Special Issue "Selected Papers from the 3rd International Electronic Conference on Medicinal Chemistry"

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

Deadline for manuscript submissions: 30 April 2018

Special Issue Editor

Guest Editor
Dr. Jean Jacques Vanden Eynde

Formerly head of the Department of Organic Chemistry (FS), University of Mons-UMONS, 7000 Mons, Belgium
Website | E-Mail
Interests: heterocycles; microwave-induced synthesis; medicinal chemistry; green chemistry

Special Issue Information

Dear Colleagues,

This Special Issue comprises selected papers from the 3rd International Electronic Conference on Medicinal Chemistry (ECMC-3), held 1–30 November, 2017, on sciforum.net, an online platform for hosting scholarly e-conferences and discussion groups. For more information on ECMC-3, please go to: http://sciforum.net/conference/ecmc-3.

Dr. Jean Jacques Vanden Eynde
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. Pharmaceuticals is an international peer-reviewed open access quarterly 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 850 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.

Related Special Issues

Published Papers (2 papers)

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Open AccessArticle Vitamin E Phosphate Nucleoside Prodrugs: A Platform for Intracellular Delivery of Monophosphorylated Nucleosides
Pharmaceuticals 2018, 11(1), 16; doi:10.3390/ph11010016
Received: 23 December 2017 / Revised: 30 January 2018 / Accepted: 30 January 2018 / Published: 6 February 2018
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Abstract
Vitamin E phosphate (VEP) nucleoside prodrugs are designed to bypass two mechanisms of tumor resistance to therapeutic nucleosides: nucleoside transport and kinase downregulation. Certain isoforms of vitamin E (VE) have shown activity against solid and hematologic tumors and result in chemosensitization. Because gemcitabine
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Vitamin E phosphate (VEP) nucleoside prodrugs are designed to bypass two mechanisms of tumor resistance to therapeutic nucleosides: nucleoside transport and kinase downregulation. Certain isoforms of vitamin E (VE) have shown activity against solid and hematologic tumors and result in chemosensitization. Because gemcitabine is one of the most common chemotherapeutics for the treatment of cancer, it was used to demonstrate the constructs utility. Four different VE isoforms were conjugated with gemcitabine at the 5′ position. Two of these were δ-tocopherol-monophosphate (MP) gemcitabine (NUC050) and δ-tocotrienol-MP gemcitabine (NUC052). NUC050 was shown to be able to deliver gemcitabine-MP intracellularly by a nucleoside transport independent mechanism. Its half-life administered IV in mice was 3.9 h. In a mouse xenograft model of non-small cell lung cancer (NSCLC) NCI-H460, NUC050 at a dose of 40 mg/kg IV qwk × 4 resulted in significant inhibition to tumor growth on days 11–31 (p < 0.05) compared to saline control (SC). Median survival was 33 days (NUC050) vs. 25.5 days (SC) ((hazard ratio) HR = 0.24, p = 0.017). Further, NUC050 significantly inhibited tumor growth compared to historic data with gemcitabine at 135 mg/kg IV q5d × 3 on days 14–41 (p < 0.05). NUC052 was administered at a dose of 40 mg/kg IV qwk × 2 followed by 50 mg/kg qwk × 2. NUC052 resulted in inhibition to tumor growth on days 14–27 (p < 0.05) and median survival was 34 days (HR = 0.27, p = 0.033). NUC050 and NUC052 have been shown to be safe and effective in a mouse xenograft of NSCLC. Full article
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Open AccessMeeting Report Third International Electronic Conference on Medicinal Chemistry (ECMC-3)
Pharmaceuticals 2018, 11(1), 18; doi:10.3390/ph11010018
Received: 6 February 2018 / Revised: 7 February 2018 / Accepted: 7 February 2018 / Published: 9 February 2018
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Abstract
The third International Electronic Conference on Medicinal Chemistry, organized and sponsored by MDPI AG, publisher, and the journal Pharmaceuticals, took place in November 2017 on the SciForum website (www.sciforum.net/conference/ecmc-3). Around 300 authors from 34 different countries participated at the event, which hosted
[...] Read more.
The third International Electronic Conference on Medicinal Chemistry, organized and sponsored by MDPI AG, publisher, and the journal Pharmaceuticals, took place in November 2017 on the SciForum website (www.sciforum.net/conference/ecmc-3). Around 300 authors from 34 different countries participated at the event, which hosted more than 70 presentations, keynotes, videos, and posters. A short description of some works presented during that scientific meeting is disclosed in this report. Full article

Planned Papers

The below list represents only planned manuscripts. Some of these manuscripts have not been received by the Editorial Office yet. Papers submitted to MDPI journals are subject to peer-review.

Title: Arylideneketones with Potent Trypanosomicidal Activity that Causes Late Apoptosis/Necrosis Like Nifurtimox
Article type: Article
Authors: Elena Aguilera 1,*, Florencia Mosquillo 2, Leticia Pérez 2, Hugo Cerecetto 3, Guzmán Álvarez 4 and Mercedes González 1
Affiliations: 1 Grupo de Química Medicinal, Facultad de Ciencias Universidad de la República, Iguá. 4225, Montevideo, 11400, Uruguay.
2 Laboratorio de Interacciones Moleculares, Facultad de Ciencias, Universidad de la República, Iguá, 4225, Montevideo. 11400, Uruguay.
3 Área de Radiofarmacia, Centro de Investigaciones Nucleares, Universidad de la República, Mataojo S/N, Montevideo, 11400, Uruguay.
4 Laboratorio de Moléculas Bioactivas Centro Universitario Regional Litoral Norte Universidad de la República, Rute 3 km 363, Paysandú, 60000. Uruguay.

Title: Late-stage C-H Arylation of Thiazolo[5,4-f]quinazolin-9(8H)-one Backbone: Synthesis of an Array of Potential Kinase Inhibitors
Article type: Article
Authors: Florence Couly 1, Carole Dubouilh-benard 1, Laurent Meijer 2, Corinne Fruit 1 and Thierry Besson 1,*
Affiliation: 1 Normandie Univ, COBRA, UMR 6014 & FR 3038; Univ Rouen. CNRS, IRCOF, 1 Rue Tesnière, 76821 Mont St Aignan Cedex, France.
2 Manros Therapeutics, Centre de Perharidy, 29680 Roscoff, France.

Title: A Short Peptide Inhibitor as an Activity-Based Probe for Matriptase-2
Article type: Article
Authors: Martin Mangold *, Michael Gütschow and Marit Stirnberg
Affiliation: Pharmaceutical Institute, Pharmaceutical Chemistry I, University of Bonn

Title: Study of Interactions between D-Mannitol and Polynucleotides
Article type: Article
Authors: Volodymyr Shchodryi * and Zenoviy Tkachuk
Affiliation: Institute of molecular biology and genetics NAS of Ukraine

Title: Searching bioactive molecules in prostate cancer from Mayan traditional medicinal plants
Article type: Article
Authors: Juan Trinidad 1,2, Rafael Fort 2, Juliette Dourron 1 , Francisco J. Aguirre 3, María Ana Duhagon 2,*, Guzmán Álvarez 1,*
Affiliation: 1 Laboratorio de Moléculas Bioactivas, CENUR Litoral Norte, Universidad de la República, Ruta 3 (km 363), Paysandú, C.P. 60000, Uruguay.
2 Laboratorio de Interacciones Moleculares, Facultad de Ciencias, Universidad de la República.
3 Cuerpo Académico en Ciencias de la Salud y Biotecnología, Facultad de Ciencias Químico Biológicas, Universidad Autónoma de Campeche, México

Title: In Silico SAR Studies of HIV-1 Inhibitors
Article type: Article
Authors: Ismail Hdoufane, Imane Bjij, Mahmoud E. S. Soliman,  Alia Tadjer, Didier Villemin, Jane Bogdanov, Driss Cherqaoui
Affiliation: Department of Chemistry, Faculty of Science Semlalia, BP 2390, Marrakech, Morocco

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