroscopy and viscosity measurements. Docking studies depict the interactions between 1–3 and DNA. Computations were also employed in order to rationalize the activity of these compounds. This is based on the contribution of metal aromaticity in the case of compounds 2 and 3 where the short Cu···Cu distance (2.7724(6) (2) and 2.7251(11) (3) Ǻ, respectively) suggests d 10 –d 10 interaction between metal centres. Electronic supplementary material The online version of this article (https://doi.org/10.1007/s11030-019-10014-z) contains supplementary material, which is available to authorized users. * C. N. Banti cbanti@uoi.gr * N. Kourkoumelis nkourkou@uoi.gr * S. K. Hadjikakou shadjika@uoi.gr 1 Section of Inorganic and Analytical Chemistry, Department of Chemistry, University of Ioannina, 45110 Ioannina, Greece 2 Department of Chemistry, University of Cyprus, 1678 Nicosia, Cyprus 3 Medical Physics Laboratory, Medical School, University of Ioannina, Ioannina, Greece