ISSN:
0018-019X
Keywords:
Chemistry
;
Organic Chemistry
Source:
Wiley InterScience Backfile Collection 1832-2000
Topics:
Chemistry and Pharmacology
Notes:
The syntheses and biological activities of some nitrostyrene derivatives of adenosine 5′-glutarates, a novel class of selective, bi-substrate-type inhibitors of the EGF receptor protein tyrosine kinase with IC50 values around 1 μM. Only marginal inhibition of the tyrosine kinases v-able and c-src and of the serine/threonine kinase PKC was observed. Compounds 8, 9, 11, and 12 - lacking the adenosine moiety - were ten times less active than the most potent derivatives, whereas 17 - lacking the nitrostyryl part - showed no inhibitory activity at all. Most of the compounds showed potent antiproliferative activity against an EGF-dependent mouse keratinocyte cell line.
Additional Material:
1 Tab.
Type of Medium:
Electronic Resource
URL:
http://dx.doi.org/10.1002/hlca.19920750304
Permalink