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Second Edition: Organic Synthesis in Drug Discovery

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

Deadline for manuscript submissions: closed (30 November 2022) | Viewed by 2785

Special Issue Editor


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Guest Editor
Department of Chemistry, University of Aberdeen, Meston Walk, Aberdeen AB24 3UE, UK
Interests: organic synthesis; aromatic chemistry; heteroaromatic chemistry; stereochemistry; history of dyes; supramolecular chemistry; prebiotic chemistry; drug-DNP complexing; optical limiting; organic minerals; ammonia free hair dyeing
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

It is our pleasure to announce the launch of the Second Edition of our Special Issue in Molecules on the topic of organic synthesis in drug discovery. This can be interpreted in a broad light and can cover the topics listed in the key words. It is recommended that each paper should have a short introduction which indicates which classes of biologically active compound the work is relevant to. Compounds reported in the papers should have full synthetic characterisation data and some biological data. Known compounds should have a literature reference. Compounds without biological data may be published if the compounds are or are related to a known class of active substance such as steroids, central nervous system (CNS) active drugs, building blocks for active natural products or pharmaceuticals, etc. Industrial pharmaceutical discovery or synthesis or late-stage drug selection is welcome. The aim is to highlight the role that organic synthesis plays in developing methods that may be exploited for finding lead compounds and drugs by the pharmaceutical industry.

Dr. Michael John Plater
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. 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 2700 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

  • organic synthesis
  • medicinal chemistry synthesis
  • synthetic methodology
  • asymmetric synthesis
  • heterocyclic synthesis
  • synthesis of new ring systems
  • free radicals in synthesis
  • diversity in synthesis
  • catalytic asymmetric synthesis
  • organometallic chemistry
  • total synthesis
  • flow chemistry
  • stereoelectronic effects
  • tetrahedral intermediates
  • reactive intermediates in synthesis
  • molecular rearrangements in synthesis
  • curly arrow reaction mechanisms

Published Papers (1 paper)

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Research

18 pages, 2829 KiB  
Article
Synthesis, Leishmanicidal, Trypanocidal, Antiproliferative Assay and Apoptotic Induction of (2-Phenoxypyridin-3-yl)naphthalene-1(2H)-one Derivatives
by Zuleima Blanco, Esteban Fernandez-Moreira, Michael R. Mijares, Carmen Celis, Gricelis Martínez, Juan B. De Sanctis, Soňa Gurská, Petr Džubák, Marián Hajdůch, Ali Mijoba, Yael García, Xenón Serrano, Nahum Herrera, Jhonny Correa-Abril, Yonathan Parra, Jorge Ángel, Hegira Ramírez and Jaime E. Charris
Molecules 2022, 27(17), 5626; https://doi.org/10.3390/molecules27175626 - 31 Aug 2022
Cited by 2 | Viewed by 2557
Abstract
The coexistence of leishmaniasis, Chagas disease, and neoplasia in endemic areas has been extensively documented. The use of common drugs in the treatment of these pathologies invites us to search for new molecules with these characteristics. In this research, we report 16 synthetic [...] Read more.
The coexistence of leishmaniasis, Chagas disease, and neoplasia in endemic areas has been extensively documented. The use of common drugs in the treatment of these pathologies invites us to search for new molecules with these characteristics. In this research, we report 16 synthetic chalcone derivatives that were investigated for leishmanicidal and trypanocidal activities as well as for antiproliferative potential on eight human cancers and two nontumor cell lines. The final compounds 823 were obtained using the classical base-catalyzed Claisen–Schmidt condensation. The most potent compounds as parasiticidal were found to be 22 and 23, while compounds 18 and 22 showed the best antiproliferative activity and therapeutic index against CCRF-CEM, K562, A549, and U2OS cancer cell lines and non-toxic VERO, BMDM, MRC-5, and BJ cells. In the case of K562 and the corresponding drug-resistant K562-TAX cell lines, the antiproliferative activity has shown a more significant difference for compound 19 having 10.3 times higher activity against the K562-TAX than K562 cell line. Flow cytometry analysis using K562 and A549 cell lines cultured with compounds 18 and 22 confirmed the induction of apoptosis in treated cells after 24 h. Based on the structural analysis, these chalcones represent new compounds potentially useful for Leishmania, Trypanosoma cruzi, and some cancer treatments. Full article
(This article belongs to the Special Issue Second Edition: Organic Synthesis in Drug Discovery)
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