Camptothecin-7-yl-methanthiole: Semisynthesis and Biological Evaluation (pages 2134–2143)
Dr. Michael S. Christodoulou, Dr. Franco Zunino, Dr. Valentina Zuco, Dr. Stella Borrelli, Dr. Daniela Comi, Dr. Gabriele Fontana, Dr. Marisa Martinelli, Prof. Dr. James B. Lorens, Dr. Lasse Evensen, Prof. Dr. Maurizio Sironi, Dr. Stefano Pieraccini, Prof. Dr. Lisa Dalla Via, Prof. Dr. Ornella Maria Gia and Prof. Dr. Daniele Passarella
Article first published online: 19 OCT 2012 | DOI: 10.1002/cmdc.201200322
Substitution prevails! The introduction of a methylenthiol group at position 7 of camptothecin (CPT) was carried out in four steps, along with the corresponding disulfide prodrug. Antiproliferation assays, mechanism of action studies, and molecular modeling analysis indicate that these 7-modified CPT derivatives maintain the biological activity and drug–target interaction characteristics of the parent compound.