Thiocamptothecin

Cristian Samorì; Andrea Guerrini; Greta Varchi; Franco Zunino; Giovanni Luca Beretta; Cristina Femoni; Ezio Bombardelli; Gabriele Fontana; Arturo Battaglia

doi:10.1021/jm8001982

Thiocamptothecin

Cristian Samorì, Andrea Guerrini, Greta Varchi, Franco Zunino, Giovanni Luca Beretta, Cristina Femoni, Ezio Bombardelli, Gabriele Fontana, Arturo Battaglia

Research output: Contribution to journal › Article

16 Scopus citations

Abstract

The synthesis and the X-ray structure of 16a-thiocamptothecin (TCPT), the thiopyridone analog of camptothecin (CPT), are accomplished. The crystal contains two structurally identical, yet independent molecules. Both of them are connected to other molecules via two intermolecular hydrogen bonds. S-Methylation of TCPT leads to the cleavage of the C-ring. The cytotoxic activity of TCPT was evaluated against different human tumor cell lines using CPT as reference compound.

Original language	English (US)
Pages (from-to)	3040-3044
Number of pages	5
Journal	Journal of Medicinal Chemistry
Volume	51
Issue number	10
DOIs	https://doi.org/10.1021/jm8001982
State	Published - May 22 2008

ASJC Scopus subject areas

Molecular Medicine
Drug Discovery

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abstract = "The synthesis and the X-ray structure of 16a-thiocamptothecin (TCPT), the thiopyridone analog of camptothecin (CPT), are accomplished. The crystal contains two structurally identical, yet independent molecules. Both of them are connected to other molecules via two intermolecular hydrogen bonds. S-Methylation of TCPT leads to the cleavage of the C-ring. The cytotoxic activity of TCPT was evaluated against different human tumor cell lines using CPT as reference compound.",

author = "Cristian Samor{\`i} and Andrea Guerrini and Greta Varchi and Franco Zunino and Beretta, {Giovanni Luca} and Cristina Femoni and Ezio Bombardelli and Gabriele Fontana and Arturo Battaglia",

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T1 - Thiocamptothecin

AU - Samorì, Cristian

AU - Guerrini, Andrea

AU - Varchi, Greta

AU - Zunino, Franco

AU - Beretta, Giovanni Luca

AU - Femoni, Cristina

AU - Bombardelli, Ezio

AU - Fontana, Gabriele

AU - Battaglia, Arturo

PY - 2008/5/22

Y1 - 2008/5/22

N2 - The synthesis and the X-ray structure of 16a-thiocamptothecin (TCPT), the thiopyridone analog of camptothecin (CPT), are accomplished. The crystal contains two structurally identical, yet independent molecules. Both of them are connected to other molecules via two intermolecular hydrogen bonds. S-Methylation of TCPT leads to the cleavage of the C-ring. The cytotoxic activity of TCPT was evaluated against different human tumor cell lines using CPT as reference compound.

AB - The synthesis and the X-ray structure of 16a-thiocamptothecin (TCPT), the thiopyridone analog of camptothecin (CPT), are accomplished. The crystal contains two structurally identical, yet independent molecules. Both of them are connected to other molecules via two intermolecular hydrogen bonds. S-Methylation of TCPT leads to the cleavage of the C-ring. The cytotoxic activity of TCPT was evaluated against different human tumor cell lines using CPT as reference compound.

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JO - Journal of Medicinal Chemistry

JF - Journal of Medicinal Chemistry

SN - 0022-2623

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