SYNTHESIS AND ANTIPROLIFERATIVE ACTIVITY OF FLAVONOID DERIVATIVES: EFFECT OF B-RING SUBSTITUTION

Flavones, flavonols, flavanones and isoflavones constitute four important categories of naturally occurring flavonoids. These compounds possess good antiproliferative activity and can act as adjuvants to existing anticancer therapy. We have synthesized twenty synthetic flavonoids including flavones, flavonols, flavanones and isoflavones using Claisen-Schmidt condensation, Baker-Venkataraman rearrangement and related reactions. The synthesized compounds were evaluated for antiproliferative activity against MCF-7, K562 and HepG2 cell lines. Flavanones showed good activity against HepG2 cell lines whereas some flavones and isoflavones were active in inhibiting the growth of K562 and MCF-7 cell lines. The study underlines the importance of electron rich substituents on the B-ring of synthetic flavonoids.