- Mild and convenient one-pot synthesis of 2-amino-1,3,4-oxadiazoles promoted by trimethylsilyl isothiocyanate (TMSNCS)
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A mild, convenient, and efficient one-pot synthesis of amino-1,3,4- oxadiazoles is described. In situ preparation of various thiosemicarbazides by the reaction of different carboxylic acid hydrazides with trimethylsilyl isothiocyanate (TMSNCS), followed by cyclodesulfurization of thiosemicarbazides under basic conditions in the presence of I2/KI resulted in 2-amino-1,3,4-oxadiazoles in high yields (79-94%).
- Guda, Dinneswara Reddy,Cho, Hyeon Mo,Lee, Myong Euy
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- Novel panaxadiol triazole derivatives induce apoptosis in HepG-2 cells through the mitochondrial pathway
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In this study, we introduced 1, 2, 4-triazole groups into panaxadiol (PD) to obtain 18 panaxadiol triazole derivatives. Five cancer cells and one normal cell were evaluated for cytotoxicity by MTT assay. The results showed that most of the derivatives could inhibit cancer cell proliferation, and the anti-proliferative activity of compound A1 was the most significant. For HepG-2 cells, the IC50 value was 4.21 ± 0.54 μM, which was nearly 15 times higher than the activity of PD. Further studies showed that compound A1 could induce apoptosis in HepG-2 cells, and could enhance the expression of Cl-caspase-3, Cl-caspase-9 and Cl-PARP. Moreover, Western blot analysis showed that after treating HepG-2 cells with compound A1, the expression of p53 protein was increased and the ratio of Bax/Bcl-2 was gradually increased. The cytoplasmic Bax is then translocated to the mitochondria, causing the release of Cyt c protein. Therefore, the results indicate that compound A1 induces apoptosis through the mitochondrial pathway and can be used the potential to develop new anti-proliferative agents.
- Xiao, Shengnan,Wang, Xude,Xu, Lei,Li, Tao,Cao, Jiaqing,Zhao, Yuqing
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- Synthesis and evaluation of bioactivity of thiazolo[3,2-b]-[1,2,4]- triazoles and isomeric thiazolo[2,3-c]-[1,2,4]-triazoles
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Synthesis of 2-(o-nitrophenyl)-6-arylthiazolo[3,2-b]-[1,2,4]-triazoles 4 and its isomer 3-(o-nitrophenyl)-5-arylthiazolo[2,3-c]-[1,2,4]-triazoles 6 has been achieved starting from the appropriate 1-(o-nitrobenzoyl)-3- thiosemicarbazide 1. Compound 1 on co
- Kumar,Kumar,Makrandi
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p. 1223 - 1229
(2013/10/21)
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- Trimethylsilyl isothiocyanate (TMSNCS): An efficient reagent for the one-pot synthesis of mercapto-1,2,4-triazoles
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A mild, convenient, and efficient one-pot synthesis of mercapto-1,2,4- triazoles is described. Various hydrazides efficiently reacted with trimethylsilyl isothiocyanate (TMSNCS) under basic condition to give mercapto-1,2,4-triazoles in high yields.
- Guda, Dinneswara Reddy,Wang, Tengjiao,Cho, Hyeon Mo,Lee, Myong Euy
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supporting information
p. 5238 - 5242
(2012/11/07)
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