title: Arylthioindoles, potent inhibitors of tubulin polymerization.
abstract: Several arylthioindoles had excellent activity as inhibitors both of tubulin polymerization and of the growth of MCF-7 human breast carcinoma cells. Methyl 3-[(3,4,5-trimethoxyphenyl)thio]-5-methoxy-1H-indole-2-carboxylate (21), the most potent derivative, showed IC(50) = 2.0 microM, 1.6 times more active than colchicine and about as active as combretastatin A-4 (CSA4). Compound 21 inhibited the growth of the MCF-7 cells at IC(50) = 13 nM. Colchicine and CSA4 had 13 nM and 17 nM IC(50) values, respectively, with these cells.
authors.affiliation: Dipartimento di Studi Farmaceutici, Università di Roma, La Sapienza, I-00185 Rome, Italy.
authors.forename: Gabriella
authors.initials: G
authors.lastname: De Martino
authors.forename: Giuseppe
authors.initials: G
authors.lastname: La Regina
authors.forename: Antonio
authors.initials: A
authors.lastname: Coluccia
authors.forename: Michael C
authors.initials: MC
authors.lastname: Edler
authors.forename: Maria Chiara
authors.initials: MC
authors.lastname: Barbera
authors.forename: Andrea
authors.initials: A
authors.lastname: Brancale
authors.forename: Elizabeth
authors.initials: E
authors.lastname: Wilcox
authors.forename: Ernest
authors.initials: E
authors.lastname: Hamel
authors.forename: Marino
authors.initials: M
authors.lastname: Artico
authors.forename: Romano
authors.initials: R
authors.lastname: Silvestri
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D001704:Biopolymers; D045744:Cell Line, Tumor; D018360:Crystallography, X-Ray; D003864:Depression, Chemical; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D007211:Indoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D008958:Models, Molecular; D013440:Sulfides / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D014404:Tubulin / Q000737:chemistry*; D050257:Tubulin Modulators
chemical_list: D000970:Antineoplastic Agents; D001704:Biopolymers; D007211:Indoles; D013440:Sulfides; D014404:Tubulin; D050257:Tubulin Modulators