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1. One-Pot Synthesis of Benzopyran-4-ones with Cancer Preventive and Therapeutic Potential

Author

Clarissa Gerhäuser, Lidia Brodziak-Jarosz, Stéphanie Philippot, Jana Panning, Barbora Orlikova, Tobias P. Dick, Tzvetomira Tzanova, Marc Diederich, Filipe A. Almeida Paz, Diana C. G. A. Pinto, Oualid Talhi, Denyse Bagrel, Claus Jacob, Gilbert Kirsch, Clemens Zwergel, Artur M. S. Silva, Universidade de Aveiro, Centre de Recherche Scientifique et Technique en Analyses Physico-Chimiques (CRAPC), German Cancer Research Center - Deutsches Krebsforschungszentrum [Heidelberg] (DKFZ), Saarland University [Saarbrücken], Hôpital Kirchberg, Hôpital Kirchberg [Luxembourg], Structure et Réactivité des Systèmes Moléculaires Complexes (SRSMC), Université de Lorraine (UL)-Centre National de la Recherche Scientifique (CNRS)-Institut de Chimie du CNRS (INC), Seoul National University [Seoul] (SNU), and ABC Platform

Subjects
0301 basic medicine, Antioxidant, Stereochemistry, Decarboxylation, DPPH, medicine.medical_treatment, Medicinal chemistry, CARCINOMA-CELLS, 01 natural sciences, Antioxidants, 03 medical and health sciences, chemistry.chemical_compound, Cascade reaction, Michael addition, medicine, [CHIM]Chemical Sciences, CYTOTOXICITY, Physical and Theoretical Chemistry, 2-STYRYLCHROMONES, AGENTS, Drug discovery, 010405 organic chemistry, Chemistry, DERIVATIVES, Organic Chemistry, FLAVONOIDS, anticancer agents, antioxidants, domino reactions, drug discovery, medicinal chemistry, michael addition, oxygen heterocycles, organic chemistry, physical and theoretical chemistry, CHROMONES, 3. Good health, 0104 chemical sciences, Benzopyran, 030104 developmental biology, Oxygen heterocycles, Anticancer agents, SCAVENGERS, Chromone, Michael reaction, Domino reactions, Trolox, ANTIOXIDANT ACTIVITY, XANTHOHUMOL
Abstract

International audience; A one-pot synthesis of novel benzopyran-4-ones is described. In a tandem reaction, organobase-catalysed Michael addition of (RCOCH2COR2)-C-1 on chromone-3-carboxylic acid led to decarboxylation and pyran-4-one ring opening of the latter. This was followed by chromone- and/or chromanone ring closure of the resulting Michael adducts when R-1 is an ortho-hydroxyaryl group. Antioxidant testing of 14 derivatives identified strong antiradical properties of chromanones 3o-r (2.1-3.1 mu mol Trolox equiv./mu mol compound in the DPPH assay). Chromanones 3p and 3r and 2-styrylchromone 3k were also most potent in inducing the cytoprotective Keap1-Nrf2 signalling pathway in a reporter gene assay (fivefold induction at concentrations

Published
2016
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2. Bis(4-hydroxy-2H-chromen-2-one): synthesis and effects on leukemic cell lines proliferation and NF-κB regulation

Author

Oualid Talhi, Diana Pinto, Claus Jacob, Artur M. S. Silva, José A. Fernandes, Jana Panning, Filipe A. Almeida Paz, Marc Diederich, and Michael Schnekenburger

Subjects
EXPRESSION, Models, Molecular, Cell Survival, Clinical Biochemistry, INHIBITION, Pharmaceutical Science, Antineoplastic Agents, Biochemistry, Jurkat cells, Peripheral blood mononuclear cell, ACTIVATION, chemistry.chemical_compound, Structure-Activity Relationship, Drug Discovery, Gene expression, Tumor Cells, Cultured, Humans, Molecular Biology, Incubation, IC50, Cell Proliferation, Dose-Response Relationship, Drug, Molecular Structure, Chemistry, Organic Chemistry, Cell Cycle, DEATH, NF-kappa B, PATHWAYS, NF-κB, K562 CELLS, CANCER, Molecular biology, APOPTOSIS, 3. Good health, Blot, DIFFERENTIATION, Cell culture, Chromones, Molecular Medicine, Drug Screening Assays, Antitumor, K562 Cells, CURCUMIN
Abstract

Synthesis of the bis-4-hydroxycoumarin-type compound, 3,3'-[3-(2-hydroxyphenyl)-3-oxopropane-1,1-diyl] bis(4-hydroxy-2H-chromen-2-one), was performed by two alternative pathways, either involving a basic organocatalyzed 1,4-conjugate addition tandem reaction of 4-hydroxycoumarin on chromone-3-carboxylic acid, or a double condensation of 4-hydroxycoumarin on omega-formyl-2'-hydroxyacetophenone. The anti-proliferative effects of the bis-4-hydroxycoumarin-type compound on human K-562 (chronic myeloid leukaemia) and JURKAT (acute T-cell leukaemia) cell lines using trypan blue staining, as well as its involvement in nuclear factor-kappa B (NF-kappa B) regulation analyzed by luciferase reporter gene assay, gene expression analysis and western blots were analysed. This compound inhibited TNF alpha-induced NF-kappa B activation in K-562 (IC50 17.5 mu M) and JURKAT (IC50 19.0 mu M) cell lines, after 8 h of incubation. Interestingly, it exerted mainly cytostatic effects at low doses on both cell lines tested, whereas it decreased JURKAT cell viability starting at 50 mu M from 24 h of treatment. Importantly, it did not affect the viability of peripheral blood mononuclear cells (PBMCs) from healthy donors, even at concentrations above 100 mu M. (C) 2014 Elsevier Ltd. All rights reserved.

Published
2014

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