Discovery of a potent and highly fluorescent sirtuin inhibitor

MedChemComm ◽  
2015 ◽  
Vol 6 (10) ◽  
pp. 1857-1863 ◽  
Author(s):  
Y. K. Yoon ◽  
M. A. Ali ◽  
A. C. Wei ◽  
T. S. Choon ◽  
A. N. Shirazi ◽  
...  

Highly fluorescent sirtuin inhibitor was discovered to possess growth inhibitory effect against multiple cancer cell lines.

2002 ◽  
Author(s):  
T. Mori ◽  
M. Ohnishi ◽  
M. Komiyama ◽  
A. Tsutsui ◽  
H. Yabushita ◽  
...  

2000 ◽  
Vol 28 (4) ◽  
pp. 227-233 ◽  
Author(s):  
Yosuke Kanishi ◽  
Yoichi Kobayashi ◽  
Seiko Noda ◽  
Bunpei Ishizuka ◽  
Kaoru Saito

2021 ◽  
Vol 22 (19) ◽  
pp. 10491
Author(s):  
Mohammed S. Abdel-Maksoud ◽  
Ahmed A. B. Mohamed ◽  
Rasha M. Hassan ◽  
Mohamed A. Abdelgawad ◽  
Garri Chilingaryan ◽  
...  

A new series of 4-(1H-benzo[d]imidazol-1-yl)pyrimidin-2-amine linked sulfonamide derivatives 12a–n was designed and synthesized according to the structure of well-established V600EBRAF inhibitors. The terminal sulfonamide moiety was linked to the pyrimidine ring via either ethylamine or propylamine bridge. The designed series was tested at fixed concentration (1 µM) against V600EBRAF, finding that 12e, 12i and 12l exhibited the strongest inhibitory activity among all target compounds and 12l had the lowest IC50 of 0.49 µM. They were further screened on NCI 60 cancer cell lines to reveal that 12e showed the most significant growth inhibition against multiple cancer cell lines. Therefore, cell cycle analysis of 12e was conducted to investigate the effect on cell cycle progression. Finally, virtual docking studies was performed to gain insights for the plausible binding modes of vemurafenib, 12i, 12e and 12l.


Sign in / Sign up

Export Citation Format

Share Document