Structure-activity correlation of flavonoids for inhibition of bovine lens aldose reductase.

An Ethnopharmacological Study from the Coimbatore District, Tamil Nadu, India: Traditional Knowledge Compared With Modern Biological Science

“…Some were kaempferol, myricetin, quercetin, myricitrin, quercitrin and kaempferol-3-rhamnoside (Blanc & Saqui, 1972;Hoppe, 1975: 486;Lin & Hsu, 1988;Yoshida et al, 1988). These flavonoids inhibit lens aldose reductase in humans, rats and cows (Chaudhry et al, 1983;Cohen et al, 1986;Iinuma et al, 1989;Segelman et al, 1977;Shimizu et al, 1984). The biological activity of flavonoids inhibiting lens aldose reductases thus appears to substantiate the traditional use of E. hirta.…”

Organocatalytic Enantioselective Conjugate Addition of Malonic Acid Half Thioesters to Coumarin‐3‐carboxylic Acids Using N‐Heteroarenesulfonyl Cinchona Alkaloid Amides

“…Therefore, there are several reports on enantioselective decarboxylative conjugate additions of MAHTs or β‐keto acids to α,β‐unsaturated ketones,5 aldehydes,6 sulfones,7 and nitro compounds,8,9 however, there are no reports on the enantioselective conjugate addition of MAHTs to α,β‐unsaturated esters. Furthermore, the conjugate addition of simple ester enolate equivalents with coumarin derivatives as cyclic α,β‐unsaturated esters has attracted considerable attention since the reaction gives chiral coumarin derivatives, which often exhibit a broad range of biological activities, such as an aldose reductase inhibitor,10 antiherpetic active compounds,11 estrogenically active compounds,12 a sirtuin inhibitor,13 and other biologically active compounds 14,15. Recently, Wang and co‐workers reported the synthesis of racemic 4‐substituted 3,4‐dihydrocoumarin by the conjugate addition of MAHTs to coumarin‐3‐carboxylic acids through a double decarboxylation process 16.…”

Syntheses and Biological Activities of Chroman-2-ones. A Review

“…Compounds 9 and 10 exhibited relatively high cytotoxic activity against three human carcinoma cell lines namely liver (HEPG2), cervix (HELA) and colon (HCT116). 18 and complete inactivation of α-chymotrypsin was effected by a series of halomethylated derivatives of dihydrocoumarins at pH 7 and a temperature 25 • C. 41 3,4-Dihydrocoumarins also display biological activities like aldose reductase inhibition, 42 protein kinases, 43 antiherpetic, 44 and moderate estrogenic activity. 45 Nishimura et al have observed that 4-aryl-3,4-dihydrocoumarin derivatives (18a, R = H and 18b, R = Ac) have an estrogenic activity comparable to that of the isoflavone, genistein.…”