Design and Synthesis of Novel Sulfonamide-Containing Bradykinin hB2Receptor Antagonists. 2. Synthesis and Structure−Activity Relationships of α,α-Cycloalkylglycine Sulfonamides

2007 ◽  
Vol 50 (3) ◽  
pp. 550-565 ◽  
Author(s):  
Daniela Fattori ◽  
Cristina Rossi ◽  
Christopher I. Fincham ◽  
Valerio Caciagli ◽  
Fernando Catrambone ◽  
...  
Keyword(s):  
Structure Activity Relationships ◽  
Design And Synthesis ◽  
Structure Activity

scholarly journals Structure–Activity Relationships Aided Design and Synthesis of xCT Antiporter Inhibitors

ChemMedChem ◽  
2021 ◽  
Author(s):  
Davide Cirillo ◽  
Shahin Sarowar ◽  
Per Øyvind Enger ◽  
Hans-René Bjørsvik
Keyword(s):  
Structure Activity Relationships ◽  
Design And Synthesis ◽  
Structure Activity ◽  
Aided Design

scholarly journals Design and synthesis of analogues of RA-VII—an antitumor bicyclic hexapeptide from Rubiae radix

2021 ◽  
Author(s):  
Yukio Hitotsuyanagi
Keyword(s):  
Efficient Method ◽  
Core Structure ◽  
Structure Activity Relationships ◽  
Design And Synthesis ◽  
The Core ◽  
Structure Activity ◽  
Tyrosine Derivatives ◽  
Natural Peptides

AbstractThe 14-membered cycloisodityrosine is the core structure of RA-series antitumor bicyclic peptides obtained from Rubia plants (Rubiaceae). In this study, an efficient method for the synthesis of cycloisodityrosines from commercially available l-tyrosine derivatives was developed. Using synthetic cycloisodityrosines and cycloisodityrosines with modified structures, several RA-VII analogues were designed and synthesized to explore structure–activity relationships of the cycloisodityrosine moiety of the RA-series peptides, and newly isolated natural peptides were synthesized to establish their structures. Graphic abstract

scholarly journals Rational Design and Synthesis of Selective PRMT4 Inhibitors: a New Chemotype for Development of Cancer Therapeutics

2020 ◽  
Author(s):  
Mathew Sutherland ◽  
Alice Li ◽  
Anissa Kaghad ◽  
Dimitrios Panagopoulos ◽  
Fengling Li ◽  
...  
Keyword(s):  
Rational Design ◽  
Histone H3 ◽  
Cancer Therapeutics ◽  
Histone Proteins ◽  
Methyl Transferase ◽  
Structure Activity Relationships ◽  
Design And Synthesis ◽  
New Class ◽  
Structure Activity ◽  
Arginine Residues

ABSTRACTProtein arginine N-methyl transferase 4 (PRMT4) asymmetrically dimethylates arginine residues of histone H3 and non-histone proteins. The overexpression of PRMT4 in several cancers has stimulated interest in the discovery of inhibitors as biological tools and potentially therapeutics. While several PRMT4 inhibitors have been reported, most display poor selectivity against other members of the PRMT family of methyl transferases. Here, we report the structure-based design of a new class of alanine containing 3-arylindoles as potent and selective PRMT4 inhibitors and describe key structure activity relationships for this class of compounds.

scholarly journals Exploiting structure–activity relationships of QS-21 in the design and synthesis of streamlined saponin vaccine adjuvants

2020 ◽  
Vol 56 (5) ◽  
pp. 719-722
Author(s):  
Mattia Ghirardello ◽  
Ane Ruiz-de-Angulo ◽  
Nagore Sacristan ◽  
Diego Barriales ◽  
Jesús Jiménez-Barbero ◽  
...  
Keyword(s):  
Molecular Level ◽  
Vaccine Adjuvants ◽  
Adjuvant Activity ◽  
Structure Activity Relationships ◽  
Design And Synthesis ◽  
Structure Activity

This work provides new streamlined saponin vaccine adjuvants and molecular-level insights into saponin conformation that correlate with potent adjuvant activity.

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