Related Experiment Video
Updated: Jan 12, 2026
Amide Coupling Reaction for the Synthesis of Bispyridine-based Ligands and Their Complexation to Platinum as Dinuclear Anticancer Agents
Published on: May 28, 2014
Platinum(II) complexes of fluorinated pyrrole carbothioamides: enhanced anticancer activity and overcoming cisplatin
Haiming Tang1,2, Chen Chen2, Yuhang Fu1
1College of Chemistry and Environmental Engineering, Sichuan University of Science and Engineering, Zigong 643000, People's Republic of China.
Abstract:
A series of fluorinated pyrrole-derived thioamide ligands was synthesized via a solvent-free reaction of (substituted) pyrrole with various aryl isothiocyanates. Subsequent reactions of these ligands with cis-[PtCl2(PPh3)2] afforded a set of charge-neutral platinum(II) complexes, featuring a variety of fluorine-containing substituents on the phenyl ring of the ligand. All compounds were characterized by NMR spectroscopy and electrospray ionization-mass spectrometry. Single-crystal X-ray diffraction analysis of a representative complex revealed that the ligand coordinated to the platinum center in a bidentate fashion through the deprotonated pyrrole nitrogen and the sulfur atom of the thioamide group, forming a five-membered chelate ring. The antiproliferative activity of selected ligands and their corresponding Pt(II) complexes was evaluated against HCT116, NCI-H460, A2780, and A2780cis human cancer cell lines, and significantly increased potency was found for a Pt complex as compared to its ligand.
Related Concept Videos
02:56Treatment Resistant Cancers
02:50Combination Therapies and Personalized Medicine
The combination of the drug acetazolamide and sulforaphane is a good example of combination therapy to treat cancer. The cells in the interior of a large tumor often die due to the hypoxic and...
02:52Stereoisomerism
Isomers are different chemical species that have the same chemical formula.
Transition metal complexes often exist as geometric isomers, in which the same atoms are connected through the same types of bonds but with differences in their orientation in space. Coordination complexes with two different ligands in the cis and trans positions from a ligand of interest form isomers. For example, the octahedral [Co(NH3)4Cl2]+ ion has two isomers (Figure 1) In the cis...
02:57Targeted Cancer Therapies
There are several types of targeted therapies against...