Structural and in vitro biological studies of organotin(IV) precursors; Selective inhibitory activity against human breast cancer cells, positive to estrogen receptors

 
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2012 (EN)
Structural and in vitro biological studies of organotin(IV) precursors; Selective inhibitory activity against human breast cancer cells, positive to estrogen receptors (EN)

V.Ξ™. Balas, C.N. Banti, N. Kourkoumelis, S.K. Hadjikakou, G.D Geromichalos, D. Sahpazidou, L. Male, M.B. Hursthouse, B. Bednarz, M. Kubicki, K. Charalabopoulos and (EN)

Πανεπιστήμιο Ιωαννίνων. Σχολή Θετικών Επιστημών. Τμήμα Χημείας (EL)
V.Ξ™. Balas, C.N. Banti, N. Kourkoumelis, S.K. Hadjikakou, G.D Geromichalos, D. Sahpazidou, L. Male, M.B. Hursthouse, B. Bednarz, M. Kubicki, K. Charalabopoulos and (EN)

Crystals of Ph3SnCl (1) were grown from a methanol/acetonitrile solution. Compounds [Ph3SnOH]n (2) and [(Ph2Sn)4Cl2O2(OH)2] (3) were crystallized from diethyl ether/methanol/acetonitrile and hot acetone/water solutions respectively, of the white precipitation, formed by adding KOH to solutions of 1 and [Ph2SnCl2] in 1 : 1 and 1 : 2 molar ratios respectively. Complex 1 was characterized by X-ray crystallography. X-ray structure determination of compounds 2 and 3 confirmed the previously reported identities. The molecular structure of 1, reported here, is a new polymorphic form of the known one for Ph3SnCl. Four independent [Ph3SnCl] molecules constitute the crystal structure of 1. The moieties are packed in two pairs in a tail-to-tail arrangement. Complexes 1-3 were evaluated for their in vitro cytotoxic activity (cell viability) against human cancer cell lines: HeLa (human cervical), MCF-7 (breast, estrogen receptor (ER) positive), MDA-MB-231 (breast, ER negative), A549 (lung), Caki-1 (kidney carcinoma), 786-O (renal adenocarcinoma), K1 (thyroid carcinoma), and the normal human lung cell line MRC-5 (normal human fetal lung fibroblast cells) versus, the normal immortalized human mammary gland epithelial cell line MTSV17 with a sulforhodamine B (SRB) assay. The results show potent cytotoxic activity of the complexes against all cell lines used, which was superior to that of cisplatin (CDDP). Compounds 1-3 showed higher activity against breast cancer cells MCF-7 (ER positive) than against of MDA-MB-231 (ER negative). These findings prompted us to search for possible interaction of these complexes with other cellular elements of fundamental importance in cell proliferation. The influence of these complexes 1-3 upon the catalytic peroxidation of linoleic acid to hydroperoxylinoleic acid by the enzyme lipoxygenase (LOX), as well as their binding affinity towards calf thymus-DNA, were kinetically and theoretically studied. (EN)

Πανεπιστήμιο Ιωαννίνων (EL)
University of Ioannina (EN)

Australian Journal of Chemistry (EN)

English

2012


CSIRO (EN)



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