Abstract
Despite the fact that a large number of chemotherapeutic anticancer agents have been discovered, cancer still remains a great cause of deaths worldwide. The purpose of our researches is to discover a new antitumor drug. In this aim, two new Cu(II) complexes, [Cu(L)2(py)2(H2O)2](C1) and [Cu(L)2(phen)](C2) with a new ligand, N-(5-trifluoromethyl-[1,3,4]-thiadiazole-2-yl)-benzensulfonamide(HL) were synthesized. The complexes were characterized by elemental analysis, spectral and magnetic determinations. The nuclease activity studies of the complexes confirm their capacity to cleavage the DNA molecule. Both complexes have in vitro antioxidant activity (DPPH, FRAP methods), in vitro (using xanthine /xanthine oxidase system) and in vivo (using S.cerevisiae)SOD mimetic activity.The results of MTT assay on two carcinoma cell lines (HeLa and WM35) indicate that both complexes have antitumor activity, but (C2) has a superior activity compared with (C1) and with Cisplatin. On normal fibroblast (HDFa), (C1) showed toxicity comparable with Cisplatin, but (C2) showed a lower one. Bacterial assays were also performed (by the disk diffusion method) and both complexes have antibacterial activity against S. aureus, E. coli, P. aeroginosa and B. cereus. All the biological studies are in concordance and show that both complexes have biologic activity but (C2)is much more active.
Highlights
New The complexes were characterized by elemental analysis, spectral and magnetic determinations
The results reveal that both complexes have similar antibacterial activity against S aureus, E. coli and P
The antibacterial activity may be due to the following mechanisms: inhibition of ribonucleoside diphosphate reductase enzyme which helps in DNA synthesis; by oxidative rupture, creation of lesions in DNA strand or by binding to the nitrogen base of DNA or RNA results in inhibit base replication [55]
Summary
2-amino-5-fluoromethyl-[1,3,4]–thiadiazole, sulfonyl chlorides, pyridine and phenatroline were provided by Aldrich and were used without further purification. IR spectra were recorded using KBr disks on a Perkin-Elmer FT-IR 1730 instrument, in the 4000-400 cm–1 range. Methanol which contained 2 mL of a 1 M NaOH solution Another mixture was prepared by dissolving p0h.5enmanmthorol linCeu(SpOh4en5)Hin2O25 and mL. Of 1,10By adding the ligand solution in the Cu(II)-phenanthroline mixture, the color turns to green. After stirring at 35ÚC for an hour, the reaction mixture was filtered in order to remove the precipitate (a complex of copper with phenanthroline). The filtrate was left to stand at room temperature and, after a few days, green crystalline powder was formed. To test for the presence of reactive oxygen species (ROS) generated during strand scission and for possible complex-DNA interaction sites, various reactive oxygen intermediate scavengers and groove binders were added to the reaction mixtures.
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