Design, Synthesis and Docking Studies of Flavokawain B Type Chalcones and Their Cytotoxic Effects on MCF-7 and MDA-MB-231 Cell Lines.

ABSTRACT: Flavokawain B (1) is a natural chalcone extracted from the roots of Piper methysticum, and has been proven to be a potential cytotoxic compound. Using the partial structure of flavokawain B (FKB), about 23 analogs have been synthesized. Among them, compounds 8, 13 and 23 were found in new FKB derivatives. All compounds were evaluated for their cytotoxic properties against two breast cancer cell lines, MCF-7 and MDA-MB-231, thus establishing the structure-activity relationship. The FKB derivatives 16 (IC₅₀ = 6.50 ± 0.40 and 4.12 ± 0.20 μg/mL), 15 (IC₅₀ = 5.50 ± 0.35 and 6.50 ± 1.40 μg/mL) and 13 (IC₅₀ = 7.12 ± 0.80 and 4.04 ± 0.30 μg/mL) exhibited potential cytotoxic effects on the MCF-7 and MDA-MB-231

SUBMITTER: Abu Bakar A 

PROVIDER: S-EPMC6017189 | biostudies-literature | 2018 Mar

REPOSITORIES: biostudies-literature