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Synthesis, structure and biological activity of amide-functionalized titanocenyls: Improving their cytotoxic properties |
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| Authors: | Li Ming Gao Arnold L Rheingold |
| Institution: | a Department of Chemistry, University of Puerto Rico, Mayagüez, 00681, Puerto Rico b Department of Pharmacology, Toxicology and Physiology, Ponce School of Medicine, Ponce, 00732-7004, Puerto Rico c Department of Chemistry and Biochemistry, University of California, San Diego, La Jolla, CA 92093-0358, USA |
| Abstract: | Nine amide-functionalized titanocenyls have been synthesized and characterized by spectroscopic and analytical methods and the solid state structure of Cp(CpCO-NH-C6H4-OCF3)TiCl2 was determined by single crystal X-ray diffraction. X-ray analysis of Cp(CpCO-NH-C6H4-OCF3)TiCl2 showed that titanium is in a pseudo tetrahedral geometry and contains a Ti-O(amide) coordination. In principle, Ti-O coordination should provide more hydrolytic stability to the corresponding titanocenyls than titanocene dichloride. The cytotoxic activities of these amide-functionalized titanocenyls on HT-29 colon cancer cell line were determined by MTT assay to elucidate structure-activity relationship. All complexes were more cytotoxic than titanocene dichloride and there is no correlation between the para substituents on the phenyl ring and their cytotoxicities. |
| Keywords: | Titanocene dichloride Amide-functionalized titanocenyls HT-29 colon cancer cell Anticancer |
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