- Synthesis, spectral and structural studies of zinc(II) complexes of salicylaldehyde N(4)-phenylthiosemicarbazone
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Five Zn(II) complexes of salicylaldehyde N(4)-phenylthiosemicarbazone (H2L) have been synthesized and physicochemically characterized. Out of the five Zn(II) complexes, one is binuclear {[(ZnL)2]·3C2H5OH (1)} an
- Seena,Kurup, M.R. Prathapachandra
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- Thiosemicarbazone-based selective proliferation inactivators inhibit gastric cancer cell growth, invasion, and migration
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A series of novel thiosemicarbazone derivatives were synthesized and evaluated for their antiproliferative activity against several selected tumor cell lines of different origins using the MTT assay. The preliminary results indicated that the MGC-803 cell line was remarkably sensitive to all the synthesized compounds. Among this series, compound 5n showed the best inhibitory activity with an IC50 value of 0.93 μM (about 10-fold more potent than 3-AP) against MGC-803. Further mechanism studies revealed that compound 5n could obviously inhibit the proliferation of MGC-803 cells by inducing apoptosis and arresting the cell cycle at the S phase. Compound 5n also showed marked inhibition of cell migration and invasion, without significant cytotoxicity against gastric epithelial immortalized GES-1 cells.
- Hu, Biao,Wang, Bo,Zhao, Bing,Guo, Qian,Li, Zhong-Hua,Zhang, Xin-Hui,Liu, Guang-Yao,Liu, Ying,Tang, Ying,Luo, Fan,Du, Ya,Chen, Ya-Xin,Ma, Li-Ying,Liu, Hong-Min
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- Thiosemicarbazone-based lead optimization to discover high-efficiency and low-toxicity anti-gastric cancer agents
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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.
- 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
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- Modifying aroylhydrazone prochelators for hydrolytic stability and improved cytoprotection against oxidative stress
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BSIH ((E)-N′-(2-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)benzylidene)isonicotinohydrazide) is a prodrug version of the metal chelator SIH ((E)-N′-(2-hydroxybenzylidene)isonicotinohydrazide) in which a boronate group prevents metal chelation until reac
- Wang, Qin,Franz, Katherine J.
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p. 5962 - 5972
(2018/11/23)
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- Novel thiosemicarbazone derivatives as potential antitumor agents: Synthesis, physicochemical and structural properties, DNA interactions and antiproliferative activity
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The paper describes synthesis of several novel thiosemicarbazone derivatives. Furthermore, crystal and molecular structure of 4-diethylamino-salicylaldehyde 4-phenylthiosemicarbazone revealed planarity of conjugated aromatic system, which suggested the po
- Dilovic, Ivica,Rubcic, Mirta,Vrdoljak, Visnja,Pavelic, Sandra Kraljevic,Kralj, Marijeta,Piantanida, Ivo,Cindric, Marina
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p. 5189 - 5198
(2008/12/20)
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- Oxovanadium(V) complexes of salicylaldehyde and 3-methoxysalicylaldehyde 4-phenylthiosemicarbazones. formation of two new thiazoline compounds
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In the reaction of tris(2,4-pentandionato)vanadium(III) with salicylaldehyde 4-phenylthiosemicarbazone (H2L1) and 3-methoxysalicylaldehyde 4-phenylthiosemicarbazone (H2L2), two new mononuclear complexes of vanad
- Cindric, Marina,Rubcic, Mirta,Dlovic, Ivica,Giester, Gerald,Kamenar, Boris
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experimental part
p. 583 - 590
(2009/09/25)
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