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

Access to Document

10.1016/j.bmcl.2004.09.039

Cite this

@article{883cf35e8e7d449bbac8409257a0a8dd,

title = "Synthesis and cytotoxic activity of substituted Luotonin A derivatives",

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.",

keywords = "Antitumor agents, Cytotoxic alkaloid, Topoisomerase I",

author = "Sabrina Dallavalle and Lucio Merlini and Beretta, {Giovanni Luca} and Stella Tinelli and Franco Zunino",

year = "2004",

month = dec,

day = "6",

doi = "10.1016/j.bmcl.2004.09.039",

language = "English",

volume = "14",

pages = "5757--5761",

journal = "Bioorganic and Medicinal Chemistry Letters",

issn = "0960-894X",

publisher = "Elsevier Limited",

number = "23",

}

TY - JOUR

T1 - Synthesis and cytotoxic activity of substituted Luotonin A derivatives

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.

AB - 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.

KW - Antitumor agents

KW - Cytotoxic alkaloid

KW - Topoisomerase I

UR - http://www.scopus.com/inward/record.url?scp=7044241040&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=7044241040&partnerID=8YFLogxK

U2 - 10.1016/j.bmcl.2004.09.039

DO - 10.1016/j.bmcl.2004.09.039

M3 - Article

C2 - 15501036

AN - SCOPUS:7044241040

VL - 14

SP - 5757

EP - 5761

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

SN - 0960-894X

IS - 23

ER -

Synthesis and cytotoxic activity of substituted Luotonin A derivatives

Abstract

Keywords

ASJC Scopus subject areas

Access to Document

Other files and links

Fingerprint

Cite this