title: An overview on the development of new potentially active camptothecin analogs against cancer.
abstract: Camptothecin (CPT) and its derivatives comprise an important group of heterocyclic compounds that are well recognized for their anticancer activities. Efforts have been made over the years aiming to develop new CPT analogs with better clinical efficacy, improved pharmacokinetic profile and lower toxicity. First generation of analogs, irinotecan (CPT-11) and topotecan (TPT) was approved for use by FDA in 1996 for the treatment of colorectal (CPT-11) and cervical, ovarian and small lung cancers (TPT). Other analogs of CPT are currently in different phases of clinical trials. As CPT represents an important lead compound in the field of antitumor- research, in this review we will highlight some recent discoveries (2008-2013) on the development of novel camptothecin-based compounds as potential anticancer agents.
authors.forename: Eliza de Lucas
authors.initials: Ede L
authors.lastname: Chazin
authors.forename: Raisa da Rocha
authors.initials: Rda R
authors.lastname: Reis
authors.forename: Walcimar Trindade Vellasco
authors.initials: WT
authors.lastname: Junior
authors.forename: Lucas Fajardo Elmor
authors.initials: LF
authors.lastname: Moor
authors.affiliation: Universidade Federal Fluminense, Instituto de Quimica, Programa de Pos-Graduacao em Quimica, Outeiro de Sao Joao Batista, s/nº, Centro, Niteroi, 24020-141, Rio de Janeiro, Brazil. gqothatyana@vm.uff.br.
authors.forename: Thatyana Rocha Alves
authors.initials: TR
authors.lastname: Vasconcelos
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000737:chemistry* / Q000493:pharmacokinetics / Q000494:pharmacology / Q000627:therapeutic use*; D002166:Camptothecin / Q000031:analogs & derivatives* / Q000493:pharmacokinetics / Q000494:pharmacology / Q000627:therapeutic use*; D055808:Drug Discovery; D006801:Humans; D009369:Neoplasms / Q000188:drug therapy*; D059004:Topoisomerase I Inhibitors / Q000737:chemistry* / Q000493:pharmacokinetics / Q000494:pharmacology / Q000627:therapeutic use*
chemical_list: D000970:Antineoplastic Agents; D059004:Topoisomerase I Inhibitors; D002166:Camptothecin