Design, Synthesis and Primary Biological Evaluation of the Novel Antitumor Agent Indoline-3-One and Its Derivatives

2013 ◽  
pp. 875-882 ◽  
Author(s):  
Haiyong Jia ◽  
Guojun Pan ◽  
Yiqian Wang ◽  
Shaopeng Wen ◽  
Qiannan Guo ◽  
...  
Keyword(s):  
Antitumor Agent ◽  
Biological Evaluation ◽  
The Novel ◽  
Design Synthesis

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.

scholarly journals Novel 1-Amidino-4-Phenylpiperazines as Potent Agonists at Human TAAR1 Receptor: Rational Design, Synthesis, Biological Evaluation and Molecular Docking Studies

2020 ◽  
Vol 13 (11) ◽  
pp. 391 ◽  
Author(s):  
Valeria Francesconi ◽  
Elena Cichero ◽  
Evgeny V. Kanov ◽  
Erik Laurini ◽  
Sabrina Pricl ◽  
...  
Keyword(s):  
Rational Design ◽  
Pharmacophore Model ◽  
Docking Studies ◽  
Biological Evaluation ◽  
The Novel ◽  
Design Synthesis ◽  
Innovative Therapies ◽  
Spatial Geometry ◽  
Targeting Ability ◽  
20 Nm

Targeting trace amine-associated receptor 1 (TAAR1) receptor continues to offer an intriguing opportunity to develop innovative therapies in different pharmacological settings. Pursuing our endeavors in the search for effective and safe human TAAR1 (hTAAR1) ligands, we synthesized a new series of 1-amidino-4-phenylpiperazine derivatives (1–16) based on the application of a combined pharmacophore model/scaffold simplification strategy for an in-house series of biguanide-based TAAR1 agonists. Most of the novel compounds proved to be more effective than their prototypes, showing nanomolar EC50 values in functional activity at hTAAR1 and low general cytotoxicity (CC50 > 80 µM) when tested on the Vero-76 cell line. In this new series, the main determinant for TAAR1 agonism ability appears to result from the appropriate combination between the steric size and position of the substituents on the phenyl ring rather than from their different electronic nature, since both electron-withdrawing and electron donor groups are permitted. In particular, the ortho-substitution seems to impose a more appropriate spatial geometry to the molecule that entails an enhanced TAAR1 potency profile, as experienced, in the following order, by compounds 15 (2,3-diCl, EC50 = 20 nM), 2 (2-CH3, EC50 = 30 nM), 6 (2-OCH3, EC50 = 93 nM) and 3 (2-Cl, EC50 = 160 nM). Apart from the interest in them as valuable leads for the development of promising hTAAR1 agonists, these simple small molecules have further allowed us to identify the minimal structural requirements for producing an efficient hTAAR1 targeting ability.

Design, synthesis and primary biological evaluation of the novel 2-pyridone derivatives as potent non-nucleoside HBV inhibitors

2017 ◽  
Vol 136 ◽  
pp. 144-153 ◽  
Author(s):  
Haiyong Jia ◽  
Yang Song ◽  
Ji Yu ◽  
Peng Zhan ◽  
Diwakar Rai ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
The Novel ◽  
Design Synthesis

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
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