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 IC50 values ranging from 0.03 to 12.2 mu M. 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.

Synthesis and biological evaluation of new camptothecin derivatives obtained by modification of position 20 / E. Riva, D. Comi, S. Borrelli, F. Colombo, B. Danieli, J. Borlak, L. Evensen, J.B. Lorens, G. Fontana, O.M. Gia, L. Dalla Via, D. Passarella. - In: BIOORGANIC & MEDICINAL CHEMISTRY. - ISSN 0968-0896. - 18:24(2010 Dec), pp. 8660-8668.

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

S. Borrelli;B. Danieli;D. Passarella
Ultimo
2010

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 IC50 values ranging from 0.03 to 12.2 mu M. 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.
Camptothecin derivative; Inhibition of angiogenesis; Topoisomerase inhibition
Settore CHIM/06 - Chimica Organica
dic-2010
Article (author)
File in questo prodotto:
Non ci sono file associati a questo prodotto.
Pubblicazioni consigliate

I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.

Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/2434/155187
Citazioni
  • ???jsp.display-item.citation.pmc??? 3
  • Scopus 26
  • ???jsp.display-item.citation.isi??? 26
social impact