Design, Synthesis, and Evaluation of the Antiproliferative Activity of a Series of Novel Fused Xanthenone Aminoderivatives in Human Breast Cancer Cells

Derivatives of two novel, structurally related heterocyclic ring systems, xantheno[3,4-d]imidazole and chromeno[4,3,2-c,d]imidazo[4,5-f]indazole, bearing aminoalkyl side chains, have been synthesized, and their antiproliferative activity has been studied against the aggressive human breast MDA-MB-23...

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Bibliographic Details
Published in:Journal of medicinal chemistry 2007-04, Vol.50 (7), p.1716-1719
Main Authors: Giannouli, Vasiliki, Kostakis, Ioannis K, Pouli, Nicole, Marakos, Panagiotis, Kousidou, Olga Ch, Tzanakakis, George N, Karamanos, Nikos K
Format: Article
Language:English
Subjects:
Antineoplastic agents
Antineoplastic Agents - chemical synthesis
Antineoplastic Agents - chemistry
Antineoplastic Agents - pharmacology
Benzopyrans - chemical synthesis
Benzopyrans - chemistry
Benzopyrans - pharmacology
Biological and medical sciences
Breast Neoplasms
Drug Design
Drug Screening Assays, Antitumor
Female
General aspects
Heterocyclic Compounds, 4 or More Rings - chemical synthesis
Heterocyclic Compounds, 4 or More Rings - chemistry
Heterocyclic Compounds, 4 or More Rings - pharmacology
Humans
Imidazoles - chemical synthesis
Imidazoles - chemistry
Imidazoles - pharmacology
Medical sciences
Pharmacology. Drug treatments
Xanthenes - chemical synthesis
Xanthenes - chemistry
Xanthenes - pharmacology
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Summary:Derivatives of two novel, structurally related heterocyclic ring systems, xantheno[3,4-d]imidazole and chromeno[4,3,2-c,d]imidazo[4,5-f]indazole, bearing aminoalkyl side chains, have been synthesized, and their antiproliferative activity has been studied against the aggressive human breast MDA-MB-231 cell line. The pyrazole-fused analogue 27a possesses a pronounced antiproliferative effect on the tested cell line, evident at 1 μM, and achieves an IC50 of 6.5 μM.
ISSN:0022-2623
1520-4804
DOI:10.1021/jm061410m