3-Bromophenyl 6-acetoxymethyl-2-oxo-2H-1-benzopyran-3-carboxylate inhibits cancer cell invasion in vitro and tumour growth in vivo.
I. Kempen,D. Papapostolou,N. Thierry,Lionel Pochet,Stéphane Counerotte,Bernard Masereel,Jean-Michel Foidart,Michèle Reboud-Ravaux,Agnès Noël,Bernard Pirotte +9 more
TLDR
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.read more
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Current developments of coumarin-based anti-cancer agents in medicinal chemistry
Saeed Emami,Sakineh Dadashpour +1 more
TL;DR: The current developments of coumarin-based anticancer agents are covered and the structure-activity relationship of the most potent compounds are discussed.
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Recent Advances in the Synthesis of Coumarin Derivatives via Knoevenagel Condensation: A Review
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.
Journal ArticleDOI
Synthesis of new coumarin 3-(N-aryl) sulfonamides and their anticancer activity.
Natala Srinivasa Reddy,Muralidhar R. Mallireddigari,Stephen C. Cosenza,Kiranmai Gumireddy,Stanley C. Bell,E. Premkumar Reddy,M. V. Ramana Reddy +6 more
TL;DR: All the compounds tested for antiproliferative activity in different cancer cell lines have shown GI(50) values less than 100 microM.
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Vitamin K2 inhibits the growth and invasiveness of hepatocellular carcinoma cells via protein kinase A activation
Motoyuki Otsuka,Naoya Kato,Run-Xuan Shao,Yujin Hoshida,Hideaki Ijichi,Yukihiro Koike,Hiroyoshi Taniguchi,Masaru Moriyama,Yasushi Shiratori,Takao Kawabe,Masao Omata +10 more
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.
Journal ArticleDOI
Synthesis of new conjugated coumarin-benzimidazole hybrids and their anticancer activity.
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.
References
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