BIOMAT Database Logo BIOMAT Database Logo

Synthesis and bioactivities of novel pyrazole oxime derivatives containing a 1,2,3-thiadiazole moiety. 2016

Hong Dai, and Shushan Ge, and Gang Li, and Jia Chen, and Yujun Shi, and Linyu Ye, and Yong Ling
College of Chemistry and Chemical Engineering, Nantong University, Nantong 226019, People's Republic of China; School of Pharmacy, Nantong University, Nantong 226001, People's Republic of China.

A series of new pyrazole oxime compounds bearing a 1,2,3-thiadiazole ring were designed, synthesized, and evaluated for their insecticidal, acaricidal and antitumor activities. Bioassays demonstrated that some title compounds displayed satisfactory insecticidal and acaricidal properties. Especially, compounds 8d and 8h exhibited 90% insecticidal activities against Aphis craccivora at the concentration of 100μg/mL. Interestingly, some of the target compounds possessed significant antitumor activities against four human cancer cell lines in vitro. Among them, compounds 8e (IC50=7.19μM), 8l (IC50=6.56μM), 8m (IC50=8.12μM), and 8r (IC50=7.06μM) had better inhibitory activities against HCT-116 cells than the control 5-fluorouracil (IC50=29.50μM). Additionally, compounds 8j, 8m, and 8r showed wonderful inhibitory activities against SGC-7901 cells with the IC50 values of 11.46, 9.41, and 8.64μM, respectively, which were superior to that of the control 5-fluorouracil.

UI MeSH Term Description Entries
D010091 Oximes Compounds that contain the radical R2C Aldoximes,Hydroxyimino Compounds,Ketoxime,Ketoximes,Oxime,Compounds, Hydroxyimino
D011720 Pyrazoles Azoles of two nitrogens at the 1,2 positions, next to each other, in contrast with IMIDAZOLES in which they are at the 1,3 positions.
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D013830 Thiadiazoles Heterocyclic compounds composed of a five-membered heterocyclic ring which contains one sulfur and two nitrogen atoms. Thiadiazole
D045325 HCT116 Cells Human COLORECTAL CARCINOMA cell line. HCT 116 Cells,HCT-116 Cells,Cell, HCT 116,Cell, HCT-116,Cell, HCT116,Cells, HCT 116,Cells, HCT-116,Cells, HCT116,HCT 116 Cell,HCT-116 Cell,HCT116 Cell
D020128 Inhibitory Concentration 50 The concentration of a compound needed to reduce population growth of organisms, including eukaryotic cells, by 50% in vitro. Though often expressed to denote in vitro antibacterial activity, it is also used as a benchmark for cytotoxicity to eukaryotic cells in culture. IC50,Concentration 50, Inhibitory

Related Publications

Hong Dai, and Shushan Ge, and Gang Li, and Jia Chen, and Yujun Shi, and Linyu Ye, and Yong Ling
Synthesis and Bioactivities of Novel Pyrazole Oxime Derivatives Containing a 5-Trifluoromethylpyridyl Moiety.
February 2016, Molecules (Basel, Switzerland),
Hong Dai, and Shushan Ge, and Gang Li, and Jia Chen, and Yujun Shi, and Linyu Ye, and Yong Ling
Synthesis and bioactivities of novel thioether/sulfone derivatives containing 1,2,3-thiadiazole and 1,3,4-oxadiazole/thiadiazole moiety.
November 2013, Bioorganic & medicinal chemistry letters,
Hong Dai, and Shushan Ge, and Gang Li, and Jia Chen, and Yujun Shi, and Linyu Ye, and Yong Ling
Synthesis and Bioactivities of Novel Galactoside Derivatives Containing 1,3,4-Thiadiazole Moiety.
January 2022, Frontiers in chemistry,
Hong Dai, and Shushan Ge, and Gang Li, and Jia Chen, and Yujun Shi, and Linyu Ye, and Yong Ling
Design, Synthesis and Bioactivities of Novel Isoxazole-Containing Pyrazole Oxime Derivatives.
November 2017, Molecules (Basel, Switzerland),
Hong Dai, and Shushan Ge, and Gang Li, and Jia Chen, and Yujun Shi, and Linyu Ye, and Yong Ling
Design, Synthesis and Bioactivities of Novel Dichloro-Allyloxy-Phenol-Containing Pyrazole Oxime Derivatives.
December 2015, Molecules (Basel, Switzerland),
Hong Dai, and Shushan Ge, and Gang Li, and Jia Chen, and Yujun Shi, and Linyu Ye, and Yong Ling
Synthesis and antiviral activities of pyrazole derivatives containing an oxime moiety.
November 2008, Journal of agricultural and food chemistry,
Hong Dai, and Shushan Ge, and Gang Li, and Jia Chen, and Yujun Shi, and Linyu Ye, and Yong Ling
Synthesis and biological activities of novel pyrazole oxime derivatives containing a 2-chloro-5-thiazolyl moiety.
November 2008, Journal of agricultural and food chemistry,
Hong Dai, and Shushan Ge, and Gang Li, and Jia Chen, and Yujun Shi, and Linyu Ye, and Yong Ling
Synthesis, structure, and biological activity of novel (oxdi/tri)azoles derivatives containing 1,2,3-thiadiazole or methyl moiety.
May 2012, Molecular diversity,
Hong Dai, and Shushan Ge, and Gang Li, and Jia Chen, and Yujun Shi, and Linyu Ye, and Yong Ling
Synthesis of Some New 1,3,4-Thiadiazole, Thiazole and Pyridine Derivatives Containing 1,2,3-Triazole Moiety.
February 2017, Molecules (Basel, Switzerland),
Hong Dai, and Shushan Ge, and Gang Li, and Jia Chen, and Yujun Shi, and Linyu Ye, and Yong Ling
Design, Synthesis, and Biological Activities of Novel Pyrazole Oxime Compounds Containing a Substituted Pyridyl Moiety.
May 2017, Molecules (Basel, Switzerland),
Copied contents to your clipboard!