scholarly journals Resorcylic Acid Lactones with Cytotoxic and NF-κB Inhibitory Activities and Their Structure–Activity Relationships

2011 ◽  
Vol 74 (5) ◽  
pp. 1126-1131 ◽  
Author(s):  
Sloan Ayers ◽  
Tyler N. Graf ◽  
Audrey F. Adcock ◽  
David J. Kroll ◽  
Susan Matthew ◽  
...  
Keyword(s):  
Structure Activity Relationships ◽  
Structure Activity ◽  
Inhibitory Activities ◽  
Resorcylic Acid Lactones

scholarly journals Anti-inflammatory, antiallergic and COVID-19 protease inhibitory activities of phytochemicals from the Jordanian hawksbeard: identification, structure–activity relationships, molecular modeling and impact on its folk medicinal uses

RSC Advances ◽  
2020 ◽  
Vol 10 (62) ◽  
pp. 38128-38141
Author(s):  
Sherif S. Ebada ◽  
Nariman A. Al-Jawabri ◽  
Fadia S. Youssef ◽  
Dina H. El-Kashef ◽  
Tim-Oliver Knedel ◽  
...  
Keyword(s):  
Molecular Modeling ◽  
World Health Organization ◽  
World Health ◽  
Medicinal Uses ◽  
Structure Activity Relationships ◽  
Structure Activity ◽  
The World ◽  
Inhibitory Activities ◽  
Novel Coronavirus ◽  
Health Organization

On Wednesday 11th March, 2020, the world health organization (WHO) announced novel coronavirus (COVID-19, also called SARS-CoV-2) as a pandemic.

Inhibitory activities against topoisomerase I and II by isoaurostatin derivatives and their structure–activity relationships

2005 ◽  
Vol 15 (8) ◽  
pp. 2065-2068 ◽  
Author(s):  
Keitarou Suzuki ◽  
Tadashi Okawara ◽  
Tatuya Higashijima ◽  
Kazumi Yokomizo ◽  
Tohru Mizushima ◽  
...  
Keyword(s):  
Topoisomerase I ◽  
Structure Activity Relationships ◽  
Structure Activity ◽  
Inhibitory Activities

scholarly journals Structure-Activity Relationships of Aminocoumarin-Type Gyrase and Topoisomerase IV Inhibitors Obtained by Combinatorial Biosynthesis

2006 ◽  
Vol 50 (4) ◽  
pp. 1136-1142 ◽  
Author(s):  
Ruth H. Flatman ◽  
Alessandra Eustaquio ◽  
Shu-Ming Li ◽  
Lutz Heide ◽  
Anthony Maxwell
Keyword(s):  
Combinatorial Biosynthesis ◽  
Systematic Evaluation ◽  
Topoisomerase Iv ◽  
Structure Activity Relationships ◽  
Structure Activity ◽  
Series Of Experiments ◽  
Inhibitory Activities ◽  
Gyrase Inhibitors ◽  
Insight Into ◽  
Highly Evolved

ABSTRACT Novobiocin and clorobiocin are gyrase inhibitors produced by Streptomyces strains. Structurally, the two compounds differ only by substitution at two positions: CH3 versus Cl at position 8′ of the aminocoumarin ring and carbamoyl versus 5-methyl-pyrrol-2-carbonyl (MePC) at the 3"-OH of noviose. Using genetic engineering, we generated a series of analogs carrying H, CH3, or Cl at 8′ and H, carbamoyl, or MePC at 3"-OH. Comparison of the gyrase inhibitory activities of all nine structural permutations confirmed that acylation of 3"-OH is essential for activity, with MePC being more effective than carbamoyl. Substitution at 8′ further enhanced activity, but the effect of CH3 or Cl depended on the nature of the acyl group at 3": in the presence of carbamoyl at 3", CH3 resulted in higher activity; in the presence of MePC at 3", Cl resulted in higher activity. This suggests that the structures of both natural compounds are highly evolved for optimal interaction with gyrase. In a second series of experiments, clorobiocin derivatives with and without the methyl group at 4"-OH of noviose, and with different positions of the MePC group of noviose, were tested. Again clorobiocin was superior to all of its analogs. The activities of all compounds were also tested against topoisomerase IV (topo IV). Clorobiocin stood out as a remarkably effective topo IV inhibitor. The relative activities of the different compounds toward topo IV showed a pattern similar to that of the relative gyrase-inhibitory activities. This is the first report of a systematic evaluation of a series of aminocoumarins against both gyrase and topo IV. The results give further insight into the structure-activity relationships of aminocoumarin antibiotics.

Synthesis and structure–activity relationships of novel indirubin derivatives as potent anti-proliferative agents with CDK2 inhibitory activities

2006 ◽  
Vol 14 (1) ◽  
pp. 237-246 ◽  
Author(s):  
Myoung Ju Moon ◽  
Sang Kook Lee ◽  
Jong-Won Lee ◽  
Woo Keun Song ◽  
Si Wouk Kim ◽  
...  
Keyword(s):  
Structure Activity Relationships ◽  
Structure Activity ◽  
Inhibitory Activities
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