938-40-9Relevant articles and documents
Indane-Fused Spiropentadiene Chromanones: A Pd-Catalyzed Spiroannulation Followed by Cyclization via C-H Activation Strategy
Sharma, Abhilash,Hazarika, Hemanta,Sarmah, Manashi,Das, Babulal,Gogoi, Pranjal
, p. 11382 - 11395 (2020)
Pd-catalyzed spiroannulation of 4-bromocoumarin with alkynes has been illustrated. The reaction highlights an interesting process for cascade formation of two five-membered rings through spiroannulation followed by cyclization via C-H activation. This method offers an attractive platform for the synthesis of a broad range of indane-fused spiropentadiene chromanones in good yields.
Fragment-type 4-azolylcoumarin derivatives with anticancer properties
Simic, Milena,Petkovic, Milos,Jovanovic, Predrag,Jovanovic, Milos,Tasic, Gordana,Besu, Irina,Zizak, Zeljko,Aleksic, Ivana,Nikodinovic-Runic, Jasmina,Savic, Vladimir
, (2021)
Several coumarin derivatives with a directly attached azole substituent at C-4 were synthesized and biologically studied for their anticancer properties. The cell lines used for this investigation (HeLa, K-562, MDA-MB-53, and MCF-7) demonstrated different sensitivities. The best response in the MTT (3-(4,5-dimethyl-2-thiazolyl)-2,5-diphenyl-2H-tetrazolium bromide) assay was shown by K-562 cells, with compounds displaying activity (3c, IC50 3.06 μM; 4a, IC50 5.24 μM; 4c, IC50 4.7 μM) similar to that of cisplatin (IC50 ~6 μM), which was used as the standard. The studied azole-substituted coumarins demonstrated weaker activity toward other cell lines, except for compound 4c, which was equally potent in the case of MCF-7 cells. Additional biological evaluations supported interference with the cell cycle as a potential mechanism of action and confirmed the absence of toxicity in zebrafish embryos. On the basis of these initial results, 4-azole coumarins should be explored further. Although their activity would need additional optimization, the fact that these compounds are fragment-like structures with MW 300 and clog P 3 offers enough flexibility to fine-tune their drug-like properties.
Coumarin derivative and analogue, preparation method and application thereof
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Paragraph 0095-0098, (2021/03/31)
The invention relates to a coumarin derivative and analogue, a preparation method and application thereof, belongs to the field of chemical medicines, and provides a compound shown as a formula I or apharmaceutically acceptable salt thereof, and a preparation method and application of the compound. According to the invention, biological experiments show that the compound has a strong in-vitro anti-fibrosis effect, can obviously reduce deposition of intercellular collagenous fibers on TGF-beta induced NRK-49F cells, and has inhibition on migration of HUVEC cells; and the compound with the structure has a certain curative effect on carbon tetrachloride induced hepatic fibrosis and bleomycin induced pulmonary fibrosis mouse models, is relatively low in toxicity, and provides a new choice forclinical treatment of tissue fibrosis diseases including hepatic fibrosis, pulmonary fibrosis and renal fibrosis.
