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D. Papapostolou

Bio: D. Papapostolou is an academic researcher. The author has contributed to research in topics: Biological activity & In vivo. The author has an hindex of 1, co-authored 1 publications receiving 100 citations.

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Journal ArticleDOI
TL;DR: These two coumarin derivatives may serve as new lead compounds of an original class of antitumour agents and are evaluated for antiinvasive and antimigrative properties among which two compounds revealed important activity.
Abstract: In search for new anticancer agents, we have evaluated the antiinvasive and antimigrative properties of recently developed synthetic coumarin derivatives among which two compounds revealed important activity: 3-chlorophenyl 6-acetoxymethyl-2-oxo-2H-1-benzopyran-3-carboxylate and 3-bromophenyl 6-acetoxymethyl-2-oxo-2H-1-benzopyran-3-carboxylate. Both drugs were able to inhibit cell invasion markedly in a Boyden chamber assay, the bromo derivative being more potent than the reference matrix metalloprotease (MMP) inhibitor GI 129471. In vivo, tumour growth was reduced when nude mice grafted with HT1080 or MDA-MB231 cells were treated i.p. 3 days week(-1) with the bromo coumarin derivative. These effects were not associated with the inhibition of urokinase, plasmin, MMP-2 or MMP-9. The mechanism of action of the drugs remains to be elucidated. However, these two coumarin derivatives may serve as new lead compounds of an original class of antitumour agents.

106 citations


Cited by
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Journal ArticleDOI
TL;DR: The current developments of coumarin-based anticancer agents are covered and the structure-activity relationship of the most potent compounds are discussed.

352 citations

Journal ArticleDOI
TL;DR: In this paper, the authors summarized various methods for the synthesis of coumarins via Knoevenagel condensation, including mild, efficient, and environmentally friendly protocols with good yield and purity.

172 citations

Journal ArticleDOI
TL;DR: All the compounds tested for antiproliferative activity in different cancer cell lines have shown GI(50) values less than 100 microM.

158 citations

Journal ArticleDOI
TL;DR: Similar to an acyclic retinoid—which was previously reported to prevent the recurrence of HCC—vitamin K2, another lipid‐soluble vitamin, may be a promising therapeutic means for the management of H CC.

124 citations

Journal ArticleDOI
TL;DR: A series of novel coumarin-benzimidazole hybrids, 3-(1H-benzo-2-yl)-7-(substituted amino)-2H-chromen- 2-one derivatives of biological interest displayed appreciable anticancer activities against leukemia, colon cancer and breast cancer cell lines.

109 citations