Background: The quinoline scaffold has been an attraction due to its pharmacological activities such
as anti-HIV, anti-neoplastic, anti-asthmatic, anti-tuberculotic, anti-fungal, and anti-bacterial.
Objective: The designed quinoline-3-carboxylate derivatives were synthesized through a two-step reaction and
evaluated for antiproliferative activity against MCF-7 and K562 cell lines.
Methods: Synthesized compounds were characterized by modern analytical techniques like NMR, 2DNMR,
mass, and IR. Moreover, the purity of compounds was analyzed through the HPLC. In the progress of biological
results, all synthesized compounds were evaluated for antiproliferative activity against MCF-7 and K562 cell lines.
Results: The synthesized compounds exhibited micromolar inhibition in all over the ranges, however, some of
the compounds showed better activity than the standard anticancer drug such, as 4m and 4n with the IC50 value
of 0.33μM against the MCF-7 cell line, and the compounds 4k and 4m showed potential activity against the
K562 cell line with the IC50 value of 0.28μM. The anti-cancer activities of compounds were found to be through
the up-regulation of intrinsic apoptosis pathways.
Conclusion: The biological data of all compounds in both cell lines were utilized for the structural activity
relationship of the quinoline-3-carboxylate pharmacophore. The active lead was further validated through rigorous
in silico studies for the drug-likeness (QED) and Absorption, Distribution, Metabolism, Excretion, and
Toxicity (ADMET) properties.
Here in the present research is utilized for the demonstration of an important pharmacophore, which could be
utilized for further development to become a lead as an anticancer agent with minimal toxicity.