Novel hybrids from lamellarin D and combretastatin A 4 as cytotoxic agents.
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.
Shen
Li
L
ZJU-ENS Joint Laboratory of Medicinal Chemistry, College of Pharmaceutical Sciences, Zhejiang University, Hangzhou 310058, China.
Yang
Xiaochun
X
Yang
Bo
B
He
Qiaojun
Q
Hu
Yongzhou
Y
D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D003374:Coumarins / Q000737:chemistry*; D003603:Cytotoxins / Q000737:chemistry* / Q000494:pharmacology*; D006576:Heterocyclic Compounds, 4 or More Rings / Q000737:chemistry*; D006801:Humans; D020128:Inhibitory Concentration 50; D007546:Isoquinolines / Q000737:chemistry*; D008958:Models, Molecular; D008968:Molecular Conformation; D013267:Stilbenes / Q000737:chemistry*
D003374:Coumarins; D003603:Cytotoxins; D006576:Heterocyclic Compounds, 4 or More Rings; D007546:Isoquinolines; D013267:Stilbenes; C455554:lamellarin D; C058728:fosbretabulin