Background: Triazole based drugs are widely used in cancer patients for the treatment of lifethreatening
invasive fungal infections. A recent report on the usefulness of 1,2, 3- triazole scaffold for the
inhibition of tyrosine kinases stimulated our curiosity to design new molecules based on this moiety.
Methods: A series of new heterocyclic compounds containing 1,2,3 triazole moiety tethered to substituted
vanillin or isovanillin were synthesized and analysed for their anticancer activity. The cyclopentyl/
cyclohexyl ethers derived from vanillin and isovanillin were subsequently treated with MeMgI to give
the carbinols. Reaction of these carbinols with TMSN3 and ZrCl4 as Lewis acid gave the desired azides.
Click chemistry on azides with diverse acetylenes furnished the triazoles. The new triazole hybribs were
screened o against 60 human cancer cell lines at a 10M dose for their potential anticancer activity.
Results: The two active compounds (8a, 10a) showed strong inhibitory effect against different cell lines,
with highest inhibition against breast cancer panel. To elucidate the underlying molecular mechanisms,
these compounds were examined for their clonogenic potential and anchorage-independent growth of
estrogen receptor positive (MCF7 and T47D) and estrogen receptor negative (MDA-MB-231 and MDAMB-
468) breast cancer cells and investigated for induction apoptotic pathways.
Conclusion: The outcomes from the current study will add much to the existing knowledge of the
breast cancer research. This provides a rewarding conclusion and opens the way for future researchers
to design and synthesize the novel active compounds against breast cancer.