Synthesis and biological evaluation of chalcone derivatives of 1,2,4-thiadiazol-benzo[d]imidazol-2-yl)quinolin-2(1H)-one as anticancer agents

2020 ◽  
Vol 30 ◽  
pp. 100556
Author(s):  
Yazala Jyothsna Pragathi ◽  
Deekala Veronica ◽  
Kowthalam Anitha ◽  
Mandava Venkata Basaveswara Rao ◽  
Rudraraju Ramesh Raju
MedChemComm ◽  
2010 ◽  
Vol 1 (5) ◽  
pp. 355 ◽  
Author(s):  
Ahmed Kamal ◽  
J. Surendranadha Reddy ◽  
M. Janaki Ramaiah ◽  
D. Dastagiri ◽  
E. Vijaya Bharathi ◽  
...  

2020 ◽  
Vol 13 (1) ◽  
pp. 1120-1129 ◽  
Author(s):  
Belma Zengin Kurt ◽  
Nur Ozten Kandas ◽  
Aydan Dag ◽  
Fatih Sonmez ◽  
Mustafa Kucukislamoglu

2019 ◽  
Vol 89 (7) ◽  
pp. 1491-1495 ◽  
Author(s):  
V. Ramesh ◽  
G. Purna Chander Rao ◽  
D. Ramachandran ◽  
A. Kalyan Chakravarthy

Molecules ◽  
2020 ◽  
Vol 25 (22) ◽  
pp. 5348
Author(s):  
Dima A. Sabbah ◽  
Shaima’ E. Hasan ◽  
Reema Abu Khalaf ◽  
Sanaa K. Bardaweel ◽  
Rima Hajjo ◽  
...  

The emergence of phosphatidylinositol 3-kinase (PI3Kα) in cancer development has accentuated its significance as a potential target for anticancer drug design. Twenty one derivatives of N-phenyl-4-hydroxy-6-methyl-2-quinolone-3-carboxamide were synthesized and characterized using NMR (1H and 13C) and HRMS. The derivatives displayed inhibitory activity against human epithelial colorectal adenocarcinoma (Caco-2) and human colon cancer (HCT-116) cell lines: compounds 8 (IC50 Caco-2 = 98 µM, IC50 HCT-116 = 337 µM) and 16 (IC50 Caco-2 = 13 µM, IC50 HCT-116 = 240.2 µM). Results showed that compound 16 significantly affected the gene encoding AKT, BAD, and PI3K. The induced-fit docking (IFD) studies against PI3Kα demonstrated that the scaffold accommodates the kinase domains and forms H-bonds with significant binding residues.


2012 ◽  
Vol 55 (11) ◽  
pp. 5077-5087 ◽  
Author(s):  
Katarzyna Sidoryk ◽  
Marta Świtalska ◽  
Joanna Wietrzyk ◽  
Anna Jaromin ◽  
Magdalena Piętka-Ottlik ◽  
...  

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