Abstract
Five novel compounds, methyl 5-(acetyloxy)-1-(6-bromo-2-pyridinyl)-1H-pyrazole-3-carboxylate (1), methyl 1-(6-bromo-2-pyridinyl)-5-hydroxy-1H-pyrazole-3-carboxylate (2), Trimethyl 1,1′,1′′-tris(6-bromo-2-pyridinyl)-5,5′′-dihydroxy-5′-oxo-1′,5′-dihydro-1H,1′′H-4,4′: 4′,4′′-terpyrazole-3,3′,3′′-tricarboxylate (H2L1, 3), [Cu2(L2)2]·CH3OH (4), H2L2A·CH3CN (5) were synthesized. Compounds 1–5 characterized by elemental analysis, IR, and X-ray single-crystal diffraction. And 1–3 were also characterized by 1H NMR, 13C NMR and ESI-MS. The H2L1, H2L2 were formed by in-situ reaction. H2L2 and H2L2A are mesomer compounds which have two chiral carbons. The antitumor activity of compounds 1–5 against BEL-7404, HepG2, NCI-H460, T-24, A549 tumor cell lines were screened by methylthiazolyl tetrozolium (MTT) assay. The compounds 1, 2 showed weakly growth inhibition on the HepG2 cell lines. The HepG2 and A549 cell lines showed higher sensitivity to compound 4, while the IC50 values are 10.66, 28.09 μM, respectively. It is worth noting that compounds 1–5 did not show cytotoxicity to human normal liver cell line HL-7702, suggesting its cytotoxic selectivity on these tumor cell lines.
Highlights
In the past two decades, metallodrugs have been widely applied in clinics to treat various diseases [1,2]
Compound prepared in was prepared in aa way way similar similar to to that that in in the the literature, literature, except except that that (6-chloro-pyridin-2-yl)-hydrazine
When we carried carried out the the reaction reaction for for 11ininmixed mixedsolvent solvent(acetonitrile:ethanol
Summary
In the past two decades, metallodrugs have been widely applied in clinics to treat various diseases [1,2]. The great successes achieved with platinum-based antitumour agents, such as cisplatin, carboplatin and oxaliplatin, have promoted the development of metal-based anticancer drugs [3,4,5,6,7]. All of the platinum-based drugs are associated with severe side effects and the evolution of drug resistance during therapy [8], which has further raised the researchers’. Interests to synthesize and study non-platinum transition-metal complexes with satisfactory anticancer activities, less toxicities and specific antitumor mechanisms different to platinum-based anticancer drugs [9,10,11,12,13,14]. Copper can alter the metabolism of cancer cells and cause a differential response between normal and tumor cells.
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