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Special Issue "The Biomedical Importance of Indoles and Their Derivatives"

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

Deadline for manuscript submissions: closed (30 November 2017)

Special Issue Editors

Guest Editor
Prof. Dr. Patrizia Diana

Pharmaceutical Chemistry at the University of Palermo, Palermo, Italy
Website | E-Mail
Fax: +39 09123860854
Interests: drug discovery; kinases; cancer; pharmacology; biological drugs; drug resistance
Guest Editor
Dr. Barbara Parrino

Department of Biological Chemical and Pharmaceutical Sciences and Technologies (STEBICEF), University of Palermo, Viale delle Scienze Ed 16, 90128 Palermo, Italy
Website | E-Mail
Interests: marine alkaloids; heterocycles; drug discovery; synthesis; bioactive compounds; antitumor activity

Special Issue Information

Dear Colleagues,

Indole moieties represent important scaffolds in drug discovery. Indoles and their derivatives are natural and synthetic molecules which have useful biological properties such as antimicrobial, antiviral, antitubercular, anti-inflammatory, anticancer, antidiabetic, anticonvulsant, antimicrobial, antioxidant, antidepresent, and anticonvulsant activities.

This Special Issue is dedicated to “The Biomedical Importance of Indoles and Their Derivatives" and will focus on indoles and derivatives that are potentially useful as lead compounds for the development of new bioactive compounds. As the Guest Editors, we invite scientists in the fields of medicinal chemistry, biochemistry, pharmacology, and toxicology to present their recent advances in the drug discovery, isolation, synthesis, biosynthesis, structural elucidation, bioactivity evaluation and mode of action of indoles and their derivatives.

Prof. Dr. Patrizia Diana
Dr Barbara Parrino
Guest Editors

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. Molecules 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 1800 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

  • Indoles
  • Isolation
  • Structure elucidation
  • Drug discovery
  • Synthesis
  • Biosynthesis
  • Natural products
  • Biological activity

Published Papers (5 papers)

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Research

Open AccessArticle Effect of Indolic-Amide Melatonin on Blood Cell Population: A Biophysical Gaussian Statistical Analysis
Molecules 2018, 23(6), 1378; https://doi.org/10.3390/molecules23061378
Received: 13 May 2018 / Revised: 31 May 2018 / Accepted: 5 June 2018 / Published: 7 June 2018
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Abstract
The problem of the correlation of indolic molecules with special regard to melatonin and immune processes has been widely investigated. However, there are only few studies focusing on circadian variation of peripheral blood leukocytes. The purpose of this study is thus to understand
[...] Read more.
The problem of the correlation of indolic molecules with special regard to melatonin and immune processes has been widely investigated. However, there are only few studies focusing on circadian variation of peripheral blood leukocytes. The purpose of this study is thus to understand the influence of MLT on leukocyte populations and its correlation with leukocyte distribution. This is accomplished by administrating placebo and melatonin to different groups of individuals and by performing a biophysical Gaussian analysis on the number of leukocytes by means of a comparison of their p.m. vs. a.m. variations under the effect of placebo and of melatonin and via a comparison in the morning between leukocytes population of untreated group and MLT group. It is shown that: (a) melatonin has the effect of narrowing the normal distribution concentrating most of the individuals towards the mean value of the observed variation of leukocytes population and (b) the individuals who have not received either placebo or supplement have a leukocyte population that follows a normal distribution. These results confirm the crucial role played by melatonin, as the most representative of indolic amide in biological systems, in the circadian peripheral variations of leukocyte numbers because counts of white blood cells are essential in medical urgency and differential diagnosis situations. Hence, further studies are suggested to account for these physiological variations and for the evaluation of the full involvement of the action of MLT on leukocytes distribution. Full article
(This article belongs to the Special Issue The Biomedical Importance of Indoles and Their Derivatives)
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Open AccessArticle New Tripentone Analogs with Antiproliferative Activity
Molecules 2017, 22(11), 2005; https://doi.org/10.3390/molecules22112005
Received: 27 October 2017 / Revised: 16 November 2017 / Accepted: 17 November 2017 / Published: 18 November 2017
Cited by 2 | PDF Full-text (1426 KB) | HTML Full-text | XML Full-text
Abstract
Tripentones represent an interesting class of compounds due to their significant cytotoxicity against different human tumor cells in the submicro-nanomolar range. New tripentone analogs, in which a pyridine moiety replaces the thiophene ring originating the fused azaindole system endowed with anticancer activity viz
[...] Read more.
Tripentones represent an interesting class of compounds due to their significant cytotoxicity against different human tumor cells in the submicro-nanomolar range. New tripentone analogs, in which a pyridine moiety replaces the thiophene ring originating the fused azaindole system endowed with anticancer activity viz 8H-thieno[2,3-b]pyrrolizinones, were efficiently synthesized in four steps with fair overall yields (34–57%). All tripentone derivatives were tested in the range of 0.1–100 μM for cytotoxicity against two human tumor cell lines, HCT-116 (human colorectal carcinoma) and MCF-7 (human breast cancer). The most active derivative, with GI50 values of 4.25 µM and 20.73 µM for HCT-116 and MCF-7 cells, respectively, did not affect the viability of Caco-2 differentiated in normal intestinal-like cells, suggesting tumor cells as the main target of its cytotoxic action. The same compound was further investigated in order to study its mode of action. Results showed that it did not exert necrotic effects, while induced a clear shift of viable cells towards early apoptosis. Flow cytometric analysis demonstrated that this compound caused cell cycle alteration, inhibiting its progression in S and G2/M phases. Full article
(This article belongs to the Special Issue The Biomedical Importance of Indoles and Their Derivatives)
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Graphical abstract

Open AccessArticle Synthesis, Spectroscopic Characterization and Antimicrobial Potential of Certain New Isatin-Indole Molecular Hybrids
Molecules 2017, 22(11), 1958; https://doi.org/10.3390/molecules22111958
Received: 25 September 2017 / Revised: 29 October 2017 / Accepted: 8 November 2017 / Published: 15 November 2017
Cited by 3 | PDF Full-text (1992 KB) | HTML Full-text | XML Full-text
Abstract
Molecular hybridization has a wide application in medicinal chemistry to obtain new biologically active compounds. New isatin-indole molecular hybrids 5an have been synthesized and characterized by various spectroscopic tools. The in vitro antimicrobial potential of the prepared compounds 5an
[...] Read more.
Molecular hybridization has a wide application in medicinal chemistry to obtain new biologically active compounds. New isatin-indole molecular hybrids 5an have been synthesized and characterized by various spectroscopic tools. The in vitro antimicrobial potential of the prepared compounds 5an was assessed using diameter of the inhibition zone (DIZ) and minimum inhibitory concentration (MIC) assays against a panel of Gram-negative bacteria, Gram-positive bacteria and fungi. Most of the synthesized compounds 5an showed weak activities against Gram-negative bacteria while compounds 5b and 5c exhibited good activities against Gram-positive bacteria. On the other hand, compound 5j emerged as the most active compound towards Candida albicans (C. albicans), with an MIC value of 3.9 µg/mL, and compound 5g as the most active congener towards Asperagillus niger (A. niger), with an MIC value of 15.6 µg/mL. Moreover, compound 5h manifested the best anti-P. notatum effect, with an MIC value of 7.8 µg/mL, making it equipotent with compound 5g. Full article
(This article belongs to the Special Issue The Biomedical Importance of Indoles and Their Derivatives)
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Open AccessArticle Solvent-Free Addition of Indole to Aldehydes: Unexpected Synthesis of Novel 1-[1-(1H-Indol-3-yl) Alkyl]-1H-Indoles and Preliminary Evaluation of Their Cytotoxicity in Hepatocarcinoma Cells
Molecules 2017, 22(10), 1747; https://doi.org/10.3390/molecules22101747
Received: 14 September 2017 / Accepted: 13 October 2017 / Published: 17 October 2017
PDF Full-text (6731 KB) | HTML Full-text | XML Full-text | Supplementary Files
Abstract
New 1-[1-(1H-indol-3-yl) alkyl]-1H-indoles, surprisingly, have been obtained from the addition of indole to a variety of aldehydes under neat conditions. CaO, present in excess, was fundamental for carrying out the reaction with paraformaldehyde. Under the same reaction conditions, aromatic
[...] Read more.
New 1-[1-(1H-indol-3-yl) alkyl]-1H-indoles, surprisingly, have been obtained from the addition of indole to a variety of aldehydes under neat conditions. CaO, present in excess, was fundamental for carrying out the reaction with paraformaldehyde. Under the same reaction conditions, aromatic and heteroaromatic aldehydes afforded only classical bis (indolyl) aryl indoles. In this paper, the role of CaO, together with the regiochemistry and the mechanism of the reaction, are discussed in detail. The effect of some selected 3,3′- and 1,3′-diindolyl methane derivatives on cell proliferation of the hepatoma cell line FaO was also evaluated. Full article
(This article belongs to the Special Issue The Biomedical Importance of Indoles and Their Derivatives)
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Graphical abstract

Open AccessArticle In silico Study of the Pharmacologic Properties and Cytotoxicity Pathways in Cancer Cells of Various Indolylquinone Analogues of Perezone
Molecules 2017, 22(7), 1060; https://doi.org/10.3390/molecules22071060
Received: 30 May 2017 / Revised: 16 June 2017 / Accepted: 19 June 2017 / Published: 25 June 2017
Cited by 1 | PDF Full-text (6289 KB) | HTML Full-text | XML Full-text
Abstract
Several indolylquinone analogues of perezone, a natural sesquiterpene quinone, were characterized in this work by theoretical methods. In addition, some physicochemical, toxicological and metabolic properties were predicted using bioinformatics software. The predicted physicochemical properties are in agreement with the solubility and cLogP values,
[...] Read more.
Several indolylquinone analogues of perezone, a natural sesquiterpene quinone, were characterized in this work by theoretical methods. In addition, some physicochemical, toxicological and metabolic properties were predicted using bioinformatics software. The predicted physicochemical properties are in agreement with the solubility and cLogP values, the penetration across the cell membrane, and absorption values, as well as with a possible apoptosis-activated mechanism of cytotoxic action. The toxicological predictions suggest no mutagenic, tumorigenic or reproductive effects of the four target molecules. Complementarily, the results of a performed docking study show high scoring values and hydrogen bonding values in agreement with the cytotoxicity IC50 value ranking, i.e: indolylmenadione > indolylperezone > indolylplumbagine > indolylisoperezone. Consequently, it is possible to suggest an appropriate apoptotic pathway for each compound. Finally, potential metabolic pathways of the molecules were proposed. Full article
(This article belongs to the Special Issue The Biomedical Importance of Indoles and Their Derivatives)
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Graphical abstract

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