Synthesis and biological evaluation of N 4 ‐hydrazone derivatives of 5,7‐dihydro‐6 H ‐pyrrolo[2,3‐ d ]pyrimidin‐6‐one as novel anticancer agents with antimetastatic adjunct efficacy

2021 ◽  
Author(s):  
Zhichang Zhao ◽  
Hongjun Wang ◽  
Nana Tian ◽  
Hong Yan ◽  
Juan Wang
2020 ◽  
Vol 30 ◽  
pp. 100556
Author(s):  
Yazala Jyothsna Pragathi ◽  
Deekala Veronica ◽  
Kowthalam Anitha ◽  
Mandava Venkata Basaveswara Rao ◽  
Rudraraju Ramesh Raju

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 ◽  
...  

MedChemComm ◽  
2015 ◽  
Vol 6 (2) ◽  
pp. 334-338 ◽  
Author(s):  
Peng Huang ◽  
Zhong Hu ◽  
Liqin He ◽  
Xiaoshan Wang ◽  
Yaxian Wu

A series of novel derivatives of gambogenic acid (GNA) were synthesized and evaluated for their in vitro antiproliferative activity against four kinds of tumor cell lines. These compounds displayed potent antiproliferative activity. In particular, compound 3f exhibited superior antiproliferative activity against these tumor cell lines than GNA.


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