Synthesis and cytotoxic activity of substituted Luotonin A derivatives

Sabrina Dallavalle; Lucio Merlini; Giovanni Luca Beretta; Stella Tinelli; Franco Zunino

doi:10.1016/j.bmcl.2004.09.039

Synthesis and cytotoxic activity of substituted Luotonin A derivatives

Sabrina Dallavalle, Lucio Merlini, Giovanni Luca Beretta, Stella Tinelli, Franco Zunino

Fondazione IRCCS Istituto Nazionale dei Tumori

Research output: Contribution to journal › Article › peer-review

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.

Original language	English
Pages (from-to)	5757-5761
Number of pages	5
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	14
Issue number	23
DOIs	https://doi.org/10.1016/j.bmcl.2004.09.039
Publication status	Published - Dec 6 2004

Keywords

Antitumor agents
Cytotoxic alkaloid
Topoisomerase I

ASJC Scopus subject areas

Biochemistry
Molecular Biology
Organic Chemistry
Drug Discovery
Pharmaceutical Science

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AU - Dallavalle, Sabrina

AU - Merlini, Lucio

AU - Beretta, Giovanni Luca

AU - Tinelli, Stella

AU - Zunino, Franco

PY - 2004/12/6

Y1 - 2004/12/6

N2 - 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.

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KW - Topoisomerase I

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