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Marine Drugs
Special Issues
Synthetic Chemistry in Marine Drug Discovery: Challenges and Opportunities
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Synthetic Chemistry in Marine Drug Discovery: Challenges and Opportunities

A special issue of Marine Drugs (ISSN 1660-3397). This special issue belongs to the section "Synthesis and Medicinal Chemistry of Marine Natural Products".

Deadline for manuscript submissions: closed (31 July 2024) | Viewed by 21215

Special Issue Editors

Dr. Enol López

E-Mail Website
Guest Editor
Department of Organic Chemistry, Campus Miguel Delives, University of Valladolid, 47011 Valladolid, Spain
Interests: drug discovery; flow chemistry; catalysis
Dr. Francisco Javier Guerra

E-Mail Website
Guest Editor
Department of Organic Chemistry, Campus Miguel Delives, University of Valladolid, 47011 Valladolid, Spain
Interests: flow chemistry; API synthesis; green chemistry; nanomedicine

Special Issue Information

Dear Colleagues,

The marine world is considered the cradle of living organisms. It has been a matter of study since ancient times, allowing us to identify a vast number of biologically active chemical structures which can be used in the development of drug discovery programs. Novel technologies as well as new synthetic methodologies have facilitated the obtention of marine natural products as well as modified marine derivatives with improved pharmacological properties.

The aim of this Special Issue of Marine Drugs is to cover new advances in the synthesis of promising marine drug-like chemical scaffolds through novel technologies, new synthetic approaches, total synthesis or semisynthetic transformations.

As Guest Editors, we invite academic and industry scientists to submit original research articles and reviews to contribute to the synthetic advancement of marine pharmacology.

Dr. Enol López
Dr. Francisco Javier Guerra
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 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. 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 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.

Keywords

  • marine natural products
  • catalysis
  • flow chemistry
  • bioactivity
  • synthesis
  • drug discovery

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Published Papers (7 papers)

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Research

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9 pages, 2040 KiB  
Article
Total Synthesis of Talarolide A and atrop-Talarolide A: Hydroxamate H-Bond Bridge Stabilization of Cyclic Peptide Conformers Invokes Non-Canonical Atropisomerism
by Waleed M. Hussein, Yuxuan Zhu, Angela A. Salim and Robert J. Capon
Mar. Drugs 2024, 22(10), 454; https://doi.org/10.3390/md22100454 - 3 Oct 2024
Viewed by 1079
Abstract
The first total synthesis of the Australian marine tunicate fungus-derived cyclic peptide talarolide A (1) has confirmed the structure previously proposed on the basis of spectroscopic and chemical analyses and re-affirmed the importance of the unique hydroxamate H-bond bridge in ring [...] Read more.
The first total synthesis of the Australian marine tunicate fungus-derived cyclic peptide talarolide A (1) has confirmed the structure previously proposed on the basis of spectroscopic and chemical analyses and re-affirmed the importance of the unique hydroxamate H-bond bridge in ring conformer stabilization. The unexpected co-synthesis of atrop-talarolide A (8) revealed, for the first time, that hydroxamate H-bond bridging in the talarolide framework invokes non-canonical atropisomerism and that talarolides A (1), C (3), and D (4) all exist naturally as atropisomers. These discoveries raise the intriguing prospect that comparable functionalisation of other cyclic peptides, including those with commercial value, could provide ready access to new “unnatural atropisomeric” chemical space, with new and/or improved chemical and biological properties. Full article
(This article belongs to the Special Issue Synthetic Chemistry in Marine Drug Discovery: Challenges and Opportunities)
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29 pages, 11368 KiB  
Article
A New Renieramycin T Right-Half Analog as a Small Molecule Degrader of STAT3
by Preeyaphan Phookphan, Satapat Racha, Masashi Yokoya, Zin Zin Ei, Daiki Hotta, Hongbin Zou and Pithi Chanvorachote
Mar. Drugs 2024, 22(8), 370; https://doi.org/10.3390/md22080370 - 14 Aug 2024
Viewed by 3098
Abstract
Constitutive activation of STAT3 contributes to tumor development and metastasis, making it a promising target for cancer therapy. (1R,4R,5S)-10-hydroxy-9-methoxy-8,11-dimethyl-3-(naphthalen-2-ylmethyl)-1,2,3,4,5,6-hexahydro-1,5-epiminobenzo[d]azocine-4-carbonitrile, DH_31, a new derivative of the marine natural product Renieramycin T, showed potent activity against H292 and H460 cells, with IC50 values of [...] Read more.
Constitutive activation of STAT3 contributes to tumor development and metastasis, making it a promising target for cancer therapy. (1R,4R,5S)-10-hydroxy-9-methoxy-8,11-dimethyl-3-(naphthalen-2-ylmethyl)-1,2,3,4,5,6-hexahydro-1,5-epiminobenzo[d]azocine-4-carbonitrile, DH_31, a new derivative of the marine natural product Renieramycin T, showed potent activity against H292 and H460 cells, with IC50 values of 5.54 ± 1.04 µM and 2.9 ± 0.58 µM, respectively. Structure–activity relationship (SAR) analysis suggests that adding a naphthalene ring with methyl linkers to ring C and a hydroxyl group to ring E enhances the cytotoxic effect of DH_31. At 1–2.5 µM, DH_31 significantly inhibited EMT phenotypes such as migration, and sensitized cells to anoikis. Consistent with the upregulation of ZO1 and the downregulation of Snail, Slug, N-cadherin, and Vimentin at both mRNA and protein levels, in silico prediction identified STAT3 as a target, validated by protein analysis showing that DH_31 significantly decreases STAT3 levels through ubiquitin-proteasomal degradation. Immunofluorescence and Western blot analysis confirmed that DH_31 significantly decreased STAT3 and EMT markers. Additionally, molecular docking suggests a covalent interaction between the cyano group of DH_31 and Cys-468 in the DNA-binding domain of STAT3 (binding affinity = −7.630 kcal/mol), leading to destabilization thereafter. In conclusion, DH_31, a novel RT derivative, demonstrates potential as a STAT3-targeting drug that significantly contribute to understanding of the development of new targeted therapy. Full article
(This article belongs to the Special Issue Synthetic Chemistry in Marine Drug Discovery: Challenges and Opportunities)
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16 pages, 3462 KiB  
Article
Synthesis and Hypoglycemic Effect of Insulin from the Venom of Sea Anemone Exaiptasia diaphana
by Qiqi Guo, Tianle Tang, Jingyue Lu, Meiling Huang, Junqing Zhang, Linlin Ma and Bingmiao Gao
Mar. Drugs 2024, 22(3), 111; https://doi.org/10.3390/md22030111 - 27 Feb 2024
Cited by 1 | Viewed by 2108
Abstract
Sea anemone venom, abundant in protein and peptide toxins, serves primarily for predatory defense and competition. This study delves into the insulin-like peptides (ILPs) present in sea anemones, particularly focusing on their role in potentially inducing hypoglycemic shock in prey. We identified five [...] Read more.
Sea anemone venom, abundant in protein and peptide toxins, serves primarily for predatory defense and competition. This study delves into the insulin-like peptides (ILPs) present in sea anemones, particularly focusing on their role in potentially inducing hypoglycemic shock in prey. We identified five distinct ILPs in Exaiptasia diaphana, exhibiting varied sequences. Among these, ILP-Ap04 was successfully synthesized using solid phase peptide synthesis (SPPS) to evaluate its hypoglycemic activity. When tested in zebrafish, ILP-Ap04 significantly reduced blood glucose levels in a model of diabetes induced by streptozotocin (STZ) and glucose, concurrently affecting the normal locomotor behavior of zebrafish larvae. Furthermore, molecular docking studies revealed ILP-Ap04’s unique interaction with the human insulin receptor, characterized by a detailed hydrogen-bonding network, which supports a unique mechanism for its hypoglycemic effects. Our findings suggest that sea anemones have evolved sophisticated strategies to activate insulin receptors in vertebrates, providing innovative insights into the design of novel drugs for the treatment of diabetes. Full article
(This article belongs to the Special Issue Synthetic Chemistry in Marine Drug Discovery: Challenges and Opportunities)
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14 pages, 3716 KiB  
Article
Synthesis of the Isodityrosine Moiety of Seongsanamide A–D and Its Derivatives
by Yang Xie, Zhou Xu, Pei Hu, Xiao-Ting Tian, Yi-Hong Lu, Hao-Dong Jiang, Cheng-Gang Huang and Zhi-Cai Shang
Mar. Drugs 2023, 21(7), 373; https://doi.org/10.3390/md21070373 - 25 Jun 2023
Cited by 1 | Viewed by 1302
Abstract
The concise and highly convergent synthesis of the isodityrosine unit of seongsanamide A–D and its derivatives bearing a diaryl ether moiety is described. In this work, the synthetic strategy features palladium-catalyzed C(sp3)–H functionalization and a Cu/ligand-catalyzed coupling reaction. We report a [...] Read more.
The concise and highly convergent synthesis of the isodityrosine unit of seongsanamide A–D and its derivatives bearing a diaryl ether moiety is described. In this work, the synthetic strategy features palladium-catalyzed C(sp3)–H functionalization and a Cu/ligand-catalyzed coupling reaction. We report a practical protocol for the palladium-catalyzed mono-arylation of β-methyl C(sp3)–H of an alanine derivative bearing a 2-thiomethylaniline auxiliary. The reaction is compatible with a variety of functional groups, providing practical access to numerous β-aryl-α-amino acids; these acids can be converted into various tyrosine and dihydroxyphenylalanine (DOPA) derivatives. Then, a CuI/N,N-dimethylglycine-catalyzed arylation of the already synthesized DOPA derivatives with aryl iodides is described for the synthesis of isodityrosine derivatives. Full article
(This article belongs to the Special Issue Synthetic Chemistry in Marine Drug Discovery: Challenges and Opportunities)
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Review

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22 pages, 3208 KiB  
Review
Seaweeds as Source of Bioactive Pigments with Neuroprotective and/or Anti-Neurodegenerative Activities: Astaxanthin and Fucoxanthin
by Estela Guardado Yordi, Amaury Pérez Martínez, Matteo Radice, Laura Scalvenzi, Reinier Abreu-Naranjo, Eugenio Uriarte, Lourdes Santana and Maria Joao Matos
Mar. Drugs 2024, 22(7), 327; https://doi.org/10.3390/md22070327 - 22 Jul 2024
Viewed by 4126
Abstract
The marine kingdom is an important source of a huge variety of scaffolds inspiring the design of new drugs. The complex molecules found in the oceans present a great challenge to organic and medicinal chemists. However, the wide variety of biological activities they [...] Read more.
The marine kingdom is an important source of a huge variety of scaffolds inspiring the design of new drugs. The complex molecules found in the oceans present a great challenge to organic and medicinal chemists. However, the wide variety of biological activities they can display is worth the effort. In this article, we present an overview of different seaweeds as potential sources of bioactive pigments with activity against neurodegenerative diseases, especially due to their neuroprotective effects. Along with a broad introduction to seaweed as a source of bioactive pigments, this review is especially focused on astaxanthin and fucoxanthin as potential neuroprotective and/or anti-neurodegenerative agents. PubMed and SciFinder were used as the main sources to search and select the most relevant scientific articles within the field. Full article
(This article belongs to the Special Issue Synthetic Chemistry in Marine Drug Discovery: Challenges and Opportunities)
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58 pages, 13683 KiB  
Review
Current Status of Indole-Derived Marine Natural Products: Synthetic Approaches and Therapeutic Applications
by Sergio Fernández, Virginia Arnáiz, Daniel Rufo and Yolanda Arroyo
Mar. Drugs 2024, 22(3), 126; https://doi.org/10.3390/md22030126 - 6 Mar 2024
Cited by 5 | Viewed by 3493
Abstract
Indole is a versatile pharmacophore widely distributed in bioactive natural products. This privileged scaffold has been found in a variety of molecules isolated from marine organisms such as algae and sponges. Among these, indole alkaloids represent one of the biggest, most promising family [...] Read more.
Indole is a versatile pharmacophore widely distributed in bioactive natural products. This privileged scaffold has been found in a variety of molecules isolated from marine organisms such as algae and sponges. Among these, indole alkaloids represent one of the biggest, most promising family of compounds, having shown a wide range of pharmacological properties including anti-inflammatory, antiviral, and anticancer activities. The aim of this review is to show the current scenario of marine indole alkaloid derivatives, covering not only the most common chemical structures but also their promising therapeutic applications as well as the new general synthetic routes developed during the last years. Full article
(This article belongs to the Special Issue Synthetic Chemistry in Marine Drug Discovery: Challenges and Opportunities)
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21 pages, 8936 KiB  
Review
Continuous Flow Chemistry: A Novel Technology for the Synthesis of Marine Drugs
by Laura F. Peña, Paula González-Andrés, Lucía G. Parte, Raúl Escribano, Javier Guerra, Asunción Barbero and Enol López
Mar. Drugs 2023, 21(7), 402; https://doi.org/10.3390/md21070402 - 13 Jul 2023
Cited by 4 | Viewed by 5101
Abstract
In this perspective, we showcase the benefits of continuous flow chemistry and photochemistry and how these valuable tools have contributed to the synthesis of organic scaffolds from the marine environment. These technologies have not only facilitated previously described synthetic pathways, but also opened [...] Read more.
In this perspective, we showcase the benefits of continuous flow chemistry and photochemistry and how these valuable tools have contributed to the synthesis of organic scaffolds from the marine environment. These technologies have not only facilitated previously described synthetic pathways, but also opened new opportunities in the preparation of novel organic molecules with remarkable pharmacological properties which can be used in drug discovery programs. Full article
(This article belongs to the Special Issue Synthetic Chemistry in Marine Drug Discovery: Challenges and Opportunities)
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