Synthesis and biological profiling of parthenolide ether analogs

2019 ◽  
Vol 17 (45) ◽  
pp. 9703-9707 ◽  
Author(s):  
Robert R. A. Freund ◽  
Philipp Gobrecht ◽  
Pascal Moser ◽  
Dietmar Fischer ◽  
Hans-Dieter Arndt
Keyword(s):  
Cyclic Ether ◽  
Structure Activity Relationships ◽  
Structure Activity ◽  
Derivatives Of ◽  
Tubulin Carboxypeptidase

Cyclic ether derivatives of parthenolide were synthesized by using two cyclization strategies, relying on 2-(silyloxy) allylboration. Characterization for tubulin carboxypeptidase inhibition generated new insights into structure–activity relationships.

Structure−Activity Relationships of 17α-Derivatives of Estradiol as Inhibitors of Steroid Sulfatase

2000 ◽  
Vol 43 (23) ◽  
pp. 4465-4478 ◽  
Author(s):  
Roch P. Boivin ◽  
Van Luu-The ◽  
Roger Lachance ◽  
Fernand Labrie ◽  
Donald Poirier
Keyword(s):  
Steroid Sulfatase ◽  
Structure Activity Relationships ◽  
Structure Activity ◽  
Derivatives Of

ChemInform Abstract: Synthesis and Structure-Activity Relationships of 5-Substituted Tryptamine Derivatives of o-Tolylpiperazine as Agonists at 5-HT1D Receptors.

ChemInform ◽  
2010 ◽  
Vol 27 (21) ◽  
pp. no-no
Author(s):  
M. PEREZ ◽  
P. J. PAUWELS ◽  
C. PALMIER ◽  
G. W. JOHN ◽  
J. P. VALENTIN ◽  
...  
Keyword(s):  
Structure Activity Relationships ◽  
Structure Activity ◽  
Derivatives Of

Struktur-Wirkungsbeziehungen polyfunktioneller Diterpene des Tigliantyps, IV [1-3]. Derivate des Tiglians mit fehlendem oder geöffnetem Cyclopropanring und ihre irritierende und tumorpromovierende Wirkung / Structure-Activity Relationships of Polyfunctional Diterpenes of the Tigliane Type, IV [1-3]. Derivatives of Tigliane without or with Opened Cyclopropane Ring and their Irritant and Promoting Activity

1980 ◽  
Vol 35 (11) ◽  
pp. 1470-1475 ◽  
Author(s):  
Bernd Sorg ◽  
Michael Gschwendt ◽  
Heinz Walter Thielmann ◽  
Erich Hecker
Keyword(s):  
Cyclopropane Ring ◽  
Complete Removal ◽  
Total Loss ◽  
Structure Activity Relationships ◽  
Type Iv ◽  
Structure Activity ◽  
Biological Tests ◽  
Derivatives Of

Abstract The synthesis of the esters 6d-8d, 9 c and 10 c is described. These compounds are closely structurally related to the irritant and tumorpromoting 12-O-tetradecanoylphorbol-13-acetate (TPA, 2 a) and to phorbol-12,13-didecanoate (PDD, 2 c) except that they possess no cyclopropane ring. Biological tests show that opening or complete removal of the cyclopropane ring leads to nearly total loss of irritant or tumorpromoting (tested in the case of 9 c and 10 c) activity.

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