Syntheses, antiproliferative activity and theoretical characterization of acitretin-type retinoids with changes in the lipophilic part

…, NK Karamanos, D Kletsas, D Papaioannou…

Index: Magoulas, George E.; Bariamis, Stavros E.; Athanassopoulos, Constantinos M.; Haskopoulos, Anastasios; Dedes, Petros G.; Krokidis, Marios G.; Karamanos, Nikos K.; Kletsas, Dimitris; Papaioannou, Dionissios; Maroulis, George European Journal of Medicinal Chemistry, 2011 , vol. 46, # 2 p. 721 - 737

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Citation Number: 18

Abstract

Acitretin analogs, incorporating changes in the lipophilic part, were efficiently synthesized from commercially available aromatic aldehydes or methyl ketones using the Wittig or Horner–Wadsworth–Emmons reaction. Their antiproliferative activity was evaluated against human breast MCF-7 epithelial cells. Analogs 3, 4, 8 and 11 exhibited strong, dose- dependent, antiproliferative activity on the tested cell line. Analog 3, incorporating three ...