7271-45-6Relevant articles and documents
Novel panaxadiol triazole derivatives induce apoptosis in HepG-2 cells through the mitochondrial pathway
Xiao, Shengnan,Wang, Xude,Xu, Lei,Li, Tao,Cao, Jiaqing,Zhao, Yuqing
, (2020/07/23)
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.
Deamination of some N-amino nitrogen heterocycles using Preyssler's anion
Heravi, Majid M.,Sadjadi, Sodeh,Hekmatshoar, Rahim,Oskooie, Hossein A.,Bamoharram, Fatemeh F.
, p. 107 - 110 (2008/09/20)
Some N-aminotriazines and -triazoles were treated with Preyssler's anion as catalyst in acetic acid to afford the corresponding deaminated triazines and triazoles. The reaction is suggested to proceed via formation of N-nitrosamines with subsequent N-NO b
Condensation of 3-methyl/ethyl-5-mercapto-s-triazole with 3- acetylcoumarin and its derivatives
Vardhan, V. Aditya,Kumar, V. Ravi,Rao, V. Rajeswar
, p. 18 - 23 (2007/10/03)
3-Methyl/ethyl-5-mercapto-s-triazoles 2 on condensation with either 3- (2-bromoacetyl)coumarins or with substituted 3-acetyl comarins using bromine in the presence of trichloro-(N,N'-ethylene-bis-aminobenzamide) lanthanum and samarium as a catalyst, followed by cyclization of the intermediate 3-alkyl- 5-coumarinacyl-thio-s-triazole 3 using PPA furnish 3-alkyl-5- coumarinylthiazolo[3,2-b]-s-triazoles 4 and not the isomeric 3-alkyl-5- coumarinylthiazolo[2.3-c]-s-triazoles 6. 2-Acetyl- or 2-propanoylhydrazino- 4-coumarinyl-thlazolo hydrobromides 5 obtained from the reaction of acetyl/propanoyl thiosemicarbazides 1 with either substituted 3-(2- bromoacetyl) coumarins or with bromine and substituted 3-acetylcoumarin using trichloro-(N,N'-ethylene-bis-aminobenzamide)lanthanum (III) and samarium (III) as a catalyst, on treatment with phosphoryl chloride undergo facile cyclization yielding 5-alkyl-5-coumarinylthiazolo[2.3-c]-s-triazole 6.