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Article ; Online: Palladium-Catalyzed Benzodiazepines Synthesis

Michael S. Christodoulou / Egle M. Beccalli / Sabrina Giofrè

Catalysts, Vol 10, Iss 634, p

2020 Volume 634

Abstract: This review is focused on palladium-catalyzed reactions as efficient strategies aimed at the synthesis of different classes of benzodiazepines. Several reaction typologies are reported including hydroamination, amination, C–H arylation, N-arylation, and ... ...

Abstract	This review is focused on palladium-catalyzed reactions as efficient strategies aimed at the synthesis of different classes of benzodiazepines. Several reaction typologies are reported including hydroamination, amination, C–H arylation, N-arylation, and the Buchwald–Hartwig reaction, depending on the different substrates identified as halogenated starting materials (activated substrates) or unactivated unsaturated systems, which then exploit Pd(0)- or Pd(II)-catalytic species. In particular, the use of the domino reactions, as intra- or intermolecular processes, are reported as an efficient and eco-compatible tool to obtain differently functionalized benzodiazepines. Different domino reaction typologies are the carboamination, aminoarylation, aminoacethoxylation, aminohalogenation, and aminoazidation.
Keywords	Pd-catalysis ; benzodiazepine ; cyclization ; domino process ; intramolecular Buchwald–Hartwig ; N-arylation ; Chemical technology ; TP1-1185 ; Chemistry ; QD1-999
Subject code	540
Language	English
Publishing date	2020-06-01T00:00:00Z
Publisher	MDPI AG
Document type	Article ; Online
Database	BASE - Bielefeld Academic Search Engine (life sciences selection)

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Article ; Online: Targeting Ovarian Cancer with Chalcone Derivatives

Elif Merve Aydin / İdil Su Canıtez / Eleonora Colombo / Salvatore Princiotto / Daniele Passarella / Sabrina Dallavalle / Michael S. Christodoulou / Irem Durmaz Şahin

Molecules, Vol 28, Iss 23, p

Cytotoxicity and Apoptosis Induction in HGSOC Cells

2023 Volume 7777

Abstract: Ovarian cancer ranks as the eighth most prevalent form of cancer in women across the globe and stands as the third most frequent gynecological cancer, following cervical and endometrial cancers. Given its resistance to standard chemotherapy and high ... ...

Abstract	Ovarian cancer ranks as the eighth most prevalent form of cancer in women across the globe and stands as the third most frequent gynecological cancer, following cervical and endometrial cancers. Given its resistance to standard chemotherapy and high recurrence rates, there is an urgent imperative to discover novel compounds with potential as chemotherapeutic agents for treating ovarian cancer. Chalcones exhibit a wide array of biological properties, with a particular focus on their anti-cancer activities. In this research, we documented the synthesis and in vitro study of a small library of chalcone derivatives designed for use against high-grade serous ovarian cancer (HGSOC) cell lines, specifically OVCAR-3, OVSAHO, and KURAMOCHI. Our findings revealed that three of these compounds exhibited cytotoxic and anti-proliferative effects against all the tested HGSOC cell lines, achieving IC 50 concentrations lower than 25 µM. Further investigations disclosed that these chalcones prompted an increase in the subG1 phase cell cycle and induced apoptosis in OVCAR-3 cells. In summary, our study underscores the potential of chalcones as promising agents for the treatment of ovarian cancer.
Keywords	chalcones ; ovarian cancer ; OVCAR-3 ; OVSAHO ; KURAMOCHI ; Organic chemistry ; QD241-441
Subject code	610
Language	English
Publishing date	2023-11-01T00:00:00Z
Publisher	MDPI AG
Document type	Article ; Online
Database	BASE - Bielefeld Academic Search Engine (life sciences selection)

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Article ; Online: Asymmetric Hydrogenation of 1-aryl substituted-3,4-Dihydroisoquinolines with Iridium Catalysts Bearing Different Phosphorus-Based Ligands

Giorgio Facchetti / Michael S. Christodoulou / Eleonora Binda / Marco Fusè / Isabella Rimoldi

Catalysts, Vol 10, Iss 914, p

2020 Volume 914

Abstract: Starting from the chiral 5,6,7,8-tetrahydroquinolin-8-ol core, a series of amino-phosphorus-based ligands was realized. The so-obtained amino-phosphine ligand ( L1 ), amino-phosphinite ( L2 ) and amino-phosphite ( L3 ) were evaluated in iridium complexes ...

Abstract	Starting from the chiral 5,6,7,8-tetrahydroquinolin-8-ol core, a series of amino-phosphorus-based ligands was realized. The so-obtained amino-phosphine ligand ( L1 ), amino-phosphinite ( L2 ) and amino-phosphite ( L3 ) were evaluated in iridium complexes together with the heterobiaryl diphosphines tetraMe-BITIOP ( L4 ), Diophep ( L5 ) and L6 and L7 ligands, characterized by mixed chirality. Their catalytic performance in the asymmetric hydrogenation (AH) of the model substrate 6,7-dimethoxy-1-phenyl-3,4-dihydroisoquinoline 1a led us to identify Ir- L4 and Ir- L5 catalysts as the most effective. The application of these catalytic systems to a library of differently substituted 1-aryl-3,4-dihydroisoquinolines afforded the corresponding products with variable enantioselective levels. The 4-nitrophenyl derivative 3b was obtained in a complete conversion and with an excellent 94% e.e. using Ir- L4, and a good 76% e.e. was achieved in the reduction of 2-nitrophenyl derivative 6a using Ir- L5 .
Keywords	atropoisomeric chirality ; chiral diphosphines ; amino phosphine ; imines reduction ; iridium complexes ; Chemical technology ; TP1-1185 ; Chemistry ; QD1-999
Subject code	540
Language	English
Publishing date	2020-08-01T00:00:00Z
Publisher	MDPI AG
Document type	Article ; Online
Database	BASE - Bielefeld Academic Search Engine (life sciences selection)

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Article ; Online: Exploration of Novel Scaffolds Targeting Cytochrome b of Pyricularia oryzae

Cecilia Pinna / Tommaso Laurenzi / Fabio Forlani / Luca Palazzolo / Claire Beatrice Nolan / Michael S. Christodoulou / Paolo Cortesi / Andrea Pinto / Ivano Eberini / Andrea Kunova / Sabrina Dallavalle

International Journal of Molecular Sciences, Vol 24, Iss 2705, p

2023 Volume 2705

Abstract: The fulfilment of the European “Farm to Fork” strategy requires a drastic reduction in the use of “at risk” synthetic pesticides; this exposes vulnerable agricultural sectors—among which is the European risiculture—to the lack of efficient means for the ... ...

Abstract	The fulfilment of the European “Farm to Fork” strategy requires a drastic reduction in the use of “at risk” synthetic pesticides; this exposes vulnerable agricultural sectors—among which is the European risiculture—to the lack of efficient means for the management of devastating diseases, thus endangering food security. Therefore, novel scaffolds need to be identified for the synthesis of new and more environmentally friendly fungicides. In the present work, we employed our previously developed 3D model of P. oryzae cytochrome bc1 (cyt bc1 ) complex to perform a high-throughput virtual screening of two commercially available compound libraries. Three chemotypes were selected, from which a small collection of differently substituted analogues was designed and synthesized. The compounds were tested as inhibitors of the cyt bc1 enzyme function and the mycelium growth of both strobilurin-sensitive (WT) and -resistant (RES) P. oryzae strains. This pipeline has permitted the identification of thirteen compounds active against the RES cyt bc1 and five compounds that inhibited the WT cyt bc1 function while inhibiting the fungal mycelia only minimally. Serendipitously, among the studied compounds we identified a new chemotype that is able to efficiently inhibit the mycelium growth of WT and RES strains by ca. 60%, without inhibiting the cyt bc1 enzymatic function, suggesting a different mechanism of action.
Keywords	high-throughput virtual screening ; rice blast ; antifungals ; cytochrome bc1 enzymatic inhibition ; design and synthesis ; Biology (General) ; QH301-705.5 ; Chemistry ; QD1-999
Subject code	540
Language	English
Publishing date	2023-01-01T00:00:00Z
Publisher	MDPI AG
Document type	Article ; Online
Database	BASE - Bielefeld Academic Search Engine (life sciences selection)

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Article ; Online: Design and Synthesis of Hsp90 Inhibitors with B‐Raf and PDHK1 Multi‐Target Activity

Dr. Luca Pinzi / Dr. Francesca Foschi / Dr. Michael S. Christodoulou / Prof. Daniele Passarella / Prof. Giulio Rastelli

ChemistryOpen, Vol 10, Iss 12, Pp 1177-

2021 Volume 1185

Abstract: Abstract The design of multi‐target ligands has become an innovative approach for the identification of effective therapeutic treatments against complex diseases, such as cancer. Recent studies have demonstrated that the combined inhibition of Hsp90 and ... ...

Abstract	Abstract The design of multi‐target ligands has become an innovative approach for the identification of effective therapeutic treatments against complex diseases, such as cancer. Recent studies have demonstrated that the combined inhibition of Hsp90 and B‐Raf provides synergistic effects against several types of cancers. Moreover, it has been reported that PDHK1, which presents an ATP‐binding pocket similar to that of Hsp90, plays an important role in tumor initiation, maintenance and progression, participating also to the senescence process induced by B‐Raf oncogenic proteins. Based on these premises, the simultaneous inhibition of these targets may provide several benefits for the treatment of cancer. In this work, we set up a design strategy including the assembly and integration of molecular fragments known to be important for binding to the Hsp90, PDHK1 and B‐Raf targets, aided by molecular docking for the selection of a set of compounds potentially able to exert Hsp90‐B‐Raf‐PDHK1 multi‐target activities. The designed compounds were synthesized and experimentally validated in vitro. According to the in vitro assays, compounds 4 a, 4 d and 4 e potently inhibited Hsp90 and moderately inhibited the PDHK1 kinase. Finally, molecular dynamics simulations were performed to provide further insights into the structural basis of their multi‐target activity.
Keywords	docking ; in vitro assays ; molecular dynamics ; multi-target ligands ; polypharmacology ; Chemistry ; QD1-999
Subject code	540
Language	English
Publishing date	2021-12-01T00:00:00Z
Publisher	Wiley-VCH
Document type	Article ; Online
Database	BASE - Bielefeld Academic Search Engine (life sciences selection)

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Article ; Online: Fatty Acids/Tetraphenylethylene Conjugates

Elisa Impresari / Alberto Bossi / Edoardo Mario Lumina / Marco Aldo Ortenzi / Josine Marie Kothuis / Graziella Cappelletti / Daniela Maggioni / Michael S. Christodoulou / Raffaella Bucci / Sara Pellegrino

Frontiers in Chemistry, Vol

Hybrid AIEgens for the Preparation of Peptide-Based Supramolecular Gels

2022 Volume 10

Abstract: Aggregation-induced emissive materials are gaining particular attention in the last decades due to their wide application in different fields, from optical devices to biomedicine. In this work, compounds having these kinds of properties, composed of ... ...

Abstract	Aggregation-induced emissive materials are gaining particular attention in the last decades due to their wide application in different fields, from optical devices to biomedicine. In this work, compounds having these kinds of properties, composed of tetraphenylethylene scaffold combined with fatty acids of different lengths, were synthesized and characterized. These molecules were found able to self-assemble into different supramolecular emissive structures depending on the chemical composition and water content. Furthermore, they were used as N-terminus capping agents in the development of peptide-based materials. The functionalization of a 5-mer laminin-derived peptide led to the obtainment of luminescent fibrillary materials that were not cytotoxic and were able to form supramolecular gels in aqueous environment.
Keywords	aggregation-induced emission (AIE) ; peptide materials ; luminescent materials ; self-assembly ; supramolecular gel ; Chemistry ; QD1-999
Subject code	540
Language	English
Publishing date	2022-08-01T00:00:00Z
Publisher	Frontiers Media S.A.
Document type	Article ; Online
Database	BASE - Bielefeld Academic Search Engine (life sciences selection)

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Article ; Online: Biological Properties of New Chiral 2-Methyl-5,6,7,8-tetrahydroquinolin-8-amine-based Compounds

Giorgio Facchetti / Michael S. Christodoulou / Lina Barragán Mendoza / Federico Cusinato / Lisa Dalla Via / Isabella Rimoldi

Molecules, Vol 25, Iss 5561, p

2020 Volume 5561

Abstract: The synthesis of a small library of 8-substituted 2-methyl-5,6,7,8-tetrahydroquinoline derivatives is presented. All the compounds were tested for their antiproliferative activity in non-cancer human dermal microvascular endothelial cells (HMEC-1) and ... ...

Abstract	The synthesis of a small library of 8-substituted 2-methyl-5,6,7,8-tetrahydroquinoline derivatives is presented. All the compounds were tested for their antiproliferative activity in non-cancer human dermal microvascular endothelial cells (HMEC-1) and cancer cells: human T-lymphocyte cells (CEM), human cervix carcinoma cells (HeLa), human dermal microvascular endothelial cells (HMEC-1), colorectal adenocarcinoma (HT-29), ovarian carcinoma (A2780), and biphasic mesothelioma (MSTO-211H). Compounds 3a , 5a , and 2b , showing significant IC 50 values against the whole panel of the selected cells, were further synthesized and tested as pure enantiomers in order to shed light on how their stereochemistry might impact on the related biological effect. The most active compound ( R )-5a was able to affect cell cycle phases and to induce mitochondrial membrane depolarization and cellular ROS production in A2780 cells.
Keywords	Schiff bases ; ROS production ; mitochondrial damage ; tetrahydroquinolines ; antiproliferative activity ; Organic chemistry ; QD241-441
Language	English
Publishing date	2020-11-01T00:00:00Z
Publisher	MDPI AG
Document type	Article ; Online
Database	BASE - Bielefeld Academic Search Engine (life sciences selection)

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Article ; Online: Vancomycin-Iridium (III) Interaction

Giorgio Facchetti / Sara Pellegrino / Raffaella Bucci / Donatella Nava / Raffaella Gandolfi / Michael S. Christodoulou / Isabella Rimoldi

Molecules, Vol 24, Iss 15, p

An Unexplored Route for Enantioselective Imine Reduction

2019 Volume 2771

Abstract: The chiral structure of antibiotic vancomycin (Van) was exploited as an innovative coordination sphere for the preparation of an IrCp* based hybrid catalysts. We found that Van is able to coordinate iridium (Ir(III)) and the complexation was demonstrated ...

Abstract	The chiral structure of antibiotic vancomycin (Van) was exploited as an innovative coordination sphere for the preparation of an IrCp* based hybrid catalysts. We found that Van is able to coordinate iridium (Ir(III)) and the complexation was demonstrated by several analytical techniques such as MALDI-TOF, UV, Circular dichroism (CD), Raman IR, and NMR. The hybrid system so obtained was employed in the Asymmetric Transfer Hydrogenation (ATH) of cyclic imines allowing to obtain a valuable 61% e.e. ( R ) in the asymmetric reduction of quinaldine 2 . The catalytic system exhibited a saturation kinetics with a calculated efficiency of K cat /K M = 0.688 h −1 mM −1 .
Keywords	glycopeptides ; hybrid catalyst ; asymmetric hydrogen transfer ; Organic chemistry ; QD241-441
Language	English
Publishing date	2019-07-01T00:00:00Z
Publisher	MDPI AG
Document type	Article ; Online
Database	BASE - Bielefeld Academic Search Engine (life sciences selection)

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Article ; Online: Enzymatic Kinetic Resolution of 2-Piperidineethanol for the Enantioselective Targeted and Diversity Oriented Synthesis

Dario Perdicchia / Michael S. Christodoulou / Gaia Fumagalli / Francesco Calogero / Cristina Marucci / Daniele Passarella

International Journal of Molecular Sciences, Vol 17, Iss 1, p

2015 Volume 17

Abstract: 2-Piperidineethanol (1) and its corresponding N-protected aldehyde (2) were used for the synthesis of several natural and synthetic compounds. The existence of a stereocenter at position 2 of the piperidine skeleton and the presence of an easily- ... ...

Abstract	2-Piperidineethanol (1) and its corresponding N-protected aldehyde (2) were used for the synthesis of several natural and synthetic compounds. The existence of a stereocenter at position 2 of the piperidine skeleton and the presence of an easily-functionalized group, such as the alcohol, set 1 as a valuable starting material for enantioselective synthesis. Herein, are presented both synthetic and enzymatic methods for the resolution of the racemic 1, as well as an overview of synthesized natural products starting from the enantiopure 1.
Keywords	2-piperidineethanol ; piperidine alkaloids ; enzymatic resolution ; alkaloid synthesis ; Chemistry ; QD1-999 ; Science ; Q
Language	English
Publishing date	2015-12-01T00:00:00Z
Publisher	MDPI AG
Document type	Article ; Online
Database	BASE - Bielefeld Academic Search Engine (life sciences selection)

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Article: Farinose alpine Primula species: Phytochemical and morphological investigations

Colombo, Paola S / Daniele Passarella / Gelsomina Fico / Graziella Rodondi / Guido Flamini / Michael S. Christodoulou / Sara Vitalini

Phytochemistry. 2014 Feb., v. 98

2014

Abstract: This work investigated the epicuticular and tissue flavonoids, the volatiles and the glandular trichome structure of the leaves of four species of Primula L. that grow in the Italian Eastern Alps. Primula albenensis Banfi and Ferlinghetti, P. auricula L., ...

Abstract	This work investigated the epicuticular and tissue flavonoids, the volatiles and the glandular trichome structure of the leaves of four species of Primula L. that grow in the Italian Eastern Alps. Primula albenensis Banfi and Ferlinghetti, P. auricula L., P. farinosa L., P. halleri Gmelin produce farinose exudates that are deposited on the leaf surface as filamentous crystalloids.In addition to compounds already known, a new flavone, the 3,5-dihydroxyflavone, was isolated from the acetone extract of leaf farinas and three new flavonol glycosides, 3′-O-(β-galactopyranosyl)-2′-hydroxyflavone, isorhamnetin 3-O-α-rhamnopyranosyl-(1→3)-O-[α-rhamnopyranosyl-(1→6)]-O-β-galactopyranoside, quercetin 3-O-α-rhamnopyranosyl-(1→3)-O-[α-rhamnopyranosyl-(1→6)]-O-β-galactopyranoside, were isolated from the MeOH extract of the leaves. All the structures were elucidated on the basis of their 1H and 13C NMR data and 2D NMR techniques, as well as on HPLC–MS. The leaf-volatiles emitted by these Primula species were mainly sesquiterpene hydrocarbons, with the exception of P. albenensis, which produced almost exclusively a non-terpene derivative; P. halleri flowers were also examined and the volatiles emitted by the flower parts (corolla and calyx) were compared with the corresponding leaves.
Keywords	acetone ; calyx ; corolla ; glycosides ; high performance liquid chromatography ; isorhamnetin ; leaf extracts ; leaves ; mass spectrometry ; methanol ; nuclear magnetic resonance spectroscopy ; Primula ; quercetin ; sesquiterpenoids ; trichomes ; Alps region ; Italy
Language	English
Dates of publication	2014-02
Size	p. 151-159.
Publishing place	Elsevier Ltd
Document type	Article
ZDB-ID	208884-8
ISSN	1873-3700 ; 0031-9422
ISSN (online)	1873-3700
ISSN	0031-9422
DOI	10.1016/j.phytochem.2013.11.018
Database	NAL-Catalogue (AGRICOLA)

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