Background:
In this era of science, cancer is a black dot on the face of humankind. Consequently, the
search of promising anticancer agents continues.
Aims:
Here we designed and synthesized new N-substituted rhodanines (RD1-7), evaluated their multispectroscopic
interaction with calf thymus DNA, in silico and anticancer studies against MDA-MB-231cancer
cell line.
Methods:
By MTT assay rhodanine RD1 was found to be the most potent with IC50 value of 72.61 μM. In addition,
DNA binding studies (UV-vis and fluorescence) revealed strong binding affinity of RD1-7 with DNA (Kb
in the range of 1.5-7.4 × 105 M-1). Moreover, molecular docking study, experimental DNA binding and anticancer
studies are all well agreed to each other.
Results:
It was observed that H-bonding and hydrophobic attractions were responsible for stability of DNAcompound
adducts. Besides, the reported rhodanines (RD1-7) were found as minor groove binders of DNA.
Concisely, RD1-7 indicated promising pharmacological properties and hence, shows auspicious future for the
development of novel anticancer agents.
Conclusion:
The reported rhodanines showed excellent anticancer properties. Therefore, the described rhodanines
may be used as potential anticancer agents in the future.