Selected papers from the 11th National Meeting of Organic Chemistry and 4th Meeting of Therapeutic Chemistry in Portugal

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

Deadline for manuscript submissions: closed (31 August 2016)

Special Issue Editors


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LAQV/REQUIMTE, Departamento de Química e Bioquímica, Faculdade de Ciências da Universidade do Porto, Rua do Campo Alegre 687, 4169-007 Porto, Portugal
Interests: polyphenols; organic synthesis; spectroscopic methods; chromatography; natural compounds; food chemistry; color; taste

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1. Interdisciplinary Centre of Marine and Environmental Research (CIIMAR), 4450-208 Porto, Portugal
2. Laboratory of Organic and Pharmaceutical Chemistry, Faculty of Pharmacy, University of Porto, 4050-313 Porto, Portugal
Interests: medicinal chemistry; organic synthesis; heterocycles; P-glycoprotein; anticancer; antimicrobials; chiral drugs; marine natural products
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Special Issue Information

Dear Colleagues,

For the first time in Portugal, the competences of two important fields of Chemistry, Organic Chemistry and Medicinal Chemistry, were brought together into a joint meeting in 2015 under the auspices of Portuguese Chemical Society (SPQ). Selected papers are welcome to highlight the different research fields presented. Pharmaceuticals now invites valuable contributions that report original observations or reviews.

For more information about this meeting, please refer to: http://11enqo.eventos.chemistry.pt/.

Prof. Dr. Victor Freitas
Dr. Maria Emília de Sousa
Guest Editors

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Published Papers (3 papers)

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Review

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Review
Curcumin as a Modulator of P-Glycoprotein in Cancer: Challenges and Perspectives
by Vanessa Lopes-Rodrigues, Emília Sousa and M. Helena Vasconcelos
Pharmaceuticals 2016, 9(4), 71; https://doi.org/10.3390/ph9040071 - 10 Nov 2016
Cited by 86 | Viewed by 8701
Abstract
Multidrug resistance (MDR) presents a serious challenge to the efficiency of cancer treatment, and may be associated with the overexpression of drug efflux pumps. P-glycoprotein (P-gp) is a drug efflux pump often found overexpressed in cases of acquired MDR. Nevertheless, there are no [...] Read more.
Multidrug resistance (MDR) presents a serious challenge to the efficiency of cancer treatment, and may be associated with the overexpression of drug efflux pumps. P-glycoprotein (P-gp) is a drug efflux pump often found overexpressed in cases of acquired MDR. Nevertheless, there are no P-gp inhibitors being used in the current clinical practice, due to toxicity problems, drug interactions, or pharmacokinetic issues. Therefore, it is important to identify novel inhibitors of P-gp activity or expression. Curcumin is a secondary metabolite isolated from the turmeric of Curcuma longa L. which has been associated with several biological activities, particularly P-gp modulatory activity (by inhibiting both P-gp function and expression). However, curcumin shows extensive metabolism and instability, which has justified the recent and intensive search for analogs of curcumin that maintain the P-gp modulatory activity but have enhanced stability. This review summarizes and compares the effects of curcumin and several curcumin analogs on P-glycoprotein function and expression, emphasizing the potential of these molecules for the possible development of safe and effective inhibitors of P-gp to overcome MDR in human cancer. Full article
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5261 KiB  
Review
Chemical Variations on the p53 Reactivation Theme
by Carlos J. A. Ribeiro, Cecília M. P. Rodrigues, Rui Moreira and Maria M. M. Santos
Pharmaceuticals 2016, 9(2), 25; https://doi.org/10.3390/ph9020025 - 13 May 2016
Cited by 32 | Viewed by 9722
Abstract
Among the tumor suppressor genes, p53 is one of the most studied. It is widely regarded as the “guardian of the genome”, playing a major role in carcinogenesis. In fact, direct inactivation of the TP53 gene occurs in more than 50% of malignancies, [...] Read more.
Among the tumor suppressor genes, p53 is one of the most studied. It is widely regarded as the “guardian of the genome”, playing a major role in carcinogenesis. In fact, direct inactivation of the TP53 gene occurs in more than 50% of malignancies, and in tumors that retain wild-type p53 status, its function is usually inactivated by overexpression of negative regulators (e.g., MDM2 and MDMX). Hence, restoring p53 function in cancer cells represents a valuable anticancer approach. In this review, we will present an updated overview of the most relevant small molecules developed to restore p53 function in cancer cells through inhibition of the p53-MDMs interaction, or direct targeting of wild-type p53 or mutated p53. In addition, optimization approaches used for the development of small molecules that have entered clinical trials will be presented. Full article
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Meeting Report
11th National Meeting of Organic Chemistry and 4th Meeting of Therapeutic Chemistry
by Maria Emília Sousa, Maria João Araújo, Maria Luísa Do Vale, Paula B. Andrade, Paula Branco, Paula Gomes, Rui Moreira, Teresa M.V.D. Pinho e Melo and Victor Freitas
Pharmaceuticals 2016, 9(1), 15; https://doi.org/10.3390/ph9010015 - 17 Mar 2016
Cited by 1 | Viewed by 10032
Abstract
For the first time under the auspices of Sociedade Portuguesa de Química, the competences of two important fields of Chemistry are brought together into a single event, the 11st National Organic Chemistry Meeting and the the 4th National Medicinal Chemistry Meeting, to highlight [...] Read more.
For the first time under the auspices of Sociedade Portuguesa de Química, the competences of two important fields of Chemistry are brought together into a single event, the 11st National Organic Chemistry Meeting and the the 4th National Medicinal Chemistry Meeting, to highlight complementarities and to promote new synergies. Abstracts of plenary lectures, oral communications, and posters presented during the meeting are collected in this report. Full article
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