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Griseofulvin  1  is an important antifungal agent that has recently received attention due to its antiproliferative activity in mammalian cancer cells. Study of SAR of some griseofulvin analogues has led to the identification of 2′-benzyloxy griseofulvin  3 , a more potent analogue which retards tumor growth through inhibition of centrosomal clustering. However, similar to griseofulvin  1 , compound  3  exhibited poor aqueous solubility. In order to improve the poor water solubility, six new griseofulvin analogues  5 – 10  were synthesized and tested for their antiproliferative activity and water solubility. The semicarbazone  9  and aminoguanidine  10  analogues were the most potent against HCT116 and MCF-7 cell lines. In combination studies, compound  9  was found to exert synergistic effects with tamoxifen and 5-fluorouracil against MCF-7 and HCT116 cells proliferation, respectively. The flow cytometric analysis of effect of  9  on cell cycle progression revealed G2/M arrest in HCT116. In addition, compound  9  induced apoptosis in MCF-7 cells. Finally, all synthesized analogues revealed higher water solubility than griseofulvin  1  and benzyloxy analogue  3  in pH 1.2 and 6.8 buffer solutions.

Design, Synthesis, and Cytotoxicity Evaluation of Novel Griseofulvin Analogues with Improved Water Solubility