Monocarbonyl Analogs of Curcumin with Potential to Treat Colorectal Cancer

Abstract: Curcumin has a plethora of biological properties, making this compound potentially effective in the treatment of several diseases, including cancer. However, curcumin clinical use is compromised by its poor pharmacokinetics, being crucial to find novel analogs with better pharmacokinetic and pharmacological properties. Here, we aimed to evaluate the stability, bioavailability and pharmacokinetic profiles of monocarbonyl analogs of curcumin. A small library of monocarbonyl analogs of curcumin 1a–q was synthesized. Lipophilicity and stability in physiological conditions were both assessed by HPLC‐UV, while two different methods assessed the electrophilic character of each compound monitored by NMR and by UV‐spectroscopy. The potential therapeutic effect of the analogs 1a–q was evaluated in human colon carcinoma cells and toxicity in immortalized hepatocytes. Our results showed that the curcumin analog 1e is a promising agent against colorectal cancer, with improved stability and efficacy/safety profile.

Location
Deutsche Nationalbibliothek Frankfurt am Main
Extent
Online-Ressource
Language
Englisch

Bibliographic citation
Monocarbonyl Analogs of Curcumin with Potential to Treat Colorectal Cancer ; day:06 ; month:03 ; year:2023 ; extent:15
Chemistry & biodiversity ; (06.03.2023) (gesamt 15)

Creator
Clariano, Marta
Marques, Vanda
Vaz, João
Awam, Salma
Afonso, Marta B.
Jesus Perry, Maria
Rodrigues, Cecília MP

DOI
10.1002/cbdv.202300222
URN
urn:nbn:de:101:1-2023030614111279242820
Rights
Open Access; Der Zugriff auf das Objekt ist unbeschränkt möglich.
Last update
14.08.2025, 10:50 AM CEST

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Associated

  • Clariano, Marta
  • Marques, Vanda
  • Vaz, João
  • Awam, Salma
  • Afonso, Marta B.
  • Jesus Perry, Maria
  • Rodrigues, Cecília MP

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