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Synthesis and Antitumor Properties of 2,5-Bis(3'-indolyl) thiophenes: Analogues of Marine Alkaloid Nortopsentin

Synthesis and Antitumor Properties of 2,5-Bis(3'-indolyl) thiophenes: Analogues of Marine Alkaloid Nortopsentin

Authors :
Ornella Gia
Alessandra Montalbano
Patrizia Diana
Gaetano Dattolo
Anna Carbone
Lisa Dalla Via
Paola Barraja
Girolamo Cirrincione
Annamaria Martorana
DIANA, P
CARBONE, A
BARRAJA, P
MONTALBANO, A
MARTORANA, A
DATTOLO, G
GIA, O
DALLA VIA, L
CIRRINCIONE, G
Publication Year :
2007
Publisher :
Elsevier Science Limited, 2007.

Abstract

A series of 11 bis-indolylthiophenes of formula I were obtained by cyclization of bis-indole 1,4-diketones using Lawesson''s reagent. Derivs. I (R = OMe, R1 = SO2Ph), I (R = OMe, R1 = Me), I (R = Cl, R1 = Me), and I (R = OMe, R1 = H) were selected to be evaluated in the full panel of about 60 human tumor cell lines derived from nine human cancer cell types and showed antiproliferative activity generally in the micromolar range. The most sensitive cell lines were: CCRF-CEM, MOLT-4, HL60 (TB), and RPMI-8226 of the leukemia subpanel, HT29 and HCC-2998 cell lines of the colon sub-panel, NCI-H522 of the non-small cell lung cancer sub-panel, LOX IMVI of the melanoma sub-panel, and UO-31 of the renal cancer sub-panel.

Details

Language :
English
Database :
OpenAIRE
Accession number :
edsair.doi.dedup.....99e05c553553077e26ac153c4406b441