Zhang, Xin-Hui; Bo-Wang; Tao, Yuan-Yuan; Ma, Qin; Wang, Hao-Jie; He, Zhang-Xu; Wu, Hui-Pan; Li, Yi-Han; Zhao, Bing; Ma, Li-Ying; Liu, Hong-Min published the article 《Thiosemicarbazone-based lead optimization to discover high-efficiency and low-toxicity anti-gastric cancer agents》. Keywords: thiosemicarbazone diastereoselective preparation SAR anticancer human cytotoxicity; Gastric cancer; Lead optimization; Migration; Thiosemicarbazone.They researched the compound: 5-Chloropicolinaldehyde( cas:31181-89-2 ).Safety of 5-Chloropicolinaldehyde. Aromatic heterocyclic compounds can be divided into two categories: single heterocyclic and fused heterocyclic. In addition, there is a lot of other information about this compound (cas:31181-89-2) here.
A series of thiosemicarbazone derivatives I [R1 = H, 4-MeO, 2-Br, 3-Br, 4-Br; R2 = H, Me, 2-pyridyl, etc.; R3 = 2-furyl, 3-indolyl, 2-pyridyl, etc.; n = 0, 1, 2] containing different aromatic heterocyclic groups was synthesized and the tridentate donor system of the lead compound was optimized. Most of the target compounds I showed improved antiproliferative activity against MGC803 cells. SAR studies revealed that compound I [R1 = 4-MeO, R2 = Me, R3 = 2-pyridyl, n = 0] displayed significant advantages in inhibition effect with an IC50 value of 0.031μM, and better selectivity between cancer and normal cells than 3-AP and DpC (about 15- and 5-fold improved resp.). Besides, compound I [R1 = 4-MeO, R2 = Me, R3 = 2-pyridyl, n = 0] showed selective antiproliferative activity in not only other cancer cells but also different gastric cancer cell lines. In-depth mechanism studies showed that compound I [R1 = 4-MeO, R2 = Me, R3 = 2-pyridyl, n = 0] 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, compound I [R1 = 4-MeO, R2 = Me, R3 = 2-pyridyl, n = 0] could evidently suppressed the cell migration and invasion by blocking the EMT (epithelial-mesenchymal transition) process. Consequently, our studies provided a lead optimization strategy of thiosemicarbazone derivatives I which would contribute to discover high-efficiency and low-toxicity agents for the treatment of gastric cancer.
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Reference:
Phosphine ligand,
Chiral phosphine ligands in asymmetric synthesis. Molecular structure and absolute configuration of (1,5-cyclooctadiene)-(2S,3S)-2,3-bis(diphenylphosphino)butanerhodium(I) perchlorate tetrahydrofuran solvate