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

Synthesis and cytotoxic activity of substituted luotonin A derivatives / S. Dallavalle, L. Merlini, G.L. Beretta, S. Tinelli, F. Zunino. - In: BIOORGANIC & MEDICINAL CHEMISTRY LETTERS. - ISSN 0960-894X. - 14:23(2004 Dec 06), pp. 5757-5761. [10.1016/j.bmcl.2004.09.039]

Synthesis and cytotoxic activity of substituted luotonin A derivatives

S. Dallavalle
Primo
;
L. Merlini
Secondo
;
2004

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
Antitumor agents; Cytotoxic alkaloid; Topoisomerase I
Settore CHIM/06 - Chimica Organica
Settore CHIM/08 - Chimica Farmaceutica
6-dic-2004
Article (author)
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/2434/8667
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