title: Parallel synthesis of O-phenoxyethyl and O-adamantyl N-acyl thiocarbamates endowed with antiproliferative activity.
abstract: In order to further explore the antiproliferative properties of O-phenoxyethyl and O-adamantyl acylthiocarbamates (ATCs), a series of 14 derivatives was prepared by a parallel adaptation of a highly convergent one-pot three-step procedure. Ten acylthiocarbamates were selected by the National Cancer Institute drug evaluation program and screened against a panel of 55 to 58 cell lines derived from nine different types of human cancers. In general, the tested compounds showed a widespread micromolar activity with some specificity against leukemia, renal UO-31, central nervous system (CNS) SNB-75, and non-small cell lung HOP-92 cancer cell lines. Bioinformatic COMPARE analyses were carried out to identify possible mechanism(s) of action for acylthiocarbamate antiproliferative activity.
authors.affiliation: Dipartimento di Scienze Farmaceutiche, Università di Genova, Genova, Italy. andrea.spallarossa@unige.it
authors.forename: Andrea
authors.initials: A
authors.lastname: Spallarossa
authors.forename: Sara
authors.initials: S
authors.lastname: Cesarini
authors.forename: Silvia
authors.initials: S
authors.lastname: Schenone
authors.forename: Angelo
authors.initials: A
authors.lastname: Ranise
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D045744:Cell Line, Tumor; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D009369:Neoplasms / Q000188:drug therapy; D013329:Structure-Activity Relationship; D013859:Thiocarbamates / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D000970:Antineoplastic Agents; D013859:Thiocarbamates