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New, highly potent and non-toxic, chromone inhibitors of the human breast cancer resistance protein ABCG2.

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Breast cancer resistance protein (BCRP/ABCG2) is one of the major transporters involved in the efflux of anticancer compounds, contributing to multidrug resistance (MDR). Inhibition of ABCG2-mediated transport is then considered a promising strategy for overcoming MDR in tumors. We recently

Synthesis and evaluation of indole, pyrazole, chromone and pyrimidine based conjugates for tumor growth inhibitory activities--development of highly efficacious cytotoxic agents.

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Based upon the lead compounds 10 and 11, a number of conjugates were synthesized by the combination of chromone-pyrimidine, chromone-indolinone, chromone-pyrazole, indole-pyrimidine, indole-indolinone and indole-pyrazole moieties. Evaluation of these compounds for tumor growth inhibitory activities

Ferrocenyl and dicobalt hexacarbonyl chromones--new organometallics inducing oxidative stress and arresting human cancer cells in G2/M phase.

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The straightforward syntheses of four new ferrocenyl and dicobalt hexacarbonyl chromones are presented. The redox behavior of the novel metallo-chromones has been examined by cyclic voltammetry (CV), revealing a reversible behavior of the ferrocenyl groups, while the dicobalt hexacarbonyl

Anti-proliferative Effects of Chromones: Potent Derivatives Affecting Cell Growth and Apoptosis in Breast, Bone-marrow and Cervical Cancer Cells.

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Bachground: Previously, we have identified 3,3'-carbonyl-bis(chromones) (1a-h, 5e) and 3-(5-(benzylideneamino)thiozol-3-yl)-2H-chromen-2-ones (7a-j) as potent inhibitors of tissue non-specific alkaline phosphatase (TNAP). The present study was designed to investigate the cytotoxic and

Ambient ionization mass spectrometry imaging of rohitukine, a chromone anti-cancer alkaloid, during seed development in Dysoxylum binectariferum Hook.f (Meliaceae).

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Rohitukine, a chromone alkaloid, possesses anti-inflammatory, anti-cancer and immuno-modulatory properties. It has been reported from four species, belonging to the families, Meliaceae and Rubiaceae. Stem bark of Dysoxylum binectariferum (Meliaceae) accumulates the highest amount of rohitukine (3-7%

Chromones bearing amino acid residues: Easily accessible and potent inhibitors of the breast cancer resistance protein ABCG2

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The Breast Cancer Resistance Protein (BCRP/ABCG2) belongs to the G class of ABC (ATP-Binding Cassette) proteins, which is known as one of the main transporters involved in the multidrug resistance (MDR) phenotype that confer resistance to anticancer drugs. The aim of this study was to design,

Mechanistic insights into a novel chromone-appended Cu(II) anticancer drug entity: in vitro binding profile with DNA/RNA substrates and cytotoxic activity against MCF-7 and HepG2 cancer cells.

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A new chromone-appended Cu(ii) drug entity () was designed and synthesized as a potential anticancer chemotherapeutic agent. The structural elucidation was carried out thoroughly by elemental analysis, FT-IR, EPR, ESI-MS and single crystal X-ray crystallography. Complex resulted from the in situ

Synthesis and molecular docking study of new benzofuran and furo[3,2-g]chromone-based cytotoxic agents against breast cancer and p38α MAP kinase inhibitors.

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This study deals with synthesis of a new set of benzofuran and 5H-furo[3,2-g]chromone linked various heterocyclic functionalities using concise synthetic approaches aiming to gain new antiproliferative candidates against MCF-7 breast cancer cells of p38α MAP kinase inhibiting activity. The

Development of Newly Synthesized Chromone Derivatives with High Tumor Specificity against Human Oral Squamous Cell Carcinoma

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Since many anticancer drugs show severe adverse effects such as mucositis, peripheral neurotoxicity, and extravasation, it was crucial to explore new compounds with much reduced adverse effects. Comprehensive investigation with human malignant and nonmalignant cells demonstrated that derivatives of

Anti-cancer and immunostimulatory activity of chromones and other constituents from Cassia petersiana.

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Phytochemical investigation of Cassia petersiana Bolle leaves afforded four new compounds, including two chromone derivatives, 7-acetonyl-5-hydroxy-2-methylchromone (petersinone 1, 1) and 7-(propan-2'-ol-l'-yl)-5-hydroxy-2-methylchromone (petersinone 2, 2), two benzoic acid derivatives,

The Chromone Alkaloid, Rohitukine, Affords Anti-Cancer Activity via Modulating Apoptosis Pathways in A549 Cell Line and Yeast Mitogen Activated Protein Kinase (MAPK) Pathway.

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The field of cancer research and treatment has made significant progress, yet we are far from having completely safe, efficient and specific therapies that target cancer cells and spare the healthy tissues. Natural compounds may reduce the problems related to cancer treatment. Currently, many plant

The in vitro and in vivo effects of 2-(4-morpholinyl)-8-phenyl-chromone (LY294002), a specific inhibitor of phosphatidylinositol 3'-kinase, in human colon cancer cells.

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OBJECTIVE Phosphatidylinositol 3'-kinase (PI3K) and Akt/protein kinase B(PKB) allow for escape from apoptosis in various human cancer cells. We postulated that 2-(4-morpholinyl)-8-phenyl-chromone (LY294002), a PI3K inhibitor, should inactivate Akt/PKB, consequently inhibiting cell proliferation and

New 2-(2-phenylethyl)chromone derivatives from agarwood and their inhibitory effects on tumor cells.

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Two new chromone derivatives, 7-hydroxy-2-[2-(3'-methoxy-4'-hydroxyphenyl)-ethyl]chromone (1), and 6,7-dimethoxy-2-[2-(3'-hydroxyphenyl)-ethyl]chromone (2) were isolated from the EtOH extract of agarwood of Aquilaria sinensis, together with eleven known analogues. Their structures were established

Breast cancer resistance protein (BCRP/ABCG2): new inhibitors and QSAR studies by a 3D linear solvation energy approach.

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A series of compounds derived from naturally occurring flavonoids and synthetic analogs have been evaluated on cell lines overexpressing the wild-type breast cancer resistance protein (BCRP/ABCG2) half-transporter. Human ABCG2-transfected cells were used for screening their inhibitory activity. Five

Synthesis and pharmacological activities of non-flavonoid chromones: a patent review (from 2005 to 2015).

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BACKGROUND Chromones are one of the major classes of naturally occurring compounds. Their chemistry has been widely explored and extensively reviewed. The following review intends to give a broad overview of the patented chromones. Particular attention has been given to their synthesis, uses and

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