Synthesis and cytotoxicity of 3,4-disubstituted-5-(3,4,5-trimethoxyphenyl)-4H-1,2,4-triazoles and novel 5,6-dihydro-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazole derivatives bearing 3,4,5-trimethoxyphenyl moiety

Bioorganic & Medicinal Chemistry Letters
2012.0

Abstract

A series of 3,4-disubstituted-5-(3,4,5-trimethoxyphenyl)-4H-1,2,4-triazoles and some novel 5,6-dihydro-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazoles bearing 3,4,5-trimethoxyphenyl moiety were synthesized and screened for their anticancer activity. The preliminary bioassay results indicated that compounds 14 and 16 showed much stronger cytotoxicity than Doxorubicin against HepG2 cell lines with IC(50) values of 0.58 and 3.17 μM, respectively. Meanwhile compound 16 also exhibited a broad spectrum of antitumor activity against MCF-7 and MKN45 with IC(50) values of 10.92 and 13.79 μM, respectively.

Knowledge Graph

Similar Paper

Synthesis and cytotoxicity of 3,4-disubstituted-5-(3,4,5-trimethoxyphenyl)-4H-1,2,4-triazoles and novel 5,6-dihydro-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazole derivatives bearing 3,4,5-trimethoxyphenyl moiety
Bioorganic & Medicinal Chemistry Letters 2012.0
Synthesis and cytotoxicity of novel 4-(4-(substituted)-1H-1,2,3-triazol-1-yl)-N-phenethylbenzenesulfonamides
Medicinal Chemistry Research 2014.0
Design, synthesis and biological evaluation of a novel series of 1,3,4-oxadiazole bearing N-methyl-4-(trifluoromethyl)phenyl pyrazole moiety as cytotoxic agents
European Journal of Medicinal Chemistry 2012.0
Synthesis, antitumor evaluation and molecular docking studies of [1,2,4]triazolo[4,3- b ][1,2,4,5]tetrazine derivatives
Bioorganic & Medicinal Chemistry Letters 2016.0
Synthesis, characterization, antioxidant, and anticancer studies of 6-[3-(4-chlorophenyl)-1H-pyrazol-4-yl]-3-[(2-naphthyloxy)methyl][1,2,4]triazolo[3,4-b][1,3,4]thiadiazole in HepG2 cell lines
Medicinal Chemistry Research 2011.0
Synthesis, in vitro anticancer and antimycobacterial evaluation of new 5-(2,5-dimethoxyphenyl)-1,3,4-thiadiazole-2-amino derivatives
Bioorganic & Medicinal Chemistry Letters 2015.0
Design, synthesis and biological evaluation of novel 1,2,4-triazolo [3,4-b][1,3,4] thiadiazines bearing furan and thiophene nucleus
European Journal of Medicinal Chemistry 2015.0
Synthesis, Antimitotic and Antivascular Activity of 1-(3′,4′,5′-Trimethoxybenzoyl)-3-arylamino-5-amino-1,2,4-triazoles
Journal of Medicinal Chemistry 2014.0
Design, synthesis and biological evaluation of novel 3-alkylsulfanyl-4-amino-1,2,4-triazole derivatives
Bioorganic & Medicinal Chemistry Letters 2016.0
Design and synthesis of novel 1,2,3-triazole-dithiocarbamate hybrids as potential anticancer agents
European Journal of Medicinal Chemistry 2013.0