Synthesis of new cytotoxic E-ring modified camptothecins

Salvatore Cananzi; Sabrina Dallavalle; Alberto Bargiotti; Lucio Merlini; Roberto Artali; Giovanni Luca Beretta

doi:10.1016/j.tetlet.2010.09.130

Synthesis of new cytotoxic E-ring modified camptothecins

Salvatore Cananzi, Sabrina Dallavalle, Alberto Bargiotti, Lucio Merlini, Roberto Artali, Giovanni Luca Beretta

Fondazione IRCCS Istituto Nazionale dei Tumori

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

Abstract

In an effort to decrease the toxicity and improve the stability of the E-ring of camptothecin, new analogues with an 'inverted' lactone ring were designed and synthesized. The compounds retained a good cytotoxic activity on human non-small lung cancer cells H-460.

Original language	English
Pages (from-to)	6489-6492
Number of pages	4
Journal	Tetrahedron Letters
Volume	51
Issue number	50
DOIs	https://doi.org/10.1016/j.tetlet.2010.09.130
Publication status	Published - Dec 15 2010

Keywords

Antitumour activity
Camptothecin
Molecular docking
Synthesis
Topoisomerase 1

ASJC Scopus subject areas

Biochemistry
Organic Chemistry
Drug Discovery

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title = "Synthesis of new cytotoxic E-ring modified camptothecins",

abstract = "In an effort to decrease the toxicity and improve the stability of the E-ring of camptothecin, new analogues with an 'inverted' lactone ring were designed and synthesized. The compounds retained a good cytotoxic activity on human non-small lung cancer cells H-460.",

keywords = "Antitumour activity, Camptothecin, Molecular docking, Synthesis, Topoisomerase 1",

author = "Salvatore Cananzi and Sabrina Dallavalle and Alberto Bargiotti and Lucio Merlini and Roberto Artali and Beretta, {Giovanni Luca}",

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AU - Cananzi, Salvatore

AU - Dallavalle, Sabrina

AU - Bargiotti, Alberto

AU - Merlini, Lucio

AU - Artali, Roberto

AU - Beretta, Giovanni Luca

PY - 2010/12/15

Y1 - 2010/12/15

N2 - In an effort to decrease the toxicity and improve the stability of the E-ring of camptothecin, new analogues with an 'inverted' lactone ring were designed and synthesized. The compounds retained a good cytotoxic activity on human non-small lung cancer cells H-460.

AB - In an effort to decrease the toxicity and improve the stability of the E-ring of camptothecin, new analogues with an 'inverted' lactone ring were designed and synthesized. The compounds retained a good cytotoxic activity on human non-small lung cancer cells H-460.

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KW - Camptothecin

KW - Molecular docking

KW - Synthesis

KW - Topoisomerase 1

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