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To investigate the effects and mechanisms of 4-(1 H -indol-1-yl)-4-oxobutanoic acid spliced podophyllotoxin derivatives ( 3a – 3l ) on tumor cells. The MTT method was adopted to evaluate ( 3a – 3l ) antitumor activity  in vitro  against A549 cells, A549/DDP cells, MCF-7 cells. The results showed that compound  3l  had the most prominent inhibitory effect and high selectivity with IC 50  18.53 ± 1.51 µM against A549/DDP cells. Meanwhile, the effects of compound  3l  on the nuclear state, cell cycle and apoptosis of A549/DDP cells showed that compound  3l  induced apoptosis by delaying the G 2 /M phase of A549/DDP cell cycle. In addition, molecular docking of compound  3l  also showed that it could form a good hydrogen bond with ARG-158 ( d  = 2.6, 2.7 Å) and HIS-406 ( d  = 2.5 Å) at the colchicine site of tubulin. Compound  3l  could provide lead compound for the development of new multi-drug resistant anti-tumor drugs.

Synthesis and antitumor activities of 4-(1H-indol-1-yl)-4-oxobutanoic acid spliced podophyllotoxin derivatives