Samer Haidar, Ángel Amesty, Sandra Oramas-Royo, Claudia Götz, Ehab El-Awaad, Jana Kaiser, Sarah Bödecker, Amelie Arnold, Dagmar Aichele, Juan M Amaro-Luis, Ana Estévez-Braun, Joachim Jose
The human phosphatidylinositol 4-phosphate 5-kinase type I α (hPIP5K1α) plays a key role in the development of prostate cancer. In this work, seventeen derivatives of the natural diterpene totarol were prepared by copper(I)-catalysed Huisgen 1,3-dipolar cycloaddition reaction of the correspondingO-propargylated totarol with aryl or alkyl azides and screened for their inhibitory activities toward hPIP5K1α. Five compounds, 3a, 3e, 3f, 3i, and 3r, strongly inhibited the enzyme activity with IC50 values of 1...
April 23, 2024: Bioorganic & Medicinal Chemistry