Design, Synthesis and Biological Evaluation of the Novel Antitumor Agent 2-benzyl-3, 4-dihydroisoquinolin-1(2H)-one and Its Derivatives

2013 ◽  
pp. 797-804
Author(s):  
Jian Lv ◽  
Lei Lv ◽  
Xiaomin Zhang ◽  
Yao Zhou ◽  
Kui Lu ◽  
...  
Keyword(s):  
Antitumor Agent ◽  
Biological Evaluation ◽  
The Novel ◽  
Design Synthesis ◽  
Synthesis And Biological Evaluation

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 Analogues of the Antitumor Agent, 2-{4-[(7-Chloro-2-quinoxalinyl)oxy]phenoxy}propionic Acid (XK469)

2001 ◽  
Vol 44 (11) ◽  
pp. 1758-1776 ◽  
Author(s):  
Stuart T. Hazeldine ◽  
Lisa Polin ◽  
Juiwanna Kushner ◽  
Jennifer Paluch ◽  
Kathryn White ◽  
...  
Keyword(s):  
Propionic Acid ◽  
Antitumor Agent ◽  
Biological Evaluation ◽  
Design Synthesis ◽  
Synthesis And Biological Evaluation

scholarly journals Design, Synthesis and Biological Evaluation of Novel Thiazolidinone Derivatives

2021 ◽  
Vol 33 (10) ◽  
pp. 2379-2385
Author(s):  
Reshma Sathyanarayana ◽  
Boja Poojary ◽  
B. Sukesh Kumar ◽  
Vasantha Kumar ◽  
Rajesh P. Shastry ◽  
...  
Keyword(s):  
Antioxidant Activities ◽  
Radical Scavenging ◽  
Biological Evaluation ◽  
The Novel ◽  
Design Synthesis ◽  
Scavenging Effect ◽  
Elemental Analyses ◽  
Radical Scavenging Effect ◽  
Ft Ir ◽  
Synthesis And Biological Evaluation

In present study, the novel thiazolidinone derivatives were designed and synthesized. The formation of the target compounds was confirmed by the elemental analyses, FT-IR, mass spectroscopy and 1H NMR spectroscopy. These derivatives were subjected to antibacterial and antioxidant activities. The antibacterial results revealed that these derivatives were selectively active against Gram-negative Pseudomonas aeruginosa bacteria. Also, these derivatives displayed a good DPPH radical scavenging effect. Drosophila melanogaster flies were used for evaluating the toxic impact of novel thiazolidinone derivatives.

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