The relationship between chiroptical properties of differently substituted 5-dethia-5-oxacephams and their respective molecular structures was investigated. The amide chromophore of the beta-lactam unit in these compounds was found to be nonplanar with a shallow pyramidal configuration at the nitrogen atom. Due to the nonplanarity, the beta-lactam system becomes inherently dissymmetric, which is supported by a high magnitude of the n --> pi* CD band. It was also found that the helicity of the lactam moiety in investigated oxacephams is controlled by the absolute configuration at the C(6) carbon atom. On this basis, a helicity rule correlating a positive (negative) sign of the n right arrow pi Cotton effect with a negative (positive) O [double bond] C [bond] N [bond] C(6) torsional angle for policyclic beta-lactam derivatives possessing a nonplanar amide chromophore was formulated.
Mucin 1 (MUC1) is overexpressed in various cancer cells especially in breast cancer cells. There are known research works on the use of anti-MUC1 antibody with docetaxel in ovarian cancer, but there are no data about combined therapy platinum compounds with anti-MUC1 in breast cancer. The aim of the study was to evaluate the antiproliferative properties of a new dinuclear platinum(II) complex (Pt12) used with anti-MUC1 in human breast cancer cells. The dinuclear platinum(II) complex (Pt12) has been synthesized, and its cytotoxicity with anti-MUC1 has been tested in both MCF-7 and MDA-MB-231 breast cancer cells. In this study, the effects of Pt12 with anti-MUC1 on collagen and DNA biosynthesis in human breast cancer cells were compared to those evoked by cisplatin and cisplatin with anti-MUC1. The mechanism of action of Pt12 with anti-MUC1 was studied employing flow cytometry assessment of annexin V binding assay. It was found that Pt12 with anti-MUC1 was more active inhibitor of DNA and collagen synthesis as well more cytotoxic agent than Pt12 alone and cisplatin with anti-MUC1. Cytotoxicity of Pt12 with anti-MUC1 against breast cancer cells is due to apoptotic cell death as well as necrotic cell death. These results indicate that the use of Pt12 with anti-MUC1 may constitute a novel strategy in the chemotherapy of breast cancer tumors.
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