scholarly journals Novel Piperazinyl-Quinazoline-4-one Analogs: Design, Synthesis and Evaluation of In Vitro Biological Activity

2012 ◽  
Vol 1 (3) ◽  
pp. 688-696 ◽  
Author(s):  
K. N. MYANGAR ◽  
T. N. AKHAJA ◽  
D. R. NAIK ◽  
J. P. RAVAL
Keyword(s):  
Biological Activity ◽  
Design Synthesis

Design, synthesis and biological activities of pyrrole-3-carboxamide derivatives as EZH2 (enhancer of zeste homologue 2) inhibitors and anticancer agents

2020 ◽  
Vol 44 (6) ◽  
pp. 2247-2255
Author(s):  
Qifan Zhou ◽  
Lina Jia ◽  
Fangyu Du ◽  
Xiaoyu Dong ◽  
Wanyu Sun ◽  
...  
Keyword(s):  
Biological Activity ◽  
Anticancer Agents ◽  
Biological Activities ◽  
Activity Assay ◽  
Design Synthesis ◽  
Structure Activity Relationships ◽  
Structure Activity ◽  
Enhancer Of Zeste

A novel series of pyrrole-3-carboxamides targeting EZH2 have been designed and synthesized. The structure–activity relationships were summarized by combining with in vitro biological activity assay and docking results.

Design, Synthesis, and Biological Activity of Peptides which Release Growth Hormone in Vitro*

Endocrinology ◽  
1981 ◽  
Vol 108 (1) ◽  
pp. 31-39 ◽  
Author(s):  
F. A. MOMANY ◽  
C. Y. BOWERS ◽  
G. A. REYNOLDS ◽  
D. CHANG ◽  
A. HONG ◽  
...  
Keyword(s):  
Growth Hormone ◽  
Biological Activity ◽  
Design Synthesis

Design, synthesis, and in vitro biological activity of benzimidazole based factor Xa inhibitors

2000 ◽  
Vol 10 (9) ◽  
pp. 963-966 ◽  
Author(s):  
Zuchun (Spring) Zhao ◽  
Damian O Arnaiz ◽  
Brian Griedel ◽  
Steven Sakata ◽  
Jerry L Dallas ◽  
...  
Keyword(s):  
Biological Activity ◽  
Factor Xa ◽  
Factor Xa Inhibitors ◽  
Design Synthesis

Synthesis and 4D-QSAR Studies of Alanine Hydroxamic Acid Derivatives as Aminopeptidase N Inhibitors

2019 ◽  
Vol 16 ◽  
Author(s):  
Min Gao ◽  
Qiao Li Lv ◽  
Hou Pan Zhang ◽  
Guo Gang Tu
Keyword(s):  
Biological Activity ◽  
Active Site ◽  
Hydroxamic Acid ◽  
Binding Mode ◽  
Qsar Model ◽  
Aminopeptidase N ◽  
Design Synthesis ◽  
Qsar Studies ◽  
Hydroxamic Acid Derivatives

Background: As a target for anticancer treatment, aminopeptidase N (APN) shows its overexpression on diverse malignant tumor cells and associates with cancer invasion, angiogenesis and metastasis. Objective: Design, synthesis and biological activity evaluation of alanine hydroxamic acid derivatives as APN inhibitors, and investigation the binding mode of inhibitors in the APN active site. Methods: Alanine hydroxamic acid derivatives were synthesized and evaluated for their in vitro anti-cancer activity using CCK-8 assay. Molecular docking and 4D-QSAR studies were carried out to suggest the mechanism of biological activity. Results: Compared with Bestatin, compound 9b showed the best APN inhibition activity. The putative binding mode of 9b in the APN active site was also discussed. Moreover, the robust and reliable 4D-QSAR model exhibited the following statistics: R2 = 0.9352, q2LOO = 0.8484, q2LNO =0.7920, R2Pred = 0.8739. Conclusion: Newly synthesized compounds exerted acceptable anticancer activity and further investigation on current scaffold would be beneficial.

Design, Synthesis and In vitro Biological Activity of SGLT2 Inhibitors Based on the Molecule Structure of Puerarin

2018 ◽  
Vol 38 (8) ◽  
pp. 1963
Author(s):  
Yongheng Shi ◽  
Liming Bai ◽  
Li Ma ◽  
Yuyang Chen ◽  
Jiping Liu ◽  
...  
Keyword(s):  
Biological Activity ◽  
Sglt2 Inhibitors ◽  
Design Synthesis ◽  
Molecule Structure
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