Selective inhibition of receptor tyrosine kinases by synthetic analogues of aeroplysinin

Article abstract of DOI:10.1002/anie.199715411

IC₅0 values in the low micromolar range for the inhibition of receptor tyrosine kinases, which are critically involved in the transduction of mitogenic signals and thus in the regulation of cell growth and proliferation, are characteristic of synthetic analogues of marine natural product aeroplysinin 1 such as 2. In addition, they show pronounced inhibitory activity in cultured cells in vivo.