Fluorescent analogs were synthesized of the potent PI 3-kinase inhibitors, wortmannin and demethoxyviridin. The esterification of 11-deacetylwortmannin, 17-hydroxywortmannin, and demethoxyviridin with the fluorescent carboxylic acids NBD-sarcosine and 7-dimethylaminocoumarin-4-acetic acid generated six novel fluorescent esters. Potent inhibition of PI 3-kinase-alpha was observed for the derivatives of 11-desacetylwortmannin and demethoxyviridin.
Download full-text PDF |
Source |
---|---|
http://dx.doi.org/10.1016/j.bmcl.2006.01.091 | DOI Listing |
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!