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Special Issue "Synthesis of Antitumor Marine Alkaloids and Related Analogues"

A special issue of Marine Drugs (ISSN 1660-3397).

Deadline for manuscript submissions: closed (30 September 2016)

Special Issue Editor

Guest Editor
Prof. Dr. Patrizia Diana

Department of Biological Chemical and Pharmaceutical Sciences and Technologies (STEBICEF), University of Palermo, Via Archirafi, 32-90123 Palermo, Italy
Website | E-Mail
Fax: +39 09123860854
Interests: marine alkaloids; heterocycles; drug discovery; synthesis; bioactive compounds; antitumor activity

Special Issue Information

Dear Colleagues,

Oceans have been considered as the main source of medicines and, during the past two decades, thousands of compounds and their metabolites have exhibited a wide range of biological activity. Marine organisms constitute a very important source of biologically active natural products, including some of the most potent antineoplastic agents presently discovered. Due to the small amounts of biologically active substances extracted from natural materials, several total syntheses were proposed. Moreover, due to their interesting biological activities, marine alkaloids are considered to be important lead compounds for the discovery of new biologically active compounds. The use of microbial genetics and biosynthesis are useful to develop innovative methods to discover new natural products. This Special Issue dedicated to the "Synthesis of Antitumor Marine Alkaloids and Related Analogues” hopes to emphasize the importance of the study of gene cluster identification and biosynthesis of marine organisms, the total synthesis of marine organisms, the synthesis of new marine analogues, the biological evaluation of bioactive compounds, and the studies of mode action. As the Guest Editor, I invite scientists in the fields of chemistry, biochemistry, pharmacology, and toxicology.

Prof. Patrizia Diana
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 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. Marine Drugs 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

•    marine natural product
•    biosynthesis
•    gene cluster
•    total synthesis
•    synthesis of marine analogue
•    chemical transformation
•    chemical modification
•    antitumor activity

Published Papers (5 papers)

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Research

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Open AccessArticle Synthesis and Antitumor Activity of New Thiazole Nortopsentin Analogs
Mar. Drugs 2016, 14(12), 226; doi:10.3390/md14120226
Received: 10 October 2016 / Revised: 13 November 2016 / Accepted: 5 December 2016 / Published: 14 December 2016
Cited by 6 | PDF Full-text (2257 KB) | HTML Full-text | XML Full-text
Abstract
New thiazole nortopsentin analogs in which one of the two indole units was replaced by a naphthyl and/or 7-azaindolyl portion, were conveniently synthesized. Among these, three derivatives showed good antiproliferative activity, in particular against MCF7 cell line, with GI50 values in the
[...] Read more.
New thiazole nortopsentin analogs in which one of the two indole units was replaced by a naphthyl and/or 7-azaindolyl portion, were conveniently synthesized. Among these, three derivatives showed good antiproliferative activity, in particular against MCF7 cell line, with GI50 values in the micromolar range. Their cytotoxic effect on MCF7 cells was further investigated in order to elucidate their mode of action. Results showed that the three compounds act as pro-apoptotic agents inducing a clear shift of viable cells towards early apoptosis, while not exerting necrotic effects. They also caused cell cycle perturbation with significant decrease in the percentage of cells in the G0/G1 and S phases, accompanied by a concomitant percentage increase of cells in the G2/M phase, and appearance of a subG1-cell population. Full article
(This article belongs to the Special Issue Synthesis of Antitumor Marine Alkaloids and Related Analogues)
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Chart 1

Open AccessArticle Synthesis of Pelorol and Its Analogs and Their Inhibitory Effects on Phosphatidylinositol 3-Kinase
Mar. Drugs 2016, 14(6), 118; doi:10.3390/md14060118
Received: 16 April 2016 / Revised: 13 May 2016 / Accepted: 18 May 2016 / Published: 21 June 2016
PDF Full-text (1238 KB) | HTML Full-text | XML Full-text | Supplementary Files
Abstract
There are numerous biologically active substances with novel structures and unique physiological functions in marine organisms. These substances are important sources of new lead compounds. Pelorol is a natural product isolated from marine organisms that possesses a novel structure with high bioactivity. In
[...] Read more.
There are numerous biologically active substances with novel structures and unique physiological functions in marine organisms. These substances are important sources of new lead compounds. Pelorol is a natural product isolated from marine organisms that possesses a novel structure with high bioactivity. In this paper, the synthesis of pelorol has been completed, and the synthesis of some intermediates has been optimized and scaled up. Five pelorol analogs have also been prepared. Preliminary biological activity testing demonstrated that compounds 5 and 6 might be potential lead compounds for cancer therapy. Full article
(This article belongs to the Special Issue Synthesis of Antitumor Marine Alkaloids and Related Analogues)
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Open AccessArticle Novel Azetidine-Containing TZT-1027 Analogues as Antitumor Agents
Mar. Drugs 2016, 14(5), 85; doi:10.3390/md14050085
Received: 30 March 2016 / Revised: 21 April 2016 / Accepted: 22 April 2016 / Published: 28 April 2016
Cited by 3 | PDF Full-text (1676 KB) | HTML Full-text | XML Full-text | Supplementary Files
Abstract
A conformational restriction strategy was used to design and synthesize nine TZT-1027 analogues. 3-Aryl-azetidine moiety was used to replace phenylethyl group of TZT-1027 at the C-terminus. These analogues exhibited moderate to excellent antiproliferative activities, and the most potent compound 1a showed IC50
[...] Read more.
A conformational restriction strategy was used to design and synthesize nine TZT-1027 analogues. 3-Aryl-azetidine moiety was used to replace phenylethyl group of TZT-1027 at the C-terminus. These analogues exhibited moderate to excellent antiproliferative activities, and the most potent compound 1a showed IC50 values of 2.2 nM against A549 and 2.1 nM against HCT116 cell lines, respectively. However, 1a could not achieve effective inhibition at all the dose levels in the A549 xenograft model (up to 5 mg/kg, injection, once a day), which is only 16%–35% inhibition at the end of the experiment. Full article
(This article belongs to the Special Issue Synthesis of Antitumor Marine Alkaloids and Related Analogues)
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Open AccessArticle In Vitro and in Vivo Anticancer Activity of Pardaxin against Proliferation and Growth of Oral Squamous Cell Carcinoma
Mar. Drugs 2016, 14(1), 2; doi:10.3390/md14010002
Received: 4 November 2015 / Revised: 5 December 2015 / Accepted: 15 December 2015 / Published: 23 December 2015
Cited by 8 | PDF Full-text (4422 KB) | HTML Full-text | XML Full-text
Abstract
Pardaxin (H-GFFALIPKIISSPLFKTLLSAVGSALSSSGGQE-OH), a 33-amino-acid polypeptide, is an antimicrobial peptide (AMP) isolated from the marine fish species Pardachirus marmoratus. Pardaxin shows antibacterial and antitumor activities. However, pardaxin-induced inhibition of oral cancer and the mechanism of tumor reduction in buccal pouch carcinogenesis after pardaxin
[...] Read more.
Pardaxin (H-GFFALIPKIISSPLFKTLLSAVGSALSSSGGQE-OH), a 33-amino-acid polypeptide, is an antimicrobial peptide (AMP) isolated from the marine fish species Pardachirus marmoratus. Pardaxin shows antibacterial and antitumor activities. However, pardaxin-induced inhibition of oral cancer and the mechanism of tumor reduction in buccal pouch carcinogenesis after pardaxin painting remain undetermined. Additionally, the toxic effects of pardaxin on normal tissue remain unclear. The present study investigated the anticancer activity of pardaxin in oral squamous cell carcinoma (OSCC) cells in the hamster buccal pouch model with or without 7,12-dimethylbenz[a]anthracene (DMBA) pretreatment. This is the first study to confirm the effects of pardaxin on normal tissue and its nontoxic effects in vivo. Cell viability assays and colony formation tests in OSCC cell lines (SCC-4) demonstrated that pardaxin reduced cell viability in a dose-dependent manner. Immunofluorescence staining of cleaved caspase-3 in SCC-4 cells revealed that expression of activated caspase-3 in SCC-4 cells significantly increased after 24-h treatment with pardaxin. Additionally, a cell cycle analysis indicated that pardaxin treatment resulted in the cell cycle arrest of SCC-4 cells in the G2/M phase, thereby limiting cell proliferation. Furthermore, pardaxin treatment substantially alleviated carcinogenesis in the DMBA-induced hamster buccal pouch model by lowering prostaglandin E2 levels. These results suggest that pardaxin is a potential marine drug for adjuvant chemotherapy for human OSCC and oral cancer. Full article
(This article belongs to the Special Issue Synthesis of Antitumor Marine Alkaloids and Related Analogues)
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Review

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Open AccessReview New Perspectives in the Chemistry of Marine Pyridoacridine Alkaloids
Mar. Drugs 2016, 14(2), 26; doi:10.3390/md14020026
Received: 28 November 2015 / Revised: 9 January 2016 / Accepted: 15 January 2016 / Published: 26 January 2016
Cited by 1 | PDF Full-text (6538 KB) | HTML Full-text | XML Full-text
Abstract
Secondary metabolites from marine organisms are a rich source of novel leads for drug development. Among these natural products, polycyclic aromatic alkaloids of the pyridoacridine type have attracted the highest attention as lead compounds for the development of novel anti-cancer and anti-infective drugs.
[...] Read more.
Secondary metabolites from marine organisms are a rich source of novel leads for drug development. Among these natural products, polycyclic aromatic alkaloids of the pyridoacridine type have attracted the highest attention as lead compounds for the development of novel anti-cancer and anti-infective drugs. Numerous sophisticated total syntheses of pyridoacridine alkaloids have been worked out, and many of them have also been extended to the synthesis of libraries of analogues of the alkaloids. This review summarizes the progress in the chemistry of pyridoacridine alkaloids that was made in the last one-and-a-half decades. Full article
(This article belongs to the Special Issue Synthesis of Antitumor Marine Alkaloids and Related Analogues)
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