lamellarin-d and fosbretabulin

A new series of hybrids of lamellarin D and combretastatin A 4, 1,2-diphenyl-5,6-dihydropyrrolo [2,1-a] isoquinolines, were designed as cytotoxic agents based on principles of combination in medicinal chemistry and taking the parent compounds' different anti-proliferative mechanisms into consideration. Twenty-two novel hybrids were synthesized through a convenient route, with a key step of core pyrrole formation and evaluated for their anti-proliferative activities in vitro against K-562, A-549, SMMC-7721, SGC-7901 and HCT-116 cancer cell lines. The results showed that some hybrids had good anti-proliferative activities in low IC50 ranges.

Topics: Cell Line, Tumor; Cell Proliferation; Coumarins; Cytotoxins; Heterocyclic Compounds, 4 or More Rings; Humans; Inhibitory Concentration 50; Isoquinolines; Models, Molecular; Molecular Conformation; Stilbenes