2. Academic Validation
  3. Diarylpentanoids with antitumor activity: A critical review of structure-activity relationship studies

Diarylpentanoids with antitumor activity: A critical review of structure-activity relationship studies

  • Eur J Med Chem. 2020 Apr 15:192:112177. doi: 10.1016/j.ejmech.2020.112177.
Joana Moreira 1,  Lucilia Saraiva 2,  Madalena M Pinto 1,  Honorina Cidade 3
Affiliations

Affiliations

  • 1 Laboratório de Química Orgânica e Farmacêutica, Departamento de Ciências Químicas, Faculdade de Farmácia, Universidade do Porto, Rua Jorge Viterbo Ferreira nº 228, 4050-313, Porto, Portugal; Centro Interdisciplinar de Investigação Marinha e Ambiental (CIIMAR), Universidade do Porto, Edifício do Terminal de Cruzeiros do Porto de Leixões, Av. General Norton de Matos s/n, 4050-208, Matosinhos, Portugal.
  • 2 LAQV/REQUIMTE, Laboratorio de Microbiologia, Departamento de Ciências Biológicas, Faculdade de Farmácia, Universidade do Porto, Rua Jorge Viterbo Ferreira, 228, 4050-313, Porto, Portugal.
  • 3 Laboratório de Química Orgânica e Farmacêutica, Departamento de Ciências Químicas, Faculdade de Farmácia, Universidade do Porto, Rua Jorge Viterbo Ferreira nº 228, 4050-313, Porto, Portugal; Centro Interdisciplinar de Investigação Marinha e Ambiental (CIIMAR), Universidade do Porto, Edifício do Terminal de Cruzeiros do Porto de Leixões, Av. General Norton de Matos s/n, 4050-208, Matosinhos, Portugal. Electronic address: hcidade@ff.up.pt.
PMID: 32172081 DOI: 10.1016/j.ejmech.2020.112177
Abstract

Diarypentanoids are commonly considered as monocarbonyl analogues of curcumin. Since the discovery of this compound in 1962, twenty one diarylpentanoids have been isolated and almost 600 synthetic analogues with antitumor activity have been synthesized. This review reports the exploitation of diarylpentanoids to develop curcumin analogues with improved antitumor activity over the last two decades. The mechanism of action and structure-activity relationship (SAR) studies are also highlighted. More importantly, structural features for the antitumor activity that may guide the design of new and more effective diarylpentanoids are also proposed.

Keywords

Antitumor activity; C5-curcuminoids; Chemotherapy; Curcumin; Diarylpentanoids; Structure-activity relationship.

Figures