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Pharmaceuticals
Special Issues
Heterocyclic Chemistry for Cancer and CNS Diseases
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Heterocyclic Chemistry for Cancer and CNS Diseases

A special issue of Pharmaceuticals (ISSN 1424-8247).

Deadline for manuscript submissions: closed (28 February 2019)

Special Issue Editor

Prof. Dr. Jean-Pierre Bazureau

E-Mail Website
Guest Editor
Institut des Sciences Chimiques de Rennes (ISCR), UMR CNRS 6226, Groupe CORINT, Université de Rennes 1 (UR1), Campus de Beaulieu, Bât. 10A, 263 Avesnue du Général Leclerc, CS 74205, 35042 Rennes CEDEX, France
Interests: microwave-assisted organic chemistry and scale-up; “Store Operated Calcium Entry” inhibitors (Orai1) for cancer via Délikine program inhibitors; mitochondrial ion channel inhibitors for cancer; protein kinase (PKs) inhibitors for CNS (Alzheimer’s disease and Down syndrome) via Leucettine program inhibitors; fluorescence probes for studies of molecular mechanisms in cancer biology
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Heterocycles are prevalent in nature and they have the ability to engage in a wide variety of intermolecular interactions and in biochemical processes; consequently, they plays an important role in anti-cancer drug design (65% of the anti-cancer drugs that have received approval from the Food and Drug Administration (FDA) between 2010 and 2015 contain nitrogen-based heterocycles). New heterocyclic compounds have also been developed in the last ten years for the central nervous system (CNS), particularly for the treatment of Alzheimer's disease (AD). Molecular design for the development of cholinesterase (ChEIs) inhibitors, monoaminoxydases (MAOs) inhibitors, NMDA receptor antagonism, etc., involved the exploration of many natural products (their modified derivatives) and also synthetic heterocyclic compounds.

The purpose of the present Special Issue is to present the latest advances in the field of heterocyclic chemistry, used for possible pharmacological applications in cancer and CNS diseases (dementia, epilepsy, headache disorders, Parkinson's disease (PD), stroke and AD).

Prof. Jean-Pierre Bazureau
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 submissions that pass pre-check are 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. Pharmaceuticals is an international peer-reviewed open access monthly 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 2900 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

  • heterocycles
  • cancer
  • tumoral cells
  • central nervous system
  • cholinesterase inhibitors
  • monoaminoxydases inhibitors
  • NMDA receptor antagonism
  • Alzheimer's disease
  • Parkinson's disease
  • Stroke
  • epilepsy

Published Papers (1 paper)

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Research

18 pages, 2365 KiB  
Article
Synthesis, Evaluation of Cytotoxicity and Molecular Docking Studies of the 7-Acetamido Substituted 2-Aryl-5-bromo-3-trifluoroacetylindoles as Potential Inhibitors of Tubulin Polymerization
by Malose J. Mphahlele and Nishal Parbhoo
Pharmaceuticals 2018, 11(2), 59; https://doi.org/10.3390/ph11020059 - 11 Jun 2018
Cited by 10 | Viewed by 3866
Abstract
The 3-trifluoroacetyl–substituted 7-acetamido-2-aryl-5-bromoindoles 5a–h were prepared and evaluated for potential antigrowth effect in vitro against human lung cancer (A549) and cervical cancer (HeLa) cells and for the potential to inhibit tubulin polymerization. The corresponding intermediates, namely, the 3-unsubstituted 7-acetyl-2-aryl-5-bromoindole 2a– [...] Read more.
The 3-trifluoroacetyl–substituted 7-acetamido-2-aryl-5-bromoindoles 5a–h were prepared and evaluated for potential antigrowth effect in vitro against human lung cancer (A549) and cervical cancer (HeLa) cells and for the potential to inhibit tubulin polymerization. The corresponding intermediates, namely, the 3-unsubstituted 7-acetyl-2-aryl-5-bromoindole 2a–d and 7-acetamido-2-aryl-5-bromoindole 4a–d were included in the assays in order to correlate both structural variations and cytotoxicity. No cytotoxicity was observed for compounds 2a–d and their 3-trifluoroacetyl–substituted derivatives 5a–d against both cell lines. The 7-acetamido derivatives 4–d exhibited modest cytotoxicity against both cell lines. All of the 3-trifluoroacetyl–substituted 7-acetamido-2-aryl-5-bromoindoles 5e–h were found to be more active against both cell lines when compared to the chemotherapeutic drug, Melphalan. The most active compound, 5g, induced programmed cell death (apoptosis) in a caspase-dependent manner for both A549 and HeLa cells. Compounds 5e–h were found to significantly inhibit tubulin polymerization against indole-3-carbinol and colchicine as reference standards. Molecular docking of 5g into the colchicine-binding site suggests that the compounds bind to tubulin by different type of interactions including pi-alkyl, amide-pi stacked and alkyl interactions as well as hydrogen bonding with the protein residues to elicit anticancer activity. Full article
(This article belongs to the Special Issue Heterocyclic Chemistry for Cancer and CNS Diseases)
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