He, Zhangxu; Qiao, Hui; Yang, Feifei; Zhou, Wenjuan; Gong, Yunpeng; Zhang, Xinhui; Wang, Haojie; Zhao, Bing; Ma, Liying; Liu, Hong-min; Zhao, Wen published the article 《Novel thiosemicarbazone derivatives containing indole fragment as potent and selective anticancer agent》. Keywords: thiosemicarbazone diastereoselective preparation antitumor activity SAR cytotoxicity apoptosis; Apoptosis; Migration; Proliferation; Selectivity; Thiosemicarbazone.They researched the compound: 5-Chloropicolinaldehyde( cas:31181-89-2 ).HPLC of Formula: 31181-89-2. 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 novel thiosemicarbazone derivatives I [R1 = Ph, benzyl, phenylethyl,etc.; R2 = 2-pyridyl, 3-methyl-2-pyridyl, 4-methyl-2-pyridyl,etc.; R3 = H, Me] containing indole fragment were designed and synthesized. Most compounds exhibited excellent antiproliferative activity against PC3, MGC803 and EC109 cell lines with low micromolar IC50 (0.14-12μM). Especially, compound I [R1 = 2-(5-chloro-1H-indol-3-yl)ethyl; R2 = 5-methyl-2-pyridyl; R3 = H] can selectively inhibit PC3 cells in three tested tumor cells with IC50 value of 0.14 μM, which was attributed to a synergistic effect after introducing indole fragment into the TSC structure. Meanwhile, compound I [R1 = 2-(5-chloro-1H-indol-3-yl)ethyl; R2 = 5-methyl-2-pyridyl; R3 = H] displayed more selectivity in PC3 cells toward two normal WPMY-1 and GES-1 cell lines, compared to those of 3-AP and DPC. It was also found that I [R1 = 2-(5-chloro-1H-indol-3-yl)ethyl; R2 = 5-methyl-2-pyridyl; R3 = H] can effectively inhibit PC3 cell proliferation, colonization and induce apoptosis. Compound I [R1 = 2-(5-chloro-1H-indol-3-yl)ethyl; R2 = 5-methyl-2-pyridyl; R3 = H] may significantly suppress migration and invasion by blocking the EMT process but had no effect on cell cycle. Collectively, this findings indicated that I [R1 = 2-(5-chloro-1H-indol-3-yl)ethyl; R2 = 5-methyl-2-pyridyl; R3 = H] with structure of thiosemicarbazone containing indole may serve as a useful anticancer lead for further optimization and development.
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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