title: Synthesis of a new bis(indolyl)methane that inhibits growth and induces apoptosis in human prostate cancer cells.
abstract: The synthesis and the antiproliferative activity against the human breast MCF-7, SkBr3 and the prostate LNCaP cancer cell lines of a series of bis(indolyl)methane derivatives are reported. The synthesis of new compounds was first accomplished by the reaction of different indoles with trimethoxyacetophenone in the presence of catalytic amounts of hydrochloric acid. A second procedure involving the use of oxalic acid dihydrate [(CO2H)2·2H2O] and N-cetyl-N,N,N-trimethylammonium bromide in water was carried out and led to better yields. Compound 5b significantly reduced LNCaP prostate cancer cell viability in a dose-dependent manner, with an IC50 of 0.64 ± 0.09 μM. To determine whether the growth inhibition was associated with the induction of apoptosis, treated cells were stained using DAPI. LNCaP cells treated with 1 μM of 5b showed the morphological changes characteristic of apoptosis after 24 h of incubation.
authors: a Department of Pharmacy, Health and Nutritional Sciences , University of Calabria , via Pietro Bucci, I-87036 , Rende (CS) , Italy.
authors: Mariangela
authors: M
authors: Marrelli
authors: Xavier
authors: X
authors: Cachet
authors: Filomena
authors: F
authors: Conforti
authors: Rosa
authors: R
authors: Sirianni
authors: Adele
authors: A
authors: Chimento
authors: Vincenzo
authors: V
authors: Pezzi
authors: Sylvie
authors: S
authors: Michel
authors: Giancarlo A
authors: GA
authors: Statti
authors: Francesco
authors: F
authors: Menichini
mesh_terms: D000972:Antineoplastic Agents, Phytogenic / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D017209:Apoptosis / Q000187:drug effects; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D006801:Humans; D007211:Indoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D008297:Male; D008697:Methane / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D011471:Prostatic Neoplasms
chemical_list: D000972:Antineoplastic Agents, Phytogenic; D007211:Indoles; D008697:Methane