Abstract:
:A series of quinoline-containing c-Met inhibitors were prepared and studied. Chemistry was developed to introduce a pyridyl moiety onto the 2-aryl ring present in a lead molecule which mitigated the potential for quinone formation relative to the original compound. The study also assessed the importance of an acylthiourea moiety present in the lead structure for effective binding to the c-Met protein ATP site.
journal_name
Eur J Med Chemjournal_title
European journal of medicinal chemistryauthors
Kung PP,Funk L,Meng J,Alton G,Padrique E,Mroczkowski Bdoi
10.1016/j.ejmech.2007.08.011subject
Has Abstractpub_date
2008-06-01 00:00:00pages
1321-9issue
6eissn
0223-5234issn
1768-3254pii
S0223-5234(07)00333-9journal_volume
43pub_type
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abstract::A series of 1,2,4-triazole-3-carboxamides has been prepared from alkyl-1,2,4-triazole-3-carboxylates under mild conditions. The ability of these triazoles to displace [3H]-CP55940 from CB1 cannabinoid receptor was measured. However, they showed only poor to moderate binding affinities, indicating that substitution of ...
journal_title:European journal of medicinal chemistry
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journal_title:European journal of medicinal chemistry
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