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Synthesis of Drug Intermediates

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

Deadline for manuscript submissions: closed (30 July 2020) | Viewed by 3279

Special Issue Editor


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Guest Editor
School of Chemical and Biomedical Engineering, Nanyang Technological University, 62 Nanyang Drive, N1.2-B1-14, Singapore 637459, Singapore
Interests: carbohydrate chemistry: reactions and methodology; synthesis of natural products and drug intermediates; asymmetric catalysis; green chemistry

Special Issue Information

Dear Colleagues,

The development of synthetic routes for drug intermediates constitutes a key step in drug discovery and development. Over the past decades, several key reactions and strategies have been successfully developed to achieve efficient and practical syntheses of these intermediates. In addition, chemical catalysts and biocatalysts have been elegantly utilized for this purpose. Many researchers have reported green routes of synthesis that have significantly contributed to the reduction of chemical waste and improved the economy of such syntheses.

In this Special Issue, we invite contributions on all aspects of synthesis of small molecule drug intermediates, including development of new syntheses, significant improvement of existing routes of synthesis, catalytic and multicomponent synthesis, as well as combinatorial synthesis. Green routes of syntheses are also welcome. This Special Issue aims to highlight the important features that are key for the synthesis of drug intermediates by presenting high-quality research and insights into new or improved synthetic routes.

Prof. Zaher Judeh
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

  • drug intermediates
  • drug synthesis
  • green synthesis
  • catalysis

Published Papers (1 paper)

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Research

13 pages, 1287 KiB  
Article
Synthesis and Antiproliferative Evaluation of Novel Longifolene-Derived Tetralone Derivatives Bearing 1,2,4-Triazole Moiety
by Xia-Ping Zhu, Gui-Shan Lin, Wen-Gui Duan, Qing-Min Li, Fang-Yao Li and Shun-Zhong Lu
Molecules 2020, 25(4), 986; https://doi.org/10.3390/molecules25040986 - 22 Feb 2020
Cited by 20 | Viewed by 2682
Abstract
Seventeen novel 2-(5-amino-1-(substituted sulfonyl)-1H-1,2,4-triazol-3-ylthio)-6- isopropyl-4,4-dimethyl-3,4-dihydronaphthalen-1(2H)-one compounds were synthesized from the abundant and naturally renewable longifolene and their structures were confirmed by FT-IR, NMR, and ESI-MS. The in vitro cytotoxicity of the synthesized compounds was evaluated by standard MTT assay [...] Read more.
Seventeen novel 2-(5-amino-1-(substituted sulfonyl)-1H-1,2,4-triazol-3-ylthio)-6- isopropyl-4,4-dimethyl-3,4-dihydronaphthalen-1(2H)-one compounds were synthesized from the abundant and naturally renewable longifolene and their structures were confirmed by FT-IR, NMR, and ESI-MS. The in vitro cytotoxicity of the synthesized compounds was evaluated by standard MTT assay against five human cancer cell lines, i.e., T-24, MCF-7, HepG2, A549, and HT-29. As a result, compounds 6d, 6g, and 6h exhibited better and more broad-spectrum anticancer activity against almost all the tested cancer cell lines than that of the positive control, 5-FU. Some intriguing structure–activity relationships were found and are discussed herein by theoretical calculation. Full article
(This article belongs to the Special Issue Synthesis of Drug Intermediates)
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