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  • Title: Photoswitchable anticancer activity via trans-cis isomerization of a combretastatin A-4 analog.
    Author: Sheldon JE, Dcona MM, Lyons CE, Hackett JC, Hartman MC.
    Journal: Org Biomol Chem; 2016 Jan 07; 14(1):40-9. PubMed ID: 26503632.
    Abstract:
    Combretastatin A-4 (CA4) is highly potent anticancer drug that acts as an inhibitor of tubulin polymerization. The core of the CA4 structure contains a cis-stilbene, and it is known that the trans isomer is significantly less potent. We prepared an azobenzene analog of CA4 (Azo-CA4) that shows 13-35 fold enhancement in potency upon illumination. EC50 values in the light were in the mid nM range. Due to its ability to thermally revert to less toxic trans form, Azo-CA4 also has the ability to automatically turn its activity off with time. Azo-CA4 is less potent than CA-4 because it degrades in the presence of glutathione as evidenced by UV-Vis spectroscopy and ESI-MS. Nevertheless, Azo-CA4 represents a promising strategy for switchable potency for treatment of cancer.
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