94794-26-0Relevant articles and documents
Platinum(II) and palladium(II) aryl-thiosemicarbazone complexes: Synthesis, characterization, molecular modeling, cytotoxicity, and antimicrobial activity
Tavares,Paschoal,Motta,Carpanez,Lopes,Fontes,Dos Santos,Silva,Grazul,Fontes
, p. 956 - 968 (2014)
Platinum(II) and palladium(II) complexes [ML2] have been isolated from reaction of K2PtCl4 or K 2PdCl4 and ligands (L) derived from thiosemicarbazones. The complexes were characterized by elemental analysis, Raman, IR, and NMR spectroscopy. In addition, quantum mechanical calculations were used to predict their structures and spectroscopic properties. For the first time, theoretical calculations using 195Pt NMR data were used to support the suggested structures. The results indicate that the thionic sulfur and the azomethine nitrogen are bonded to the metal ion in a trans configuration. Antibacterial activities and cytotoxicities of the complexes to B16-F10 and CT26.WT cell lines were also investigated. Some of the complexes demonstrated superior cytotoxic activity compared to cisplatin. 2014
5-aryl-1-arylideneamino-1h-imidazole-2(3h)-thiones: Synthesis and in vitro anticancer evaluation
Abu Ali, Ola A.,Abu Almaaty, Ali H.,El-Sayed, El-Sherbiny H.,Fayad, Eman,Tantawy, Mohamed A. M.,Toson, Eslam E. M.,Zaki, Islam
, (2021/06/16)
A novel series of N-1 arylidene amino imidazole-2-thiones were synthesized, identified using IR,1H-NMR, and13C-NMR spectral data. Cytotoxic effect of the prepared compounds was carried out utilizing three cancer cell lines; MCF-7 breast cancer, HepG2 liver cancer, and HCT-116 colon cancer cell lines. Imidazole derivative 5 was the most potent of all against three cell lines. DNA flow cytometric analysis showed that, imidazoles 4d and 5 exhibit pre-G1 apoptosis and cell cycle arrest at G2/M phase. The results of the VEGFR-2 and B-Raf kinase inhibition assay revealed that compounds 4d and 5 displayed good inhibitory activity compared with reference drug erlotinib.
A Series of Benzylidenes Linked to Hydrazine-1-carbothioamide as Tyrosinase Inhibitors: Synthesis, Biological Evaluation and Structure?Activity Relationship
Hosseinpoor, Hona,Iraji, Aida,Edraki, Najmeh,Pirhadi, Somayeh,Attarroshan, Mahshid,Khoshneviszadeh, Mahsima,Khoshneviszadeh, Mehdi
, (2020/08/05)
Tyrosinase is a type 3 copper enzyme responsible for skin pigmentation disorders, skin cancer, and enzymatic browning of vegetables and fruits. In the present article, 12 small molecules of 2-benzylidenehydrazine-1-carbothioamide were designed, synthesized and evaluated for their anti-tyrosinase activities followed by molecular docking and pharmacophore-based screening. Among synthesized thiosemicarbazone derivatives, one compound, (2E)-2-[(4-nitrophenyl)methylidene]hydrazine-1-carbothioamide, is the strongest inhibitor of mushroom tyrosinase with IC50 of 0.05 μM which demonstrated a 128-fold increase in potency compared to the positive control. Kinetic studies also revealed mix type inhibition by this compound. Docking studies confirmed the complete fitting of the synthesized compounds into the tyrosinase active site. The results underline the potential of 2-benzylidenehydrazine-1-carbothioamides as potent pharmacophore to extend the tyrosinase inhibition in drug discovery.
