Synthesis and cytotoxic activity of substituted luotonin A derivatives

  • Bioorg Med Chem Lett. 2004 Dec 6;14(23):5757-61. doi: 10.1016/j.bmcl.2004.09.039.
Sabrina Dallavalle  1 ,  Lucio Merlini ,  Giovanni Luca Beretta ,  Stella Tinelli ,  Franco Zunino
Affiliations
  • 1. Dipartimento di Scienze Molecolari Agroalimentari, Sezione di Chimica, Università di Milano, Via Celoria 2, 20133 Milano, Italy. [email protected]
PMID: 15501036 DOI: 10.1016/j.bmcl.2004.09.039
Abstract

Luotonin A is a cytotoxic alkaloid that has been shown to inhibit Topoisomerase I via stabilization of the binary complex topoisomerase-DNA in the same fashion as camptothecin. The synthesis and the cytotoxic activity on the lung carcinoma cell line H460 of a series of derivatives of Luotonin A is reported. The compounds inhibit Topoisomerase I but show weak cytotoxic activity, thus confirming the peculiarity of ring E of camptothecin for antitumor activity.