C–H activation enables a rapid structure–activity relationship study of arylcyclopropyl amines for potent and selective LSD1 inhibitors

2016 ◽  
Vol 14 (36) ◽  
pp. 8576-8585 ◽  
Author(s):  
Shin Miyamura ◽  
Misaho Araki ◽  
Yosuke Ota ◽  
Yukihiro Itoh ◽  
Shusuke Yasuda ◽  
...  
Keyword(s):  
Cross Coupling ◽  
Structure Activity Relationship ◽  
Activity Relationship ◽  
Structure Activity ◽  
Relationship Study ◽  
Coupling Sequence

Potent and selective LSD1 inhibitors were synthesized rapidly by a C–H borylation and cross-coupling sequence.

Cytostatic 6-Arylpurine Nucleosides III. Synthesis and Structure-Activity Relationship Study in Cytostatic Activity of 6-Aryl-, 6-Hetaryl- and 6-Benzylpurine Ribonucleosides

2001 ◽  
Vol 66 (3) ◽  
pp. 483-499 ◽  
Author(s):  
Michal Hocek ◽  
Antonín Holý ◽  
Ivan Votruba ◽  
Hana Dvořáková
Keyword(s):  
Cross Coupling ◽  
Structure Activity Relationship ◽  
Cytostatic Activity ◽  
Activity Relationship ◽  
Coupling Reactions ◽  
Arylboronic Acids ◽  
Cross Coupling Reactions ◽  
Structure Activity ◽  
Relationship Study

A series of fifteen 6-aryl-, 6-hetaryl- and 6-benzylpurine ribonucleosides has been prepared by Pd-catalyzed cross-coupling reactions of 6-chloro-9-(2,3,5-tri-O-acetyl-β-D-ribofuranosyl)- purine with arylboronic acids, hetarylzinc halides, hetarylstannanes or benzylzinc halides followed by deprotection. Structure-activity relationship study revealed that besides 6-(4-substituted phenyl)purine nucleosides, also some 6-hetaryl- and 6-benzylpurine ribonucleosides possess considerable cytostatic activity.

Strategic structure-activity relationship study on a follistatin-derived myostatin inhibitory peptide

2021 ◽  
pp. 128163
Author(s):  
Mariko Saitoh ◽  
Kentaro Takayama ◽  
Yoshimi Roppongi ◽  
Takahiro Shimada ◽  
Akihiro Taguchi ◽  
...  
Keyword(s):  
Structure Activity Relationship ◽  
Activity Relationship ◽  
Inhibitory Peptide ◽  
Structure Activity ◽  
Relationship Study

Structure-activity relationship study of vitamin D analogs with oxolane group in their side chain

2017 ◽  
Vol 134 ◽  
pp. 86-96 ◽  
Author(s):  
Anna Y. Belorusova ◽  
Andrea Martínez ◽  
Zoila Gándara ◽  
Generosa Gómez ◽  
Yagamare Fall ◽  
...  
Keyword(s):  
Vitamin D ◽  
Structure Activity Relationship ◽  
Activity Relationship ◽  
Side Chain ◽  
Vitamin D Analogs ◽  
Structure Activity ◽  
Relationship Study
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