Shengule, Sudhir; Loa-Kum-Cheung, Wendy; Parish, Christopher; Blairvacq, Melina; Meijer, Laurent; Nakao, Yoichi; Karuso, Peter
A one-pot synthesis of ageladine A and analogues is reported. The key Pictet-Spengler reaction between 2-aminohistamine and aryl aldehydes has been successfully utilized for the synthesis of the natural product and 14 analogues. These compounds were screened for their matrix metalloprotease (MMP) and kinase inhibition to develop the first structure-activity relationship of ageladine A analogues. One compound, which showed significant kinase activity but little MMP inhibitory activity, was found...[Show more]
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