Understanding the structure–activity relationship between quercetin and naringenin: in vitro

RSC Advances ◽  
2015 ◽  
Vol 5 (128) ◽  
pp. 106171-106181 ◽  
Author(s):  
Bao Tu ◽  
Zhi-Juan Liu ◽  
Zhi-Feng Chen ◽  
Yu Ouyang ◽  
Yan-Jun Hu
Keyword(s):  
Molecular Level ◽  
Structure Activity Relationship ◽  
Activity Relationship ◽  
Structure Activity Relationships ◽  
Structure Activity

The interactions of quercetin and naringenin with DNA have been studied at molecular level, which may throw light on their structure–activity relationships, helpful for the design of analogs flavonoids and their application in drug industries.

scholarly journals From in vitro to in cellulo: structure–activity relationship of (2-nitrophenyl)methanol derivatives as inhibitors of PqsD in Pseudomonas aeruginosa

2014 ◽  
Vol 12 (32) ◽  
pp. 6094-6104 ◽  
Author(s):  
Michael P. Storz ◽  
Giuseppe Allegretta ◽  
Benjamin Kirsch ◽  
Martin Empting ◽  
Rolf W. Hartmann
Keyword(s):  
Pseudomonas Aeruginosa ◽  
Structure Activity Relationship ◽  
Activity Relationship ◽  
Structure Activity Relationships ◽  
Structure Activity ◽  
Relationship Of ◽  
Derivatives Of

More than 60 derivatives of (2-nitrophenyl)methanol were synthesized and evaluated regarding their potency to inhibit PqsD. In vitro and in cellulo structure–activity relationships were derived.

Interaction of flavones with DNA in vitro: structure–activity relationships

RSC Advances ◽  
2015 ◽  
Vol 5 (42) ◽  
pp. 33058-33066 ◽  
Author(s):  
Bao Tu ◽  
Zhi-Feng Chen ◽  
Zhi-Juan Liu ◽  
Li-Yang Cheng ◽  
Yan-Jun Hu
Keyword(s):  
Drug Discovery ◽  
Drug Design ◽  
Structure Activity Relationship ◽  
Activity Relationship ◽  
Structure Activity Relationships ◽  
Structure Activity ◽  
Relationship Of ◽  
Novel Drug

The structure–activity relationship of the different flavones has been investigated, which may meaningful for drug discovery, and novel drug design.

Recent Design and Structure-Activity Relationship Studies on Modifications of DHFR Inhibitors as Anticancer Agents

2019 ◽  
Vol 26 ◽  
Author(s):  
Agnieszka Wróbel ◽  
Danuta Drozdowska
Keyword(s):  
Anticancer Activity ◽  
Anticancer Drugs ◽  
Anticancer Agents ◽  
Physicochemical Characterization ◽  
Structure Activity Relationship ◽  
Activity Relationship ◽  
Biological Research ◽  
Structure Activity ◽  
Dhfr Inhibitors

Background: Dihydrofolate reductase (DHFR) has been known for decades as a molecular target for antibacterial, antifungal and anti-malarial treatments. This enzyme is becoming increasingly important in the design of new anticancer drugs, which is confirmed by numerous studies including modelling, synthesis and in vitro biological research. This review aims to present and discuss some remarkable recent advances on the research of new DHFR inhibitors with potential anticancer activity. Methods: The scientific literature of the last decade on the different types of DHFR inhibitors has been searched. The studies on design, synthesis and investigation structure-activity relationship were summarized and divided into several subsections depending on the leading molecule and its structural modification. Various methods of synthesis, potential anticancer activity and possible practical applications as DHFR inhibitors of new chemical compounds were described and discussed. <p> Results: This review presents the current state of knowledge on the modification of known DHFR inhibitors and the structures and searching for over eighty new molecules, designed as potential anticancer drugs. In addition, DHFR inhibitors acting on thymidylate synthase (TS), carbon anhydrase (CA) and even DNA-binding are presented in this paper. <p> Conclusion: Thorough physicochemical characterization and biological investigations it is possible to understand structure-activity relationship of DHFR inhibitors. This will enable even better design and synthesis of active compounds, which would have the expected mechanism of action and the desired activity.

Sign in / Sign up

Export Citation Format

Share Document