Thiocamptothecin

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-Me...

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Veröffentlicht in:	Journal of medicinal chemistry 2008-05, Vol.51 (10), p.3040-3044
Hauptverfasser:	Samorì, Cristian, Guerrini, Andrea, Varchi, Greta, Zunino, Franco, Beretta, Giovanni Luca, Femoni, Cristina, Bombardelli, Ezio, Fontana, Gabriele, Battaglia, Arturo
Format:	Artikel
Sprache:	eng
Schlagworte:	Antineoplastic agents Antineoplastic Agents - chemical synthesis Antineoplastic Agents - chemistry Antineoplastic Agents - pharmacology Biological and medical sciences Camptothecin - analogs & derivatives Camptothecin - chemical synthesis Camptothecin - chemistry Camptothecin - pharmacology Cell Line, Tumor Crystallography, X-Ray DNA Damage DNA Topoisomerases, Type I - chemistry General aspects Humans Medical sciences Models, Molecular Pharmacology. Drug treatments Thiones - chemical synthesis Thiones - chemistry Thiones - pharmacology
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Beschreibung
Zusammenfassung:	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.
ISSN:	0022-2623 1520-4804
DOI:	10.1021/jm8001982