Synthesis and anti-cancer, anti-metastatic evaluation of some new fluorinated isocoumarins and 3,4-dihydroisocoumarins

Synthesis of some fluorinated isocoumarins and 3,4-dihydroisocoumarins is reported. Structures of the synthesized compounds were confirmed by spectral and elemental analysis. All the synthesized compounds were evaluated for their antimetastatic activity and anti-cancer activity against breast cell line (MCF-7). Among all the tested compounds 3h [3-(3′,4′-difluorophenyl)isocoumarin] has shown excellent antimetastatic activity, however the growth inhibitory response of the tested compounds [3a–h, 4a–h, 5e–h, 6a–h and 7a, c, d] for MCF-7 human breast carcinoma cell line was moderate at higher concentrations (100–400 μM) and negligible at lower concentrations.

Graphical abstractSynthesis of a new series of dihalophenylisocoumarin and 3,4-dihydroisocoumarin derivatives is reported. Synthesized compounds were evaluated for antimetastatic activity and anti-cancer activity against breast cell line (MCF-7).Figure optionsDownload full-size imageDownload as PowerPoint slideHighlights► A new series of isocoumarin and 3,4-dihydroisocoumarin derivatives is synthesized. ► These compounds are evaluated for antimetastatic and anti-cancer activities. ► The compound 3h has shown excellent anti-metastatic activity. ► Growth inhibitory response for MCF-7 human breast carcinoma cell line was moderate.