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Special Issue "The Versatility of the Curcumin Scaffold for the Design of Bioactive Compounds"

A special issue of Molecules (ISSN 1420-3049). This special issue belongs to the section "Medicinal Chemistry".

Deadline for manuscript submissions: 30 November 2020.

Special Issue Editor

Prof. Dr. Federica Belluti
Website
Guest Editor
Department of Pharmacy and Biotechnology, Alma Mater Studiorum—University of Bologna, Via Belmeloro 6, 40126 Bologna, Italy
Interests: : naturally inspired compounds; bioactive molecules; curcumin-based analogues; chalcones; coumarins; anti-Alzheimer agents; anti-protozoan compounds; anti-cancer agents

Special Issue Information

Dear Colleagues,

The polyphenol curcumin, found in Curcuma longa L., is one of the most thoroughly investigated natural products, as documented by the impressive number of studies claiming its efficacy for both the prevention and the treatment of a wide number of disorders. This peculiar pleiotropic profile, mainly due to the concomitant modulation of multiple and structurally unrelated targets, could offer promises for addressing complex maladies, such as cancer and Alzheimer’s disease. Curcumin’s α,β-unsaturated carbonyl system, through the modification of the crucial cysteine residues of proteins, is believed to be involved in the bioactivity of this molecule. In this context, this natural compound, regarded as privileged structure, has been largely exploited in medicinal chemistry and new bioactive molecules were discovered, able to either effectively inhibit a single molecular target or innovatively modulate different interconnected pathways.

This Special Issue aims to provide both updates and new perspectives on bioactive curcumin-based analogues. Original articles, short communications, as well as a limited number of reviews of studies on this topic are welcome.

Prof. Dr. Federica Belluti
Guest Editor

Manuscript Submission Information

Manuscripts should be submitted online at www.mdpi.com by registering and logging in to this website. Once you are registered, click here to go to the submission form. Manuscripts can be submitted until the deadline. All papers will be peer-reviewed. Accepted papers will be published continuously in the journal (as soon as accepted) and will be listed together on the special issue website. Research articles, review articles as well as short communications are invited. For planned papers, a title and short abstract (about 100 words) can be sent to the Editorial Office for announcement on this website.

Submitted manuscripts should not have been published previously, nor be under consideration for publication elsewhere (except conference proceedings papers). All manuscripts are thoroughly refereed through a single-blind peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. Molecules is an international peer-reviewed open access semimonthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 2000 CHF (Swiss Francs). Submitted papers should be well formatted and use good English. Authors may use MDPI's English editing service prior to publication or during author revisions.

Keywords

  • Alzheimer’s disease
  • Bioactive compounds
  • Cancer
  • Curcumin
  • Drug design
  • Drug synthesis
  • Medicinal chemistry
  • Naturally inspired molecules
  • Structure–activity relationship (SAR) study

Published Papers (2 papers)

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Research

Open AccessArticle
Design, Synthesis and Biological Evaluation of Novel Triazole N-acylhydrazone Hybrids for Alzheimer’s Disease
Molecules 2020, 25(14), 3165; https://doi.org/10.3390/molecules25143165 - 10 Jul 2020
Abstract
Alzheimer’s disease (AD) is a multifactorial neurodegenerative disorder that involves different pathogenic mechanisms. In this regard, the goal of this study was the design and synthesis of new compounds with multifunctional pharmacological activity by molecular hybridization of structural fragments of curcumin and resveratrol [...] Read more.
Alzheimer’s disease (AD) is a multifactorial neurodegenerative disorder that involves different pathogenic mechanisms. In this regard, the goal of this study was the design and synthesis of new compounds with multifunctional pharmacological activity by molecular hybridization of structural fragments of curcumin and resveratrol connected by an N-acyl-hydrazone function linked to a 1,4-disubstituted triazole system. Among these hybrid compounds, derivative 3e showed the ability to inhibit acetylcholinesterase activity, the intracellular formation of reactive oxygen species as well as the neurotoxicity elicited by Aβ42 oligomers in neuronal SH-SY5Y cells. In parallel, compound 3e showed a good profile of safety and ADME parameters. Taken together, these results suggest that 3e could be considered a lead compound for the further development of AD therapeutics. Full article
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Open AccessFeature PaperArticle
Curcumin-1,2,3-Triazole Conjugation for Targeting the Cancer Apoptosis Machinery
Molecules 2020, 25(13), 3066; https://doi.org/10.3390/molecules25133066 - 05 Jul 2020
Abstract
The burden of neoplastic diseases is widely recognized as a severe cause of mortality. The clinical inadequacy of most anticancer therapeutics urgently prompted intense drug discovery efforts toward the identification of new chemical entities endowed with a potent and safe antitumor profile. In [...] Read more.
The burden of neoplastic diseases is widely recognized as a severe cause of mortality. The clinical inadequacy of most anticancer therapeutics urgently prompted intense drug discovery efforts toward the identification of new chemical entities endowed with a potent and safe antitumor profile. In this scenario, targeting cancer cells apoptosis machinery has emerged as a relevant strategy, useful for tackling the emergence of drug resistance. On this basis, a small library of naturally inspired hybrid molecules was obtained by combining, through a click chemistry approach, “privileged” synthons such as curcumin scaffold and 1,2,3-triazole building block. Compound 1, bearing a para-fluoro phenyl moiety, showed low-micromolar potency against T acute lymphoblastic leukemia cell growth. More in-depth biologic studies demonstrated, for this analog, cell death-inducing properties associated with its capability to simultaneously activate both the receptor and the mitochondrial apoptosis cascades. This peculiar behavior offers promises for achieving an expanded anticancer effect, namely intense cytotoxic response coupled with reduced predisposition of chemoresistance insurgence. Altogether, this study allowed the identification of compound 1 as a lead compound worth to be progressed as an anticancer drug candidate. Full article
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