Identification of Linomide Derivatives as Potential Anticancer Therapeutics using Molecular Docking Studies.

ABSTRACT: 12 analogs bearing a structural similarity to Linomide, a bonafide anticancer agent were synthesized wherein cyclization of substituted dianilides rendered 4-hydroxyquinolin-2(1H)-ones that were subjected to a Mannich reaction to yield 4-hydroxy-3-(substituted-1-ylmethyl) quinolin-2(1H)-one analogs. Characterization was performed using IR, ¹H nuclear magnetic resonance and ¹³C NMR spectral analysis. Subsequently, in vitro anticancer studies revealed that Compound 4b showed maximum cytotoxicity with IC₅₀ values of 1.539 μM/ml and 1.732 μM/ml against A549 and K562 cell lines respectively. This, however, is lower in comparison with standard Paclitaxel (IC₅₀ values of 0.3 μM/ml for both cell lines). Surprisingly, docking studies at the active

SUBMITTER: Borges E Soares GA 

PROVIDER: S-EPMC9243562 | biostudies-literature | 2022

REPOSITORIES: biostudies-literature