Pharmacological Profile of 6,12-Dihydro-3-methoxy-1-benzopyrano[3,4-b][1,4]benzothiazin-6-one, a Novel Human Estrogen Receptor Agonist.

Jacquot, Yves; Cleeren, Anny; Laı̈os, Ioanna; Ma, Yanna; Boulahdour, Athem; Bermont, Laurent; Refouvelet, Bernard; Adessi, G. L.; Leclercq, Guy; Xicluna, Alain

doi:10.1248/bpb.25.335

Cited by 12 publications

(1 citation statement)

References 44 publications

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“…4‐Aminocoumarin was obtained in 90% yield by melting 4‐hydroxycoumarin in the presence of excess ammonium acetate for 30 min. This method compared to the ones using boiling acetic acid or ethoxyethanol has more yields and needs less time 26–29. It seems 4‐aminocoumarin was converted to 4‐hydroxycoumarin in the presence of both solvents and heating, making to decrease yield.…”

Section: Chemistrymentioning

confidence: 97%

Design, Synthesis and Evaluation of Cytotoxicity of Novel Chromeno[4,3‐b]quinoline Derivatives

Miri

Motamedi

Rezaei

et al. 2010

Archiv der Pharmazie

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In the present work 15 new 1,4-dihydropyridines (DHPs) bearing a coumarin ring were synthesized and assessed on 4 different human cancer cell lines (HeLa, K562, LS180, and MCF-7). Although, all the derivatives were inactive on LS180 cell line, the results on other cells showed that these compounds had weak to moderate antitumoral activities and their IC(50) ranged from 25 to >100 µM. Among the synthesized compounds, 7-(2-nitrophenyl)-8,9,10,12-tetrahydro-7H-chromeno[4,3-b]quinoline-6,8-dione (6a) demonstrated the highest activity (IC(50) range in different cell lines: 25.4-58.6 µM). Furthermore, the calcium channel antagonist activity of the derivatives, an undesired effect when these compounds are used as antitumoral agents, was much lower than nifedipine, a reference antagonist. In conclusion, this group of compounds seems to have promising biological properties and further investigation on this group could potentially lead to the discovery of cytotoxic agents with low calcium channel blocking activity.

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Section: Chemistrymentioning

confidence: 97%