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Title: Phosphinegold(I) thiolates: Synthesis and biological activities
Keywords: Phosphinegold(I) thiolates, anti-cancer, biological activities, descriptors, gold complexes, gold
Issue Date: 3-Feb-2009
Citation: TADBUPPA PRIMJIRA (2009-02-03). Phosphinegold(I) thiolates: Synthesis and biological activities. ScholarBank@NUS Repository.
Abstract: The interest in phosphinegold(I) thiolates as an anti-cancer agent developed as aresult of the previous discovery of cytotoxicity of phosphinegold(I) thiolates. A series ofthiocarbamate ligands and its corresponding novel phosphinegold(I) thiolate weresuccessfully synthesized and characterized. The compoundsb structure was confirmed byelemental analysis and X-ray crystallography.Biological evaluation of the synthesised thiocarbamate ligands andPhosphinegold(I) thiolates were performed on a range of 7 human cancer cell lines andnormal human fiboblast for cytotoxicity study. A positive biological activity wasachieved for the Phosphinegold(I) thiolates at high concentration of 20 micromolar.Phosphinegold(I) thiolates were found to be more cytotoxic as compared to thethiocarbamate ligands at the same concentration, indicating the importance of thephosphine gold(I) function of the molecule. Descriptors such as logP, logD, polariability,PSA and the refractivity of the gold(I) complexes and its ligands were predicted using a computer software, Marvin. The descriptors were used to attempt the study of thestructure-activity relationship. Although the compoundsb cytotoxicity were observed onthe range of cancer cell lines but the structure activity relationship of the complexes wasnot established. There was little correlation between the activity and the descriptorsb value observed.
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