English (United Kingdom)

https://curated-unify.zendy.io/wp-json/zendy-region/v1/featured_content/oa?rat=en

https://curated-unify.zendy.io/wp-json/zendy-region/v1/highlighted_journal/

Global: Zendy Plus annual

Presents the access of premium content as premium feature

Premium Content

Presents the keyphrase highlighting as premium feature

Keyphrase Highlighting

Presents the summarisation as premium feature

Summarisation

Insights

Presents the pdf analysis as premium feature

PDF Analysis

Presents the zaia usage as premium feature

ZAIA

Global: Zendy Tools annual

Global: Zendy Free Plan

Global: Zendy Tools monthly

Global: Zendy Plus monthly

In continuance of search for new compounds we report herein the expedient and optimized synthesis of a series of  N -(4-substituted phenyl)-7-hydroxy-4-methyl-2-oxoquinoline-1(2 H )-carbothioamides ( 5a-g ) in good yields. The anticancer and antioxidant activities were determined as per the standard protocol. Nearly 5 dozens of cancer cell lines derived from nine different panels are used in the study and anticancer activity was calculated as growth percents (GPs) and percent growth inhibitions (%GIs). The molecular docking simulation against one of the potential targets i.e., epidermal growth factor receptor (EGFR) was done to find the putative approach of action of the title compounds  5a-g .  N -(4-Nitrophenyl)-7-hydroxy-4-methyl-2-oxoquinoline-1(2 H )-carbothioamides ( 5b ) showed the most promising anticancer activity with higher sensitivity against UO-31, HOP-92, CAKI-1, LOX IMVI and T-47D with GPs of 66.65, 72.63, 85.80, 86.11, and 86.96 respectively. The compound  5b  exhibited antioxidant activity with an IC 50  value of 15.21 ± 1.52 µM. The molecular docking simulation showed an efficient binding of compound  5b  against the activity site of EGFR with two H-bond interactions with the residues Gln791 and Thr854, a π-π stacking and a π-cationic interaction with the residue Phe856, while a salt bridge interaction with the residue Lys745.

Synthesis and Biological Evaluations of N -(4-Substituted Phenyl)-7-Hydroxy-4-Methyl-2-Oxoquinoline-1(2 H )-Carbothioamides