Synthesis and biological evaluation of new camptothecin derivatives obtained by modification of position 20.

Abstract

The preparation and biological evaluation of a novel series of dimeric camptothecin derivatives are described. All the new compounds showed a significant ability to inhibit human tumor cell growth with IC(50) values ranging from 0.03 to 12.2 μM. The interference with the activity of the nuclear enzymes topoisomerases has been demonstrated, highlighting the poison effect of one of the obtained byproducts toward topoisomerase I. A moderate antiangiogenic activity has been demonstrated for one of the obtained compounds. Moreover, the effects of four new compounds on caspases activity and ROS generation have been studied on transgenic mouse cell.

DOI: 10.1016/j.bmc.2010.09.069

Cite this paper

@article{Riva2010SynthesisAB, title={Synthesis and biological evaluation of new camptothecin derivatives obtained by modification of position 20.}, author={Elena Riva and Daniela Comi and Stella Borrelli and Francesco Colombo and Bruno Danieli and J{\"{u}rgen Borlak and Lasse Evensen and James B Lorens and Gabriele Fontana and Ornella Maria Gia and Lisa Dalla Via and Daniele Passarella}, journal={Bioorganic & medicinal chemistry}, year={2010}, volume={18 24}, pages={8660-8} }