Design, synthesis and antitumor activity of novel 4-oxobutanamide derivatives.

To find highly effective and low-toxicity antitumor drugs to overcome the challenge of cancer, we designed and synthesized a series of novel 4-oxobutanamide derivatives using the principle of molecular hybridization and tested the antiproliferative ability of the title compounds against human cervical carcinoma cells (HeLa), human breast carcinoma cells (MDA-MB-231) and human kidney carcinoma cells (A498). Among them, N-(4-methoxybenzyl)-N-(4-methoxyphenyl)-N-(3,4,5-trimethoxyphenyl) succinimide DN4 (IC = 1.94 µM) showed the best proliferation activity on A498, superior to the positive control paclitaxel (IC = 8.