63698-06-6Relevant articles and documents
Synthesis, X-ray characterization, DFT calculations and Hirshfeld surface analysis of thiosemicarbazone complexes of Mn+ ions (n = 2, 3; M = Ni, Cd, Mn, Co and Cu)
Mahmoudi, Ghodrat,Casti?eiras, Alfonso,Garczarek, Piotr,Bauzá, Antonio,Rheingold, Arnold L.,Kinzhybalo, Vasyl,Frontera, Antonio
, p. 1009 - 1023 (2016)
Two new pyridine-based heterocyclic thiosemicarbazone ligands and their Ni(ii), Cd(ii), Mn(ii), Co(iii) and Cu(ii) complexes have been synthesized and characterized by structural, analytical and spectroscopic methods. The monodeprotonated anionic forms of the ligands coordinate in a tridentate fashion via two nitrogen and one sulphur donor atoms to yield seven complexes in which metal centres vary from four-coordinated square planar to six-coordinated distorted octahedral geometries. Single-crystal X-ray crystallography showed that the molecular complexes can aggregate into larger entities depending on the anion coordinated to the metal centre. We have analysed the interesting supramolecular assemblies observed in the solid state of some complexes by means of DFT calculations. These assemblies are formed by a combination of several noncovalent interactions, including chelate ring-π, π-π, and chalcogen bonding interactions, that have been characterized using Bader's Theory of "atoms-in-molecules".
Tin complex with 2-acetyl pyridine thiosemicarbazone as ligand and synthesis method thereof
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Paragraph 0045-0048, (2020/02/14)
The invention discloses a tin complex taking 2-acetyl pyridine thiosemicarbazone as a ligand and a synthesis method thereof. The synthesis method comprises the following steps of: dissolving thiosemicarbazone in methanol, adding 2-acetyl pyridine dropwise
Rhodium complexes taking 2-acetylpyridine thiosemicarbazone as ligand and synthesis method thereof
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Paragraph 0043-0046, (2020/12/30)
The invention discloses rhodium complexes taking 2-acetylpyridine thiosemicarbazone as a ligand and a synthesis method thereof. The three kinds of new rhodium complexes are obtained by coordination ofnitrogen heterocyclic ring-containing 2-acetylpyridine thiosemicarbazone and metal rhodium. According to the invention, in-vitro proliferation inhibition activity experiments are further carried outon the synthesized rhodium complexes, and results show that the synthesized rhodium complexes have generally better in-vitro activity than ligands thereof, show very good inhibition activity, have little toxic effect on human normal cells, and are suitable for preparation of high-efficiency and low-toxicity anti-tumor drugs.
Thiosemicarbazone-based lead optimization to discover high-efficiency and low-toxicity anti-gastric cancer agents
Bo-Wang,He, Zhang-Xu,Li, Yi-Han,Liu, Hong-Min,Ma, Li-Ying,Ma, Qin,Tao, Yuan-Yuan,Wang, Hao-Jie,Wu, Hui-Pan,Zhang, Xin-Hui,Zhao, Bing
, (2020/05/19)
In this paper, a series of thiosemicarbazone derivatives containing different aromatic heterocyclic groups were synthesized and the tridentate donor system of the lead compound was optimized. Most of the target compounds showed improved antiproliferative activity against MGC803 cells. SAR studies revealed that compound 5d displayed significant advantages in inhibition effect with an IC50 value of 0.031 μM, and better selectivity between cancer and normal cells than 3-AP and DpC (about 15- and 5-fold improved respectively). Besides, compound 5d showed selective antiproliferative activity in not only other cancer cells but also different gastric cancer cell lines. In-depth mechanism studies showed that compound 5d could induce mitochondria-related apoptosis which might be related to the elevation of intracellular ROS level, and cause cell cycle arrest at S phase. Moreover, 5d could evidently suppress the cell migration and invasion by blocking the EMT (epithelial–mesenchymal transition) process. Consequently, our studies provided a lead optimization strategy of thiosemicarbazone derivatives which would contribute to discover high-efficiency and low-toxicity agents for the treatment of gastric cancer.
