Design, Synthesis and Biological Evaluation of the Novel Antitumor Agent Aurone Derivatives

2013 ◽  
Vol 781-784 ◽  
pp. 1235-1239
Author(s):  
Qian Nan Guo ◽  
Lei Lv ◽  
Yao Zhou ◽  
Peng Yu ◽  
Yuou Teng
Keyword(s):  
Biological Activities ◽  
Antitumor Agent ◽  
Biological Evaluation ◽  
The Novel ◽  
Pharmacological Activities ◽  
Design Synthesis ◽  
H Nmr ◽  
Wide Range ◽  
Inhibitory Activities ◽  
Synthesis And Biological Evaluation

Aurones belong to a class of heterocyclic flavonoids which contains a benzofuran element associated with a benzylidene linked in position 2. Aurones possess a wide range of pharmacological activities and biological activities, such as antitumor, antifungal, phytoalexin and so on. A novel series of 2-ayl-yl (5-methacrylate) aurone analogues were synthesized in six steps with the overall yield of 11%-13% and characterized by 1H NMR. Among the key intermediates and target compounds, 2-(2-furan-ylmethylene)-5-methacrylate-benzofuran-3(2H)-one (7a) and 2-(2-thienyl-ylmethylene)-5-methacrylate-benzofuran-3(2H)-one (7b) have never been reported before. Primary biological activities evaluation showed that 7a exhibited good inhibitory activities against K562 with an IC50 of 2.18 μM and against HepG2 with an IC50 of 3.95μM.

Design, Synthesis and Biological Evaluation of of Novel Anticancer Agent tert-butyl 1-phenyl-3,4-dihydro-1H-pyrido[3,4-b]indole-2(9H)-carboxylate

2013 ◽  
Vol 781-784 ◽  
pp. 2211-2214
Author(s):  
Biao Shi ◽  
Yi Qian Wang ◽  
Yao Yang ◽  
Peng Yu ◽  
Kui Lu
Keyword(s):  
Biological Activities ◽  
Biological Properties ◽  
Biological Evaluation ◽  
Nmr Spectrum ◽  
Design Synthesis ◽  
H Nmr ◽  
Growth Inhibitory ◽  
Wide Range ◽  
New Compounds ◽  
Synthesis And Biological Evaluation

Indole and its derivatives extensively exist in nature, which showed a wide range of biological activities. Recently, there is a growing tendency to develop some new methods for the synthesis of novel indole derivatives and to study their biological properties. In this paper, we would like to report the design, synthesis and biological evaluation of a novel series of tricyclic indoles by employing Pictet-Spengler reaction as key step. All the target compounds were synthesized in four steps in 68-78% overall yield, which were characterized by 1H-NMR spectrum. All this new compounds were tested in an MTT assay on HepG2 and K562 and HT-29. Two of them showed tumor cell growth inhibitory good activity.

scholarly journals Synthesis of 3-Amino-4-Substituted Monocyclic ß-Lactams—Important Structural Motifs in Medicinal Chemistry

2021 ◽  
Vol 23 (1) ◽  
pp. 360
Author(s):  
Katarina Grabrijan ◽  
Nika Strašek ◽  
Stanislav Gobec
Keyword(s):  
Important Determinant ◽  
Biological Activities ◽  
Cholesterol Absorption ◽  
Pharmacological Activities ◽  
Cerium Ammonium Nitrate ◽  
Wide Range ◽  
Cerium Ammonium ◽  
Ring Nitrogen ◽  
Inhibitory Activities ◽  
Synthetic Approaches

Monocyclic ß-lactams (azetidin-2-ones) exhibit a wide range of biological activities, the most important of which are antibacterial, anticancer, and cholesterol absorption inhibitory activities. The synthesis of decorated monocyclic ß-lactams is challenging because their ring is highly constrained and consequently reactive, which is also an important determinant of their biological activity. We present the optimized synthesis of orthogonally protected 3-amino-4-substituted monocyclic ß-lactams. Among several possible synthetic approaches, Staudinger cycloaddition proved to be the most promising method for initial ring formation, yielding monocyclic ß-lactams with different substituents at the C-4 position, a phthalimido-protected 3-amino group, and a (dimethoxy)benzyl protected ring nitrogen. Challenging deprotection methods were then investigated. Oxidative cleavage with cerium ammonium nitrate and ammonia-free Birch reduction was found to be most effective for selective removal of ring nitrogen protection. Hydrazine hydrate was used for deprotection of the phthalimido group, and the procedure had to be modified by the addition of HCl in the case of aromatic substituents at the C-4 position. The presented methods and the synthesized 3-amino-4-substituted monocyclic ß-lactam derivatives are an important step toward new ß-lactams with potential pharmacological activities.

scholarly journals Design, synthesis, and biological evaluation of novel urolithins derivatives as potential phosphodiesterase II inhibitors

2021 ◽  
Vol 11 (1) ◽  
Author(s):  
Long Tang ◽  
Jianchun Jiang ◽  
Guoqiang Song ◽  
Yajing Wang ◽  
Ziheng Zhuang ◽  
...  
Keyword(s):  
Small Molecules ◽  
Inhibitory Activity ◽  
Structural Modification ◽  
Biological Evaluation ◽  
Design Synthesis ◽  
H Nmr ◽  
Lead Compounds ◽  
Activity Test ◽  
Synthesis And Biological Evaluation ◽  
C Nmr

AbstractA series of urolithins derivatives were designed and synthesized, and their structures have been confirmed by 1H NMR, 13C NMR, and HR-MS. The inhibitory activity of these derivatives on phosphodiesterase II (PDE2) was thoroughly studied with 3-hydroxy-8-methyl-6H-benzo[C]chromen-6-one and 3-hydroxy-7,8,9,10-tetrahydro-6H-benzo[C] chromen-6-one as the lead compounds. The biological activity test showed that compound 2e had the best inhibitory activity on PDE2 with an IC50 of 33.95 μM. This study provides a foundation for further structural modification and transformation of urolithins to obtain PDE2 inhibitor small molecules with better inhibitory activity.

scholarly journals Design Synthesis and Biological Evaluation of NovelN-Nitro Acid Amide Derivatives as Lead Compounds of Herbicide

2016 ◽  
Vol 2016 ◽  
pp. 1-6
Author(s):  
Xiaojuan Qi ◽  
Wenjie Tang ◽  
Shan Gao ◽  
Min Gao ◽  
Changshui Chen ◽  
...  
Keyword(s):  
Acid Amide ◽  
Biological Evaluation ◽  
Herbicidal Activity ◽  
Acetohydroxyacid Synthase ◽  
Design Synthesis ◽  
H Nmr ◽  
Lead Compounds ◽  
Amide Derivatives ◽  
Sorghum Sudanense ◽  
Synthesis And Biological Evaluation

A series ofN-nitro acid amide derivatives compounds were synthesized based on the active site of target acetohydroxyacid synthase (AHAS, EC: 2.2.1.6) enzyme. All the structures of newly prepared compounds were thoroughly characterized by satisfied IR and1H NMR spectra. The IC50values against AHAS enzyme and EC50values for herbicidal activity againstAmaranthus mangostanus L.andSorghum sudanenseof all synthesized target compounds were determined. The compoundsII-10,II-21, andII-22with IC50values of 7.09 mg/L, 9.07 mg/L, and 9.11 mg/L and the compoundsII-8andII-22with EC50values of 9.87 mg/L and 19.88 mg/L against root ofAmaranthus mangostanus L.andSorghum sudanensewere illustrated, respectively. Meanwhile, the possible reasons for the lower activity of compounds were analyzed by molecular docking prediction.

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