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

Bioorg Med Chem. 2010 Dec 15;18(24):8660-8. doi: 10.1016/j.bmc.2010.09.069.

Elena Riva ¹, Daniela Comi, Stella Borrelli, Francesco Colombo, Bruno Danieli, Jurgen Borlak, Lasse Evensen, James B Lorens, Gabriele Fontana, Ornella Maria Gia, Lisa Dalla Via, Daniele Passarella

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Affiliation

1 Dipartimento di Chimica Organica e Industriale, Università degli Studi di Milano, Via Venezian 21, 20133 Milano, Italy.

PMID: 21071230 DOI: 10.1016/j.bmc.2010.09.069

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.

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