期刊
DALTON TRANSACTIONS
卷 40, 期 37, 页码 9557-9565出版社
ROYAL SOC CHEMISTRY
DOI: 10.1039/c1dt10995b
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资金
- NIH-MBRS at University of Puerto Rico Mayaguez [S06 GM008103-37]
- National Cancer Institute [1SC1CA157250-01]
- PSM-Moffitt Cancer Center [U56 CA126379-05]
- NSF-MRI
- NATIONAL CANCER INSTITUTE [SC1CA157250, U56CA126379] Funding Source: NIH RePORTER
- NATIONAL INSTITUTE OF GENERAL MEDICAL SCIENCES [S06GM008103] Funding Source: NIH RePORTER
Three ferrocene complexes vectorized with estrogens and vitamin D-2 were synthesized and fully characterized by spectroscopic, electrochemical and computational methods. The synthesis of these esters was accomplished by reacting ferrocenoyl chloride with the corresponding ROH groups (R = ergocalciferol, estradiol, estrone). The cytotoxicity of these complexes in HT-29 colon cancer and MCF-7 breast cancer cell lines was investigated in vitro. Only ferrocenoyl 17 beta-hydroxy-estra-1,3,5(10)-trien-3-olate showed good cytotoxic activity in both cell lines, exceeding those of ferrocenium and ferrocene. In MCF-7, ferrocenoyl 17 beta-hydroxy-estra-1,3,5(10)-trien-3-olate exhibited remarkable IC50, in the low micromolar range. This may be attributed to the presence of the estradiol vector. Docking studies between alpha-estrogen receptor ligand binding site and ferrocenoyl 17 beta-hydroxy-estra-1,3,5(10)-trien-3-olate revealed some key hydrophobic interactions that might explain the cytotoxic activity of this ester.
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