Luminescent cyclometalated platinum(II) complexes with amino acid ligands for protein binding.
Pt(C/N)(phe)(1, C/N = 2-(2'-thienyl)pyridine, phe = phenylalanine) shows a high binding affinity (ca. 10(6) dm(3) mol(-1)) and selectivity towards human serum albumin (HSA) and such binding is accompanied by an enhancement of photoluminescence at 562 nm; both the protein binding affinity and cytotoxicities of [Pt(C/N)(phe)(1), Pt(C/N)(trp)(2, trp = tryptophan) and Pt(C/N)(gly)(3, gly = glycine)] are affected by the amino acid ligand with having an IC(50) of up to 1 microM against a number of carcinoma cell lines.
Siu
Phyllis Kit-Man
PK
Department of Chemistry and Open Laboratory of Chemical Biology of the Institute of Molecular Technology for Drug Discovery and Synthesis, The University of Hong Kong, Pokfulam Road, Hong Kong.
Ma
Dik-Lung
DL
Che
Chi-Ming
CM
D000596:Amino Acids / Q000737:chemistry* / Q000378:metabolism*; D045744:Cell Line, Tumor; D003500:Cyclization; D004354:Drug Screening Assays, Antitumor; D006367:HeLa Cells; D006801:Humans; D020128:Inhibitory Concentration 50; D008024:Ligands; D049408:Luminescent Agents / Q000737:chemistry* / Q000378:metabolism; D008163:Luminescent Measurements; D015394:Molecular Structure; D009942:Organometallic Compounds / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology; D010984:Platinum / Q000737:chemistry* / Q000378:metabolism; D011485:Protein Binding; D012709:Serum Albumin / Q000737:chemistry* / Q000378:metabolism; D013329:Structure-Activity Relationship
D000596:Amino Acids; D008024:Ligands; D049408:Luminescent Agents; D009942:Organometallic Compounds; D012709:Serum Albumin; D010984:Platinum