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-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.
Samorì
Cristian
C
Laboratory of Chemistry Istituto I.S.O.F.-Consiglio Nazionale delle Ricerche (CNR) Via P. Gobetti, 101, 40129-Bologna, Italy.
Guerrini
Andrea
A
Varchi
Greta
G
Zunino
Franco
F
Beretta
Giovanni Luca
GL
Femoni
Cristina
C
Bombardelli
Ezio
E
Fontana
Gabriele
G
Battaglia
Arturo
A
D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D002166:Camptothecin / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D045744:Cell Line, Tumor; D018360:Crystallography, X-Ray; D004249:DNA Damage; D004264:DNA Topoisomerases, Type I / Q000737:chemistry; D006801:Humans; D008958:Models, Molecular; D013871:Thiones / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology
C529807:16a-thiocamptothecin; D000970:Antineoplastic Agents; D013871:Thiones; D004264:DNA Topoisomerases, Type I; D002166:Camptothecin