2. Academic Validation
  3. Thiocamptothecin

Thiocamptothecin

  • J Med Chem. 2008 May 22;51(10):3040-4. doi: 10.1021/jm8001982.
Cristian Samorì 1,  Andrea Guerrini,  Greta Varchi,  Franco Zunino,  Giovanni Luca Beretta,  Cristina Femoni,  Ezio Bombardelli,  Gabriele Fontana,  Arturo Battaglia
Affiliations

Affiliation

  • 1 Laboratory of Chemistry Istituto I.S.O.F.-Consiglio Nazionale delle Ricerche (CNR) Via P. Gobetti, 101, 40129-Bologna, Italy.
PMID: 18419110 DOI: 10.1021/jm8001982
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.

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