Abstract
AbstractEighteen isoandrographolide analogues were synthesized, characterized and tested for their anticancer activity against 60 cancer cell lines at NCI. Three of the synthesized acetals ((3,19)‐3‐Nitro‐benzylidene‐isoandrographolide (3 p), (3,19)‐4‐Nitrobenzylidene‐isoandrographolide (3 q) and (3,19)‐4‐Isopropyl‐benzylidene‐isoandrographolide (3 r)) are novel. Most of the compounds were found to be active against leukaemia and breast cancer with (3,19)‐3,5‐difluorobenzylidene‐isoandrographolide(3 o) having the best growth inhibition of 76.90 % and 87.54 % against leukaemia (MOLT‐4) and breast cancer (BT‐549) respectively. A single crystal of compound 3 o was grown and it was characterized using single‐crystal X‐ray diffraction studies. Further studies showed that the compound (3,19)‐4‐Bromobenzylidene‐isoandrographolide (IC50 3 μM) was more active than tamoxifen (IC50 12 μM) against MCF‐7 and arrested the cell cycle at G1‐Phase of MCF‐7 and was observed to be inducing apoptosis and loss of mitochondrial membrane potential.
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