aovernment College of Pharmacy, Kathora Naka, Amravati-444 604, Maharashtra, India E-mail : bhushan _ baviskar@rediffmail.com Dr. Reddy's Laboratories, Ameerpet, Hyderabad, India Manuscript received online 29 January 2012, revised 12 February 2012, accepted 18 February 2012 In continuation to our work for the development of new anticancer agents, novel clubbed triazolylindenoisoquinoline derivatives were synthesized in good yields and characterized by IR, 1H NMR, mass spectral and elemental analyses. The prepared compounds were tested for their in vitro anticancer activity against 05 human cancer cell lines including human lung (HOP62), ovarian (OVKAR3), breast (ZR751), leukemia (HL60) and prostate (DU145) cancer cell lines and showed potential anticancer activity when compared with the Doxorubicin as a reference drug. The results of anticancer activity indicate that the most of synthesized compounds showed significant to weak cytotoxic effect on the different cell lines. Among the twenty-one prepared compounds, four compounds exhibited strong topoisomerase I inhibitory activity but different from that of camptothecin.