Abstract：
:Cell cycle experiments with our previously reported 4-biphenylaminoquinazoline (1-3) multityrosine kinase inhibitors revealed an activity profile resembling that of known tubulin polymerization inhibitors. Novel 4-biarylaminoquinazoline analogues of compound 2 were synthesized and evaluated as inhibitors of several tyrosine kinases and of tubulin. Although compounds 1-3 acted as dual inhibitors, the heterobiaryl analogues possessed only anti-tubulin properties and targeted the colchicine site. Furthermore, molecular modeling studies allowed the rationalization of the pharmacodynamic properties of the compounds.
journal_name
J Med Chemjournal_title
Journal of medicinal chemistryauthors
Marzaro G,Coluccia A,Ferrarese A,Brun P,Castagliuolo I,Conconi MT,La Regina G,Bai R,Silvestri R,Hamel E,Chilin Adoi
10.1021/jm500034jsubject
Has Abstractpub_date
2014-06-12 00:00:00pages
4598-4605issue
11eissn
0022-2623issn
1520-4804journal_volume
57pub_type
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