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The newly synthesized coumarin derivative with dopamine, 3-(1-((3,4-dihydroxyphenethyl)amino)ethylidene)-chroman-2,4-dione, was completely structurally characterized by X-ray crystallography. It was shown that several types of hydrogen bonds are present, which additionally stabilize the structure. The compound was tested in vitro against different cell lines, healthy human keratinocyte HaCaT, cervical squamous cell carcinoma SiHa, breast carcinoma MCF7, and hepatocellular carcinoma HepG2. Compared to control, the new derivate showed a stronger effect on both healthy and carcinoma cell lines, with the most prominent effect on the breast carcinoma MCF7 cell line. The molecular docking study, obtained for ten different conformations of the new compound, showed its inhibitory nature against CDKS protein. Lower inhibition constant, relative to one of 4-OH-coumarine, proved stronger and more numerous interactions with CDKS protein. These interactions were carefully examined for both parent molecule and derivative and explained from a structural point of view.

Chemical and cytotoxicity examinations of the crude methanol extract of the aerial parts of Phyllanthus amarus. Schum. et Thonn. (Euphorbiaceae) were investigated. The cytotoxicity property of the P. amarus. was evaluated in vitro., using the human ovarian A2780 cancer cell. Bioassay-guided fraction of the crude extract (IC50 value of 31.2 µg/mL) showed that the dichloromethane fraction was most toxic with an IC50 value of 22.7 µg/mL, whereas the polar methanol fraction was least cytotoxic with an IC50 value of 31.2 µg/mL. This led to the isolation of a new chroman derivative from the dichloromethane fraction. On the basis of nuclear magnetic resonance and mass spectral data, the structure of the chroman was established as 4,4,8-trimethoxy chroman. The compound exhibited very little or no in vitro. cytotoxicity with an IC50 of 16.2 µg/mL, relative to actinomycin, the reference compound, with an IC50 of 2.0 ng/mL. It can therefore be concluded that the aerial parts of P. amarus., an extensively use...

A new chroman derivative, named ruakuric acid, was isolated from a strain of Aspergillus fumigatus growing in conjunction with a coral lichen. The structure was determined as 6-acetyl-5-hydroxy-4-methoxy-chroman-2-carboxylic acid (mixture of 2,4-cis,trans isomers).

A new chroman derivative, named ruakuric acid, was isolated from a strain of Aspergillus fumigatus growing in conjunction with a coral lichen. The structure was determined as 6-acetyl-5-hydroxy-4-methoxy-chroman-2-carboxylic acid (mixture of 2,4-cis,trans isomers).

The condensation of 7-benzoyloxy-4′-hydroxyisoflavone with 2-methyl-3-buten-2-ol gave 7-benzoyloxy-4′-hydroxy-3′-(3-methyl-2-butenyl)isoflavone. The hydrolysis of the alkylated isoflavone with dilute alkali afforded neobavaisoflavone [7,4′-dihydroxy-3′-(3-methyl-2-butenyl)isoflavone], which was then converted into isoneobavaisoflavone on heating with formic acid. 7-Benzyloxy-4′-hydroxyisoflavone was condensed with 2-methyl-3-buten-2-ol to give a chroman derivative, which was then converted into isoneobavaisoflavone by hydrolysis. 3′-(3-Methyl-2-butenyl)-5,7,4′-trihydroxyisoflavone was also synthesized from 7-benzoyloxy-5,4′-dihydroxyisoflavone in a similar manner.

Condensation of 7-benzoyldaidzein (III) with 2-methyl-3-buten-2-ol gave 7-benzoyl-3′-(3-methyl-2-butenyl)daidzein (IV). Hydrolysis of IV with dilute alkali gave 3′-(3-methyl-2-butenyl)daidzein (neobavaisoflavone) (I), which was converted into isoneobavaisoflavone (VI) when heated with formic acid. 7-Benzyldaidzein (VII) was condensed with 2-methyl-3-buten-2-ol to give a chroman derivative (VIII), which was converted into VI by hydrogenolysis.