Combretastatin A4 (CA-4) is structurally related to colchicines and first isolated from Combretum caffrum. CA-4 and its related derivatives possess potency on inhibition of tubulin polymerization. On the basis of their structural features, it is essential for antimicrotubule agents to possess two aryl rings in cis conformation and methoxy groups on the aryl rings. Thus, a series of l-arylpyrrolo[3,2-c]quinolin- 4-one derivatives were designed as antimicrobubule agent for the treatment of tumors. One-pot reaction of diethyl 2-(2-ethoxyethyl)malonate with various anilines by the use of microwave radiation afforded the corresponding symmetric product 2-(2-ethoxyethyl)-AyV-diaryl malonamide, which was then followed by intramolecular cyclization to provide the key intermediates l-aryl-2,3-dihydro-lH- pyrrolo[3,2-c]quinolin-4-one directly. Fifinally, the planar 1-aryl- pyrrolo[3,2-c]quinolin-4-one derivatives were obtained by dehydrogenation reaction with the use of Pd/C in diphenyl ether at reflux. synthesized target compounds 1 -arylpyrrolo[3,2-c]quinolin-4 derivatives were evaluated for in vitro cytotoxicity by SRB methods against gastric cancer cell lines AGS, lung cancer cell lines A549, and colon cancer cell lines HT-29.These derivatives exhibited selectivity on HT-29 cell lines. Further, more substituents on the aromatic ring resulted in better inhibitory acuvuy.