Special Issue "Medicinal Chemistry of Indole and Quinoline Derivatives: Trends, and Future Directions as Therapeutic Drugs"
Deadline for manuscript submissions: 20 March 2024 | Viewed by 1275
Nitrogen-containing heterocycles have made an enormous contribution to medicinal and pharmaceutical chemistry since the identification of alkaloids such as morphine and strychnine. The prevalence and potency of nitrogen-containing natural products that incorporate indole and quinoline (with melatonin, quinine, serotonin and tryptophan as other examples) frame this success.
The two bicyclic ring systems have provided a rich source of diversity, upon which medicinal and pharmaceutical chemistry has thrived, and multiple examples of therapeutics with real-life benefits exist. Examples on the WHO Essential Medicines List stretch from chloroquine (discovered in 1934) to ciprofloxacin, fluvastatin, indomethacin, mefloquine, ondansetron, primaquine, quinine and sumatriptan. More recently, aripiprazole, tadalafil and ziprasidone are some of the most commonly prescribed medicines and highlight the tangible impact of these heterocycles on people and the treatment of their diseases.
Medicinal chemistry approaches to find small-molecule lead compounds with pharmacological activity continue to use natural products, synthesis and existing small-molecule drug libraries as sources. The focus of this series of papers is the use of indole and quinoline as therapeutics.
The journal Pharmaceuticals invites both reviews and original articles which concern the use of indoles and quinolines in the discovery and development of pharmaceuticals. The scope of the Special Issue will cover, but is not limited to: new synthetic methods in the synthesis of indoles and quinolines, medicinal chemistry and structure–activity studies of indole and quinoline derivatives, natural product discovery involving indoles and quinolines, indole and quinoline drug repositioning, new combinations of indoles and quinolines, and indoles and quinolines beyond pharmaceutical applications. The collection of manuscripts will be published as a Special Issue of the journal.
Dr. Florence O. McCarthy
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.
- pharmaceutical discovery and development
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: Nature-inspired 1-phenylpyrrolo[2,1-a]isoquinoline scaffold for novel antiproliferative agents circumventing P-glycoprotein-dependent multidrug resistance
Author(s): Alisa A. Nevskaya (1), Rosa Purgatorio (2), Aryna Obidennik (1), Lada V. Anikina (3), Elena Yu. Nevskaya (1), Tatiana Borisova (1), Mauro Niso (2), Antonio Carrieri (2), Marco Catto (2), Modesto de Candia (2), Leonid G. Voskressensky (2) and Cosimo D. Altomare (1)
The Corresponding author(s): Cosimo D. Altomare
(1) Organic Chemistry Department, Peoples’ Friendship University of Russia (RUDN University), 6 Miklukho-Maklaya St., 117198 Moscow, Russia
(2) Department of Pharmacy-Pharmaceutical Sciences, University of Bari Aldo Moro, Via E. Orabona 4, 70125 Bari, Italy
(3) Institute of Physiologically Active Compounds, Russian Academy of Sciences, 142432 Chernogolovka, Russia
Abstract: Previous studies showed that some lamellarin-resembling annelated azaheterocyclic carbaldehydes and related adducts, sharing the 1-phenyl-5,6-dihydropyrrolo[2,1-a]isoquinoline (1-Ph-DHPIQ) scaffold, are cytotoxic in tumor cells and may reverse multidrug resistance (MDR) mediated by P-glycoprotein (P-gp). Herein, we synthesized and evaluated for their in-vitro antiproliferative activity in four tumor cell lines (RD, HCT116, HeLa, A549) and ability of inhibiting P-gp-mediated MDR some fifteen diversely substituted 1-Ph-DHPIQ derivatives bearing at position 2 carboxylic derivatives (COOH, COOMe), nitriles (CN) and Mannich bases (e.g., morfolinomethyl derivatives). The results improved our understanding of the structure-activity relationships of this new class of compounds and led us to disclose a novel water-soluble Mannich base, stable at pHs 2 and 7.4 at r.t., which proved to be cytotoxic to all the tested tumor cell lines in the low micromolar range (IC50 < 20 uM) and to inhibit in-vitro the efflux pumps P-gp and MRP1 responsible for multidrug resistance, with IC50s of 0.4 and 1.8 uM, respectively.