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Bioactive Compounds: Design, Synthesis and Biological Evaluation

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

Deadline for manuscript submissions: closed (15 December 2022) | Viewed by 23641

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Special Issue Editors

Dr. Samuel Martins Silvestre

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CICS—Health Sciences Research Center, Faculty of Health Sciences, University of Beira Interior, 6201-001 Covilhã, Portugal
Interests: design of bioactive compounds; chemical synthesis; biological evaluation; compounds with medicinal and pharmaceutical interests
Special Issues, Collections and Topics in MDPI journals

Prof. Dr. Paulo Jorge da Silva Almeida

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CICS-Health Sciences Research Center, Faculty of Sciences, University of Beira Interior, Covilhã, Portugal
Interests: chemical synthesis; development of new synthetic processes; heterocyclic compounds; compounds with medicinal and pharmaceutical interests
Special Issues, Collections and Topics in MDPI journals

Dr. Renato Emanuel Felix Boto

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Guest Editor

CICS-Health Sciences Research Center, Faculty of Health Sciences, University of Beira Interior, Covilhã, Portugal
Interests: organic synthesis; synthesis of new organic compounds with medicinal and pharmaceutical interests
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Bioactive compounds are molecules that have an effect on a living organism, tissue or cell and can therefore have an influence on health. These compounds can be synthetically produced and/or obtained from natural sources, mainly from secondary metabolites of plants, animals, or other types of living organisms. Some representative compounds are carotenoids, polyphenols, fatty acids, steroids, flavonoids, and polysaccharides.

Modern drug discovery efforts are based on the discovery and development of lead compounds, which can be obtained using different strategies, such as biological modulation of diseases with biomolecules extracted from natural products, biological screening of small synthetic molecules as ligands using compound libraries, or even in silico approaches.

This Special Issue aims to collect recent advances regarding the design, synthesis, and biological evaluation of bioactive compounds that can lead to the development of natural or synthetic small active molecules looking for promising drugs to prevent or threaten human illnesses.

Therefore, we kindly invite researchers to contribute manuscripts focusing not only on the design and total or semi-synthesis of bioactive compounds and relevant synthetic intermediates but also on their in vitro and in vivo biological evaluation.

Dr. Samuel Martins Silvestre
Prof. Dr. Paulo Jorge da Silva Almeida
Dr. Renato Emanuel Felix Boto
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. 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

Bioactive
Design
Synthesis
Biological evaluation
In silico evaluation

Published Papers (12 papers)

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20 pages, 5679 KiB

Open AccessArticle

3-Arylidene-2-oxindoles as Potent NRH:Quinone Oxidoreductase 2 Inhibitors

by Natalia A. Lozinskaya, Elena N. Bezsonova, Meriam Dubar, Daria D. Melekhina, Daniil R. Bazanov, Alexander S. Bunev, Olga B. Grigor’eva, Vladlen G. Klochkov, Elena V. Sokolova, Denis A. Babkov, Alexander A. Spasov and Sergey E. Sosonyuk

Molecules 2023, 28(3), 1174; https://doi.org/10.3390/molecules28031174 - 25 Jan 2023

Cited by 3 | Viewed by 1645

Abstract

The enzyme NRH:quinone oxidoreductase 2 (NQO2) plays an important role in the pathogenesis of various diseases such as neurodegenerative disorders, malaria, glaucoma, COVID-19 and cancer. NQO2 expression is known to be increased in some cancer cell lines. Since 3-arylidene-2-oxindoles are widely used in the design of new anticancer drugs, such as kinase inhibitors, it was interesting to study whether such structures have additional activity towards NQO2. Herein, we report the synthesis and study of 3-arylidene-2-oxindoles as novel NRH:quinone oxidoreductase inhibitors. It was demonstrated that oxindoles with 6-membered aryls in the arylidene moiety were obtained predominantly as E-isomers while for some 5-membered aryls, the Z-isomers prevailed. The most active compounds inhibited NQO2 with an IC₅₀ of 0.368 µM. The presence of a double bond in the oxindoles was crucial for NQO2 inhibition activity. There was no correlation between NQO2 inhibition activity of the synthesized compounds and their cytotoxic effect on the A549 cell line. Full article

(This article belongs to the Special Issue Bioactive Compounds: Design, Synthesis and Biological Evaluation)

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15 pages, 5053 KiB

Open AccessArticle

Synthesis, Biological Evaluation and Molecular Modeling Studies of Naphthoquinone Sulfonamides and Sulfonate Ester Derivatives as P2X7 Inhibitors

by Paulo Anastácio Furtado Pacheco, Daniel Tadeu Gomes Gonzaga, Natalia Lidmar von Ranke, Carlos Rangel Rodrigues, David Rodrigues da Rocha, Fernando de Carvalho da Silva, Vitor Francisco Ferreira and Robson Xavier Faria

Molecules 2023, 28(2), 590; https://doi.org/10.3390/molecules28020590 - 06 Jan 2023

Cited by 2 | Viewed by 1519

Abstract

ATP acts in the extracellular environment as an important signal, activating a family of receptors called purinergic receptors. In recent years, interest in the potential therapeutics of purinergic components, including agonists and antagonists of receptors, has increased. Currently, many observations have indicated that ATP acts as an important mediator of inflammatory responses and, when found in high concentrations in the extracellular space, is related to the activation of the P2X7 purinergic receptor. In this sense, the search for new inhibitors for this receptor has attracted a great deal of attention in recent years. Sulfonamide derivatives have been reported to be potent inhibitors of P2X receptors. In this study, ten naphthoquinone sulfonamide derivatives and five naphthoquinone sulfonate ester derivatives were tested for their inhibitory activity on the P2X7 receptor expressed in peritoneal macrophages. Some compounds showed promising results, displaying IC₅₀ values lower than that of A740003. Molecular docking and dynamic studies also indicated that the active compounds bind to an allosteric site on P2X7R. The binding free energy indicates that sulfonamides have an affinity for the P2X7 receptor similar to A740003. Therefore, the compounds studied herein present potential P2X7R inhibition. Full article

(This article belongs to the Special Issue Bioactive Compounds: Design, Synthesis and Biological Evaluation)

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13 pages, 4076 KiB

Open AccessArticle

Hepatoprotective Effect of a New FFAR1 Agonist—N-Alkylated Isobornylamine

by Darya Pon`kina, Sergey Kuranov, Mikhail Khvostov, Nataliya Zhukova, Yulia Meshkova, Mariya Marenina, Olga Luzina, Tatyana Tolstikova and Nariman Salakhutdinov

Molecules 2023, 28(1), 396; https://doi.org/10.3390/molecules28010396 - 03 Jan 2023

Cited by 3 | Viewed by 1666

Abstract

Free fatty acid receptor-1 (FFAR1) is one of the possible therapeutic targets in the search for new hepatoprotective drugs. FFAR1 agonists were found to have hypolipidemic, antifibrotic, anti-inflammatory, antiproliferative and antioxidant effects in addition to hypoglycemic action. In this work, we conducted a study of the hepatoprotective effect of the compound QS-528 (previously discovered as an agonist of FFAR1) at doses of 60, 90, 120 and 150 mg/kg on carbon tetrachloride (CCl₄)-induced liver injury. At the end of the experiment, a biochemical blood assay demonstrated that the introduction of QS-528 dose-dependently reduces the levels of liver enzymes (AST, ALT and ALKP). Histological and morphometric studies of animals’ livers treated with QS-528 at doses of 120 and 150 mg/kg showed a decrease in degenerative/necrotic changes in hepatocytes and an increase in the regenerative activity of the liver. In addition, no toxicity at a single oral dose of 1000 mg/kg and an increase in HepG2 cell viability in vitro were found. Thus, the compound QS-528 was found to exhibit a hepatoprotective effect against CCl₄-induced toxic liver damage. Full article

(This article belongs to the Special Issue Bioactive Compounds: Design, Synthesis and Biological Evaluation)

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12 pages, 983 KiB

Open AccessArticle

Controlling Pepper Mild Mottle Virus (PMMoV) Infection in Pepper Seedlings by Use of Chemically Synthetic Silver Nanoparticles

by Esam K. F. Elbeshehy, Wael M. Hassan and Areej A. Baeshen

Molecules 2023, 28(1), 139; https://doi.org/10.3390/molecules28010139 - 24 Dec 2022

Cited by 4 | Viewed by 1872

Abstract

We investigated the roles of different concentrations of chemical synthetic spherical silver nanoparticles (AgNPs) in protecting pepper seedlings of the Mecca region, which were naturally and artificially infected by the pepper mild mottle virus (PMMoV). The virus shows many infection symptoms, including pepper leaf deformation with filiform leaves and severe mosaic symptoms. Our study focused on the antiviral activity of different concentrations of spherical nanoparticles in controlling PMMoV infecting pepper seedlings. PMMoV identification was confirmed via DAS-ELISA using the following antiserum: PMMoV, cucumber mosaic virus (CMV), tobacco mosaic virus (TMV), tomato mosaic virus (ToMV), potato virus Y (PVY), and tomato spotted wilt virus (TSWV). The presence of PMMoV was confirmed using electron microscopy and reverse transcription polymerase chain reaction (RT-PCR). We evaluated the effects of exogenously applied different concentrations of AgNPs on CMV infection rate, infection severity, virus concentration, and the concentrations of photosynthetic pigments chlorophyll a, chlorophyll b, carotenoid content, phenolic compounds, and protein components in virus-infected plant cells that were treated with three different concentration of nanoparticles (200, 300, and 400 µg/L) compared to the positive and negative control. Full article

(This article belongs to the Special Issue Bioactive Compounds: Design, Synthesis and Biological Evaluation)

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22 pages, 7051 KiB

Open AccessArticle

Synthesis, Conformational Analysis and Evaluation of the 2-aryl-4-(4-bromo-2-hydroxyphenyl)benzo[1,5]thiazepines as Potential α-Glucosidase and/or α-Amylase Inhibitors

by Jackson K. Nkoana, Marole M. Maluleka, Malose J. Mphahlele, Richard M. Mampa and Yee Siew Choong

Molecules 2022, 27(20), 6935; https://doi.org/10.3390/molecules27206935 - 16 Oct 2022

Cited by 2 | Viewed by 1280

Abstract

The ambident electrophilic character of the 5-bromo-2-hydroxychalcones and the binucleophilic nature of 2-aminothiophenol were exploited to construct the 2-aryl-4-(4-bromo-2-hydroxyphenyl)benzo[1,5]thiazepines. The structures and conformation of these 2-aryl-4-(4-bromo-2-hydroxyphenyl)benzo[1,5]thiazepines were established with the use of spectroscopic techniques complemented with a single crystal X-ray diffraction method. Both ¹H-NMR and IR spectroscopic techniques confirmed participation of the hydroxyl group in the intramolecular hydrogen-bonding interaction with a nitrogen atom. SC-XRD confirmed the presence of a six-membered intramolecularly hydrogen-bonded pseudo-aromatic ring, which was corroborated by the DFT method on 2b as a representative example in the gas phase. Compounds 2a (Ar = -C₆H₅), 2c (Ar = -C₆H₄(4-Cl)) and 2f (Ar = -C₆H₄(4-CH(CH₃)₂) exhibited increased inhibitory activity against α-glucosidase compared to acarbose (IC₅₀ = 7.56 ± 0.42 µM), with IC₅₀ values of 6.70 ± 0.15 µM, 2.69 ± 0.27 µM and 6.54 ± 0.11 µM, respectively. Compound 2f, which exhibited increased activity against α-glucosidase, also exhibited a significant inhibitory effect against α-amylase (IC₅₀ = 9.71 ± 0.50 µM). The results of some computational approaches on aspects such as noncovalent interactions, calculated binding energies for α-glucosidase and α-amylase, ADME (absorption, distribution, metabolism and excretion) and bioavailability properties, gastrointestinal absorption and blood–brain barrier permeability are also presented. Full article

(This article belongs to the Special Issue Bioactive Compounds: Design, Synthesis and Biological Evaluation)

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25 pages, 3072 KiB

Open AccessFeature PaperArticle

An Insight into Symmetrical Cyanine Dyes as Promising Selective Antiproliferative Agents in Caco-2 Colorectal Cancer Cells

by João L. Serrano, Ana Maia, Adriana O. Santos, Eurico Lima, Lucinda V. Reis, Maria J. Nunes, Renato E. F. Boto, Samuel Silvestre and Paulo Almeida

Molecules 2022, 27(18), 5779; https://doi.org/10.3390/molecules27185779 - 07 Sep 2022

Cited by 6 | Viewed by 1889

Abstract

Cancer remains one of the diseases with the highest worldwide incidence. Several cytotoxic approaches have been used over the years to overcome this public health threat, such as chemotherapy, radiotherapy, and photodynamic therapy (PDT). Cyanine dyes are a class of compounds that have been extensively studied as PDT sensitisers; nevertheless, their antiproliferative potential in the absence of a light source has been scarcely explored. Herein, the synthesis of eighteen symmetric mono-, tri-, and heptamethine cyanine dyes and their evaluation as potential anticancer agents is described. The influences of the heterocyclic nature, counterion, and methine chain length on the antiproliferative effects and selectivities were analysed, and relevant structure–activity relationship data were gathered. The impact of light on the cytotoxic activity of the most promising dye was also assessed and discussed. Most of the monomethine and trimethine cyanine dyes under study demonstrated a high antiproliferative effect on human tumour cell lines of colorectal (Caco-2), breast (MCF-7), and prostate (PC-3) cancer at the initial screening (10 µM). However, concentration–viability curves showed higher potency and selectivity for the Caco-2 cell line. A monomethine cyanine dye derived from benzoxazole was the most promising compound (IC₅₀ for Caco-2 = 0.67 µM and a selectivity index of 20.9 for Caco-2 versus normal human dermal fibroblasts (NHDF)) and led to Caco-2 cell cycle arrest at the G0/G1 phase. Complementary in silico studies predicted good intestinal absorption and oral bioavailability for this cyanine dye. Full article

(This article belongs to the Special Issue Bioactive Compounds: Design, Synthesis and Biological Evaluation)

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19 pages, 5532 KiB

Open AccessArticle

Novel Lysosome-Targeting Fluorescence Off-On Photosensitizer for Near-Infrared Hypoxia Imaging and Photodynamic Therapy In Vitro and In Vivo

by Shangli Ding, Mingyan Yang, Jiajia Lv, Hongyu Li, Gang Wei, Jie Gao and Zeli Yuan

Molecules 2022, 27(11), 3457; https://doi.org/10.3390/molecules27113457 - 27 May 2022

Cited by 8 | Viewed by 1953

Abstract

Photodynamic therapy (PDT) has emerged as a new antitumor modality. Hypoxia, a vital characteristic of solid tumors, can be explored to stimulate the fluorescence response of photosensitizers (PSs). Considering the characteristics of PDT, the targeting of organelles employing PS would enhance antitumor effects. A new multifunctional cyanine-based PS (CLN) comprising morpholine and nitrobenzene groups was prepared and characterized. It generated fluorescence in the near-infrared (NIR) region in the presence of sodium dithionite (Na₂S₂O₄) and nitroreductase (NTR). The response mechanism of CLN was well investigated, thus revealing that its obtained reduction product was CLNH. The obtained fluorescence and singlet oxygen quantum yield of CLNH were 8.65% and 1.60%, respectively. Additionally, the selective experiment for substrates indicated that CLN exhibited a selective response to NTR. Thus, CLN fluorescence could be selectively switched on and its fluorescence intensity increased, following a prolonged stay in hypoxic cells. Furthermore, fluorescence colocalization demonstrated that CLN could effectively target lysosomes. CLN could generate reactive oxygen species and kill tumor cells (IC50 for 4T1 cells was 7.4 μM under a hypoxic condition), following its response to NTR. NIR imaging and targeted PDT were finally applied in vivo. Full article

(This article belongs to the Special Issue Bioactive Compounds: Design, Synthesis and Biological Evaluation)

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17 pages, 780 KiB

Open AccessArticle

New Derivatives of 5-Substituted Uracils: Potential Agents with a Wide Spectrum of Biological Activity

by Vasily A. Kezin, Elena S. Matyugina, Mikhail S. Novikov, Alexander O. Chizhov, Robert Snoeck, Graciela Andrei, Sergei N. Kochetkov and Anastasia L. Khandazhinskaya

Molecules 2022, 27(9), 2866; https://doi.org/10.3390/molecules27092866 - 30 Apr 2022

Cited by 8 | Viewed by 1755

Abstract

Pyrimidine nucleoside analogues are widely used to treat infections caused by the human immunodeficiency virus (HIV) and DNA viruses from the herpes family. It has been shown that 5-substituted uracil derivatives can inhibit HIV-1, herpes family viruses, mycobacteria and other pathogens through various mechanisms. Among the 5-substituted pyrimidine nucleosides, there are not only the classical nucleoside inhibitors of the herpes family viruses, 2′-deoxy-5-iodocytidine and 5-bromovinyl-2′-deoxyuridine, but also derivatives of 1-(benzyl)-5-(phenylamino)uracil, which proved to be non-nucleoside inhibitors of HIV-1 and EBV. It made this modification of nucleoside analogues very promising in connection with the emergence of new viruses and the crisis of drug resistance when the task of creating effective antiviral agents of new types that act on other targets or exhibit activity by other mechanisms is very urgent. In this paper, we present the design, synthesis and primary screening of the biological activity of new nucleoside analogues, namely, 5′-norcarbocyclic derivatives of substituted 5-arylamino- and 5-aryloxyuracils, against RNA viruses. Full article

(This article belongs to the Special Issue Bioactive Compounds: Design, Synthesis and Biological Evaluation)

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21 pages, 3698 KiB

Open AccessArticle

A Sub-Micromolar MraY_AA Inhibitor with an Aminoribosyl Uridine Structure and a (S,S)-Tartaric Diamide: Synthesis, Biological Evaluation and Molecular Modeling

by Martin Oliver, Laurent Le Corre, Mélanie Poinsot, Michaël Bosco, Hongwei Wan, Ana Amoroso, Bernard Joris, Ahmed Bouhss, Sandrine Calvet-Vitale and Christine Gravier-Pelletier

Molecules 2022, 27(6), 1769; https://doi.org/10.3390/molecules27061769 - 08 Mar 2022

Cited by 1 | Viewed by 1761

Abstract

New inhibitors of the bacterial tranferase MraY are described. Their structure is based on an aminoribosyl uridine scaffold, which is known to be important for the biological activity of natural MraY inhibitors. A decyl alkyl chain was introduced onto this scaffold through various linkers. The synthesized compounds were tested against the MraY_AA transferase activity, and the most active compound with an original (S,S)-tartaric diamide linker inhibits MraY activity with an IC₅₀ equal to 0.37 µM. Their antibacterial activity was also evaluated on a panel of Gram-positive and Gram-negative strains; however, the compounds showed no antibacterial activity. Docking and molecular dynamics studies revealed that this new linker established two stabilizing key interactions with N190 and H325, as observed for the highly potent inhibitors carbacaprazamycin, muraymycin D2 and tunicamycin. Full article

(This article belongs to the Special Issue Bioactive Compounds: Design, Synthesis and Biological Evaluation)

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11 pages, 5625 KiB

Open AccessArticle

In Vivo Antistress Effects of Synthetic Flavonoids in Mice: Behavioral and Biochemical Approach

by Mehreen Ghias, Syed Wadood Ali Shah, Fakhria A. Al-Joufi, Mohammad Shoaib, Syed Muhammad Mukarram Shah, Muhammad Naeem Ahmed and Muhammad Zahoor

Molecules 2022, 27(4), 1402; https://doi.org/10.3390/molecules27041402 - 18 Feb 2022

Cited by 3 | Viewed by 2034

Abstract

Natural flavonoids, in addition to some of their synthetic derivatives, are recognized for their remarkable medicinal properties. The present study was designed to investigate the in vitro antioxidant and in vivo antistress effect of synthetic flavonoids (flavones and flavonols) in mice, where stress was induced by injecting acetic acid and physically through swimming immobilization. Among the synthesized flavones (F1–F6) and flavonols (OF1–OF6), the mono para substituted methoxy containing F3 and OF3 exhibited maximum scavenging potential against DPPH (2,2-diphenyl-1-picrylhydrazyl) with IC₅₀ of 31.46 ± 1.46 μg/mL and 25.54 ± 1.21 μg/mL, respectively. Minimum antioxidant potential was observed for F6 and OF6 with IC₅₀ values of 174.24 ± 2.71 μg/mL and 122.33 ± 1.98 μg/mL, respectively, in comparison with tocopherol. The ABTS scavenging activity of all the synthesized flavones and flavonols were significantly higher than observed with DPPH assay, indicating their potency as good antioxidants and the effectiveness of ABTS (2,2′-azino-bis(3-ethylbenzothiazoline-6-sulfonate) assay in evaluating antioxidant potentials of chemical substances. The flavonoids-treated animals showed a significant (* p < 0.05, ** p < 0.01 and *** p < 0.001, n = 8) reduction in the number of writhes and an increase in swimming endurance time. Stressful conditions changed plasma glucose, cholesterol and triglyceride levels, which were used as markers when evaluating stress in animal models. The level of these markers was nearly brought to normal when pre-treated with flavones and flavonols (10 mg/kg) for fifteen days in experimental animals. These compounds also considerably reduced the levels of lipid peroxidation (TBARS: Thiobarbituric acid reactive substances), which was significant (* p < 0.05, ** p < 0.01 and *** p < 0.001, n = 8) compared to the control group. A significant rise in the level of catalase and SOD (super oxide dismutase) was also observed in the treated groups. Diazepam (2 mg/kg) was used as the standard drug. Additionally, the flavonoids markedly altered the weight of the adrenal glands, spleen and brain in stress-induced mice. The findings of the study suggest that these flavonoids could be used as a remedy for stress and are capable of ameliorating diverse physiological and biochemical alterations associated with stressful conditions. However, further experiments are needed to confirm the observed potentials in other animal models, especially in those with a closer resemblance to humans. Toxicological evaluations are also equally important. Full article

(This article belongs to the Special Issue Bioactive Compounds: Design, Synthesis and Biological Evaluation)

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Review

Jump to: Research

24 pages, 8595 KiB

Open AccessReview

Anticancer Activity of Natural and Semi-Synthetic Drimane and Coloratane Sesquiterpenoids

by Lorenz Beckmann, Uta Sandy Tretbar, Reni Kitte and Maik Tretbar

Molecules 2022, 27(8), 2501; https://doi.org/10.3390/molecules27082501 - 13 Apr 2022

Cited by 4 | Viewed by 2557

Abstract

Drimane and coloratane sesquiterpenoids are present in several plants, microorganisms, and marine life. Because of their cytotoxic activity, these sesquiterpenoids have received increasing attention as a source for new anticancer drugs and pharmacophores. Natural drimanes and coloratanes, as well as their semi-synthetic derivatives, showed promising results against cancer cell lines with in vitro activities in the low micro- and nanomolar range. Despite their high potential as novel anticancer agents, the mode of action and structure–activity relationships of drimanes and coloratanes have not been completely enlightened nor systematically reviewed. Our review aims to give an overview of known structures and derivatizations of this class of sesquiterpenoids, as well as their activity against cancer cells and potential modes-of-action. The cytotoxic activities of about 40 natural and 25 semi-synthetic drimanes and coloratanes are discussed. In addition to that, we give a summary about the clinical significance of drimane and coloratane sesquiterpenoids. Full article

(This article belongs to the Special Issue Bioactive Compounds: Design, Synthesis and Biological Evaluation)

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16 pages, 1768 KiB

Open AccessReview

Recent Advances in Divergent Synthetic Strategies for Indole-Based Natural Product Libraries

by Taegwan Kim, Min Woo Ha and Jonghoon Kim

Molecules 2022, 27(7), 2171; https://doi.org/10.3390/molecules27072171 - 27 Mar 2022

Cited by 7 | Viewed by 2403

Abstract

Considering the potential bioactivities of natural product and natural product-like compounds with highly complex and diverse structures, the screening of collections and small-molecule libraries for high-throughput screening (HTS) and high-content screening (HCS) has emerged as a powerful tool in the development of novel therapeutic agents. Herein, we review the recent advances in divergent synthetic approaches such as complexity-to-diversity (Ctd) and biomimetic strategies for the generation of structurally complex and diverse indole-based natural product and natural product-like small-molecule libraries. Full article

(This article belongs to the Special Issue Bioactive Compounds: Design, Synthesis and Biological Evaluation)

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