scholarly journals New pyrazolo‐[3,4‐ d ]‐pyrimidine derivative Src kinase inhibitors lead to cell cycle arrest and tumor growth reduction of human medulloblastoma cells

2010 ◽  
Vol 24 (8) ◽  
pp. 2881-2892 ◽  
Author(s):  
Alessandra Rossi ◽  
Silvia Schenone ◽  
Adriano Angelucci ◽  
Martina Cozzi ◽  
Valentina Caracciolo ◽  
...  
Oncogene ◽  
2006 ◽  
Vol 26 (13) ◽  
pp. 1829-1839 ◽  
Author(s):  
L Bagella ◽  
A Sun ◽  
T Tonini ◽  
G Abbadessa ◽  
G Cottone ◽  
...  

2007 ◽  
Vol 18 (9) ◽  
pp. 981-995 ◽  
Author(s):  
Daniel Nowak ◽  
Simone Boehrer ◽  
Simone Hochmuth ◽  
Bettina Trepohl ◽  
Wencke Hofmann ◽  
...  

2006 ◽  
Vol 177 (11) ◽  
pp. 8266-8272 ◽  
Author(s):  
Georg F. Weber ◽  
Florian C. Gaertner ◽  
Wolfgang Erl ◽  
Klaus-Peter Janssen ◽  
Birgit Blechert ◽  
...  

Cancers ◽  
2021 ◽  
Vol 13 (8) ◽  
pp. 1790
Author(s):  
Katarzyna Malarz ◽  
Jacek Mularski ◽  
Michał Kuczak ◽  
Anna Mrozek-Wilczkiewicz ◽  
Robert Musiol

Sulfonates, unlike their derivatives, sulphonamides, have rarely been investigated for their anticancer activity. Unlike the well-known sulphonamides, esters are mainly used as convenient intermediates in a synthesis. Here, we present the first in-depth investigation of quinazoline sulfonates. A small series of derivatives were synthesized and tested for their anticancer activity. Based on their structural similarity, these compounds resemble tyrosine kinase inhibitors and the p53 reactivator CP-31398. Their biological activity profile, however, was more related to sulphonamides because there was a strong cell cycle arrest in the G2/M phase. Further investigation revealed a multitargeted mechanism of the action that corresponded to the p53 protein status in the cell. Although the compounds expressed a high submicromolar activity against leukemia and colon cancers, pancreatic cancer and glioblastoma were also susceptible. Apoptosis and autophagy were confirmed as the cell death modes that corresponded with the inhibition of metabolic activity and the activation of the p53-dependent and p53-independent pathways. Namely, there was a strong activation of the p62 protein and GADD44. Other proteins such as cdc2 were also expressed at a higher level. Moreover, the classical caspase-dependent pathway in leukemia was observed at a lower concentration, which again confirmed a multitargeted mechanism. It can therefore be concluded that the sulfonates of quinazolines can be regarded as promising scaffolds for developing anticancer agents.


2011 ◽  
Vol 33 (2) ◽  
pp. 413-419 ◽  
Author(s):  
J. J. Johnson ◽  
S. M. Petiwala ◽  
D. N. Syed ◽  
J. T. Rasmussen ◽  
V. M. Adhami ◽  
...  

2006 ◽  
Vol 80 (2) ◽  
pp. 123-131 ◽  
Author(s):  
Peng Zhang ◽  
Hong Li ◽  
Mo-Li Wu ◽  
Xiao-Yan Chen ◽  
Qing-You Kong ◽  
...  

2008 ◽  
Vol 283 (17) ◽  
pp. 11565-11574 ◽  
Author(s):  
Chunmei Wang ◽  
Nan Li ◽  
Xingguang Liu ◽  
Yuanyuan Zheng ◽  
Xuetao Cao

2012 ◽  
Vol 108 (1) ◽  
pp. 59-67 ◽  
Author(s):  
Zhiqiang Xu ◽  
Neel Joshi ◽  
Ashima Agarwal ◽  
Sonika Dahiya ◽  
Patrice Bittner ◽  
...  

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