Patented technology of flavonoid dimers in treating cancers. Our group has been focusing on improving the potency and pharmacokinetic of flavonoids against the ATP-binding cassette (ABC) transporter-mediated MDR while retaining their low toxicity. A bivalent approach using various length of poly(ethyleneglycol) (PEG) chains was employed to link two natural and safe apigenins together. After further structural modification, there was 68-fold improvement in potency without causing any toxicity. In order to rapidly generate a large number of diverse and dimeric modulators which have better physiochemical properties as potential drug candidates, we employed "Click Chemistry" approach. From our in-house compound library, some candidates have been proved to be good modulator to reverse drug resistance, oral cancer drug, brain cancer drug and chemosensitizer to reverse drug resistance in breast cancer stem cells (bCSCs).