109248-39-7Relevant academic research and scientific papers
Synthesis and evaluation of novel carbamate-substituted flavanone derivatives as potent acetylcholinesterase inhibitors and anti-amnestic agents
Anand, Preet,Singh, Baldev
, p. 1648 - 1659 (2013)
This study was designed to synthesize and evaluate flavanone derivatives with phenylcarbamate moiety as potent acetylcholinesterase (AChE) inhibitors and anti-amnestic agents for management of AD. The synthesis of carbamate-substituted flavanone derivativ
Synthesis and evaluation of new pyrazoline derivatives as potential anticancer agents in HepG-2 cell line
Xu, Weijie,Pan, Ying,Wang, Hong,Li, Haiyan,Peng, Qing,Wei, Duncan,Chen, Cheng,Zheng, Jinhong
, (2017/03/24)
Cancer is a major public health concern worldwide. Adverse effects of cancer treatments still compromise patients' quality of life. To identify new potential anticancer agents, a series of novel pyrazoline derivatives were synthesized and evaluated for cytotoxic effects on HepG-2 (human liver hepatocellular carcinoma cell line) and primary hepatocytes. Compound structures were confirmed by 1H-NMR, mass spectrometry, and infrared imaging. An in vitro assay demonstrated that several compounds exerted cytotoxicity in the micromolar range. Benzo[b]thiophen-2-yl-[5-(4-hydroxy-3,5-dimethoxy-phenyl)-3-(2-hydroxy-phenyl)-4,5-dihydo-pyrazol-1-yl]-methanone (b17) was the most effective anticancer agent against HepG-2 cells owing to its notable inhibitory effect on HepG-2 with an IC50 value of 3.57 μM when compared with cisplatin (IC50 = 8.45 μM) and low cytotoxicity against primary hepatocytes. Cell cycle analysis and apoptosis/necrosis evaluation using this compound revealed that b17 notably arrested HepG-2 cells in the G2/M phase and induced HepG-2 cells apoptosis. Our findings indicate that compound b17 may be a promising anticancer drug candidate.
A new series of cytotoxic pyrazoline derivatives as potential anticancer agents that induce cell cycle arrest and apoptosis
Wang, Hong,Zheng, Jinhong,Xu, Weijie,Chen, Cheng,Wei, Duncan,Ni, Wenxiu,Pan, Ying
, (2017/10/13)
A new series of pyrazoline derivatives 1b–12b was designed, synthesized and evaluated for antiproliferative activity against three cancer cell lines (HepG-2, Hela and A549). Additionally, NIH/3T3 cell cytotoxicity were tested and the structure activity re
Pyrazoline derivatives and application thereof
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Paragraph 0020-0022, (2018/02/04)
The invention discloses pyrazoline derivatives. The structural formula of the pyrazoline derivatives is shown in the description, wherein R1 is hydrogen, halogeno, hydroxyl, nitro, alkyl or alkoxy; R2 is halogeno, hydroxyl, alkyl or alkoxy; R is hydrogen,
The synthesis and evaluation of novel hydroxyl substituted chalcone analogs with in vitro anti-free radicals pharmacological activity and in vivo anti-oxidation activity in a free radical-injury Alzheimer's model
Pan, Ying,Chen, Yicun,Li, Qingnan,Yu, Xiaoyu,Wang, Jinzhi,Zheng, Jinhong
, p. 1693 - 1703 (2013/04/24)
Alzheimer's disease (AD) pathogenesis involves an imbalance between free radical formation and destruction. In order to obtain a novel preclinical anti-AD drug candidate, we synthesized a series of novel hydroxyl chalcone analogs which possessed anti-free radical activity, and screened their effects on scavenging 2,2-diphenyl-1-picrylhydrazyl (DPPH) and OH free radicals in vitro. Compound C7, 4,2'-dihydroxy-3,5-dimethoxychalcone was found to have potent activity in these anti-free radical activity tests. Further research revealed that C7 could elevate glutathione peroxidase (GSH-PX) and super oxide dismutase (SOD) levels and lower malonaldehyde (MDA) level in vivo in the Alzheimer's model. The indication of C7's effect on AD needs further study.
