Synthesis and Biological Evaluation of a Natural Ester Sintenin and Its Synthetic Analogues

2005 ◽  
Vol 68 (3) ◽  
pp. 342-348 ◽  
Author(s):  
Li Hong Hu ◽  
Hong Bin Zou ◽  
Jing Xu Gong ◽  
Hai Bo Li ◽  
Lei Xiang Yang ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
Synthetic Analogues ◽  
Synthesis And Biological Evaluation ◽  
Natural Ester

scholarly journals Synthesis and Biological Evaluation of Febrifugine Analogues

2014 ◽  
Vol 9 (12) ◽  
pp. 1934578X1400901
Author(s):  
Huong Doan Thi Mai ◽  
Giang Vo Thanh ◽  
Van Hieu Tran ◽  
Van Nam Vu ◽  
Van Loi Vu ◽  
...  
Keyword(s):  
Plasmodium Falciparum ◽  
Cell Lines ◽  
Cancer Cell ◽  
Antimalarial Activity ◽  
Biological Evaluation ◽  
Strong Inhibition ◽  
Synthetic Analogues ◽  
Synthetic Compounds ◽  
Activity Evaluation ◽  
Synthesis And Biological Evaluation

A series of febrifugine analogues were designed and synthesized. Antimalarial activity evaluation of the synthetic compounds indicated that these derivatives had a strong inhibition against both chloroquine-sensitive and -resistant Plasmodium falciparum parasites. Many of them were found to be more active than febrifugine hydrochloride. The tested analogues had also a significant cytotoxicity against four cancer cell lines (KB, MCF7, LU1 and HepG2). Among the synthetic analogues, two compounds 17b and 17h displayed a moderate cytotoxicity while they exhibited a remarkable antimalarial activity.

scholarly journals Marine Terpenoid Diacylguanidines: Structure, Synthesis, and Biological Evaluation of Naturally Occurring Actinofide and Synthetic Analogues

2017 ◽  
Vol 80 (5) ◽  
pp. 1339-1346 ◽  
Author(s):  
Marianna Carbone ◽  
M. Letizia Ciavatta ◽  
Véronique Mathieu ◽  
Aude Ingels ◽  
Robert Kiss ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
Synthetic Analogues ◽  
Naturally Occurring ◽  
Structure Synthesis ◽  
Synthesis And Biological Evaluation

Synthesis and Biological Evaluation of the Antimicrobial Natural Product Lipoxazolidinone A

2018 ◽  
Author(s):  
Jonathan J. Mills ◽  
Kaylib R. Robinson ◽  
Troy E. Zehnder ◽  
Joshua G. Pierce
Keyword(s):  
Natural Products ◽  
Natural Product ◽  
Mechanism Of Action ◽  
Marine Natural Products ◽  
Biological Evaluation ◽  
Lead Compounds ◽  
Follow Up Studies ◽  
Initial Resistance ◽  
Synthesis And Biological Evaluation

The lipoxazolidinone family of marine natural products, with an unusual 4-oxazolidinone heterocycle at their core, represents a new scaffold for antimicrobial discovery; however, questions regarding their mechanism of action and high lipophilicity have likely slowed follow-up studies. Herein, we report the first synthesis of lipoxazolidinone A, 15 structural analogs to explore its active pharmacophore, and initial resistance and mechanism of action studies. These results suggest that 4-oxazolidinones are valuable scaffolds for antimicrobial development and reveal simplified lead compounds for further optimization.

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