Issue 9, 2016

New generation of camptothecin derivatives spontaneously alkylating DNA

Abstract

9-Aminomethyl derivatives of 7-ethyl-10-hydroxycamptothecin were synthesized. Interaction with a natural DNA octamer was checked using 1H NMR, PFGSE NMR and MALDI-TOF experiments, which proved covalent binding. Compounds were tested against human cancer cell lines in vitro. All compounds show high activity comparable to SN38. The obtained products are well soluble in water.

Graphical abstract: New generation of camptothecin derivatives spontaneously alkylating DNA

Supplementary files

Article information

Article type
Paper
Submitted
18 Apr 2016
Accepted
25 Jul 2016
First published
26 Jul 2016

New J. Chem., 2016,40, 7978-7985

New generation of camptothecin derivatives spontaneously alkylating DNA

B. Naumczuk, K. Wiktorska, K. Lubelska, R. Kawęcki, W. Bocian, E. Bednarek, J. Sitkowski, Z. Chilmonczyk and L. Kozerski, New J. Chem., 2016, 40, 7978 DOI: 10.1039/C6NJ01217E

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