- New (arene)ruthenium(II) complexes of 4?aryl?4H?naphthopyrans with anticancer and anti-vascular activities
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A series of four 2?amino?3?cyano?4?(3/4?pyridyl)?4H?benzo[h]chromenes 2a–d and their dichlorido(p?cymene)ruthenium(II) complexes 3a–d were tested for antiproliferative, vascular-disruptive, anti-angiogenic and DNA-binding activity. The coordination of the 4?pyridyl?4H?naphthopyrans 2 to ruthenium led to complexes with pleiotropic effects. Unlike the free ligands 2a–d, their ruthenium complexes 3a–d showed a significant affinity for DNA as demonstrated by electrophoretic mobility shift assays (EMSA) and ethidium bromide assays. Binding of 3a–d to calf thymus DNA proceeded about 10-times faster compared with cisplatin. Treatment of HT-29 colon carcinoma, 518A2 melanoma and MCF-7Topo breast cancer cells with 3a and 3b caused an accumulation of cells in the G2/M phase and an increase of the fraction of mitotic cells in the case of HT-29, due to alterations of the microtubule cytoskeleton as shown by immunofluorescence staining. Complexes 3b–c showed a dual effect on the vascular system. They suppressed angiogenesis in zebrafish embryos and they destroyed the vasculature of the chorioallantoic membrane (CAM) in fertilized chicken eggs. They also inhibited the vasculogenic mimicry, typical of U-87 glioblastoma cells in tube formation assays.
- Schmitt, Florian,Kasparkova, Jana,Brabec, Viktor,Begemann, Gerrit,Schobert, Rainer,Biersack, Bernhard
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- Diisopropyl azodicarboxylate mediated selective dehydrogenation of 2-amino-3-cyano 4H-chromenes
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Selective dehydrogenation of 2-amino-3-cyano 4H-chromenes to the corresponding 2-iminochromenes mediated by diisopropyl azodicarboxylate under neutral conditions is reported. The dehydrogenation reaction is compatible with phenolic hydroxyl group and gene
- Sharma, Himanshu,Mourya, Mohini,Guin, Debanjan,Joshi, Yogesh C.,Dobhal, Mahabeer P.,Basak, Ashok K.
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p. 1727 - 1732
(2017/04/13)
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- Convenient and efficient one-pot method for the synthesis of 2-amino-tetrahydro-4H-chromenes and 2-amino-4H-benzo[h]-chromenes using catalytic amount of aminofunctionalized MCM-41 in aqueous media
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A convenient and efficient one-pot method for the synthesis of 2-amino-tetrahydro-4H-chromene and 2-amino-4H-benzo[h]-chromene derivatives has been developed using a catalytic amount of amino-functionalized MCM-41 in aqueous medium. This efficient techniq
- Mirza-Aghayan,Nazmdeh,Boukherroub,Rahimifard,Tarlani,Abolghasemi-Malakshah
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p. 1499 - 1507
(2013/05/09)
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- Microwave-assisted reactions: three component process for the synthesis of 2-amino-2-chromenes under microwave heating
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A simple and efficient three component process for the synthesis of 2-amino-2-chromenes utilizing the reaction of aryl aldehydes 1a-1h with active methylenes 2a, b and 1-naphthol 3 in refluxing ethanol/piperidine under microwave-heating is described.
- Mekheimer, Ramadan A.,Sadek, Kamal U.
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p. 149 - 151
(2009/07/17)
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- Basic alumina catalysed synthesis of substituted 2-amino-2-chromenes via three-component reaction
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Substituted 2-amino-2-chromenes were obtained in excellent yield and selectivity simply by mixing malononitrile, α-naphthol and aromatic aldehydes in water in the presence of basic alumina as heterogeneous and reusable catalyst.
- Maggi, Raimondo,Ballini, Roberto,Sartori, Giovanni,Sartorio, Raffaella
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p. 2297 - 2299
(2007/10/03)
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- Three-component process for the synthesis of 2-amino-2-chromenes in aqueous media
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The reaction of an aldehyde, malononitrile and a phenol in water at reflux in the presence of cetyltrimethylammonium chloride (CTACl) as catalyst affords a one-pot synthesis of 2-amino-2-chromenes.
- Ballini, Roberto,Bosica, Giovanna,Conforti, Maria Lina,Maggi, Raimondo,Mazzacani, Alessandro,Righi, Paolo,Sartori, Giovanni
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p. 1395 - 1398
(2007/10/03)
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- Pharmaceutical compounds
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The invention provides pharmaceutical compounds of the formula: STR1 in which A - - - B is CH2 --CH2 or CH=CH; X is a pyridine or benzene ring; when X is pyridine n is 0; when X is benzene n is 0, 1 or 2 and when A - - - B is CH
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- Therapy for diabetic complications
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This invention provides a method of treating diabetic complications in mammals which comprises the administration of a compound of the Formula I: STR1 in which n, R1, R2, R3, and R4 are variables.
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