Background: Cancer is an important cause of human death worldwide. During the last
decades, many anticancer agents with anti-tubulin mechanism have been synthesized or extracted
from nature and some of them also entered clinical use. Indibulin is one of the most potent tubulin
polymerization inhibitors with minimal peripheral neuropathy, which is a big problem by some of
the antimitotic agents such as taxanes and vinka alkaloids. With respect to this giant benefit, herein
we decided to design and synthesize novel indibulin related compounds and investigate their
anticancer activity against HT-29, Caco-2 and T47-D cancerous cell lines as well as NIH-T3T as
normal cell line.
Objective: The aim of this study was to synthesize new anti-cancer agents and evaluates their cytotoxic
activity on diverse cancerous and normal cell lines.
Methods: Target compounds were synthesized in multistep reaction and cytotoxic activity was investigated
by MTT cell viability assay.
Results: Herein, nine novel target compounds were synthesized in moderate to good yield. Some
of the compounds exerted good cytotoxic activity against cancerous cell lines. Annexin V/PI staining
showed that compound 4g could induce apoptosis and necrosis in HT-29 cell line.
Conclusion: It is valuable to do further investigation on compound 4g which showed the highest
activity against HT-29 and Caco-2 (IC50 values are 6.9 and 7 μM respectively). Also, synthesis of
new derivatives of current synthesized compounds is suggested.