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In a bid to come up with potential anticancer agents, a class of thiosemicarbazone ligands bearing substituted thiophene were synthesized followed by complexation with various Pd(II) and Pt(II) metal precursors. The ligands (E)-1-((thiophen-2-yl)methylene)thiosemicarbazide ( L1 ), (E)-1-((4-bromothiophen-2-yl)methylene)thiosemicarbazide ( L2 ), and (E)-1-((5-bromo thiophen-2-yl)methylene)thiosemicarbazide ( L3 ) were synthesized by condensation reactions and obtained in good yields. Complexation of  L1  and  L2  with Pd(cod)Cl 2  gave  C1  (C 6 H 7 Cl 2 N 3 PdS 2 ) and  C2  (C 6 H 6 BrCl 2 N 3 PdS 2 ), respectively. Complexation of  L1  with K 2 PtCl 4  gave  C3  (C 6 H 7 Cl 2 N 3 PtS 2 ), while  L3  with K 2 PtCl 2 [(PPh) 3 ] 2  gave  C4  (C 24 H 21 BrClN 3 PPtS 2 ). The structures and coordination for all compounds were established by FTIR,  1 H-NMR,  13 C-NMR, UV-Vis, elemental analysis, and single-crystal X-ray diffraction studies for ligand  L1 . Tuning of the spectral and anticancer activity of the compounds was investigated by changing the position of the bromide substituent, metal center, and the  σ  or  π -donor/acceptor strength of the groups surrounding the metal center. The compounds had low to moderate anticancer potency with their spectral and structural properties correlating with the corresponding anticancer activity profiles. DNA binding modes were studied by spectroscopy and were comparable to known DNA intercalators. Structure-activity profiles were evident especially between  C1  and  C2  differing by the presence of a Br in position 5 of thiophene ring, which caused a remarkable increase in IC 50  values, from 14.71 ± 0.016 ( C1 ) to 43.08 ± 0.001( C2 ) in Caco-2 cells, 1.973 ± 0.048 ( C1 ) to 59.56 ± 0.010 ( C2 ) in MCF-7 cells, 16.65 ± 0.051 ( C1 ) to 72.25 ± 0.003 ( C2 ) in HeLa cells, 14.64 ± 0.037 ( C1 ) to 94.34 ± 0.003 ( C2 ) in HepG2, and 14.05 ± 0.042 ( C1 ) to &gt;100( C2 ) in PC-3 cells.

journal of chemistry

Synthesis, Characterization, and DNA-Binding Kinetics of New Pd(II) and Pt(II) Thiosemicarbazone Complexes: Spectral, Structural, and Anticancer Evaluation