Quinoline conjugated 2-azetidinone derivatives as prospective anti-breast cancer agents: In vitro antiproliferative and anti-EGFR activities, molecular docking and in-silico drug likeliness studies

Nitrogen‐Containing Heterocyclic Scaffolds as EGFR Inhibitors: Design Approaches, Molecular Docking, and Structure‐Activity Relationships

“…Additionally, an in-vitro enzyme assay was used to assess mechanism of top compounds, and the results showed that compound 77a was the most intriguing, with an IC 50 value of 97.1 μM. [151]…”

“…Compounds, 77 a , 77 b , and 77 c (Figure 75), showed the greatest with IC 50 values of 3.36, 4.38, and 2.33 μM against the MCF7 cell line and 6.41, 6.15, and 4.91 μM against the MDA‐MB‐231 cell line, respectively. Additionally, an in‐vitro enzyme assay was used to assess mechanism of top compounds, and the results showed that compound 77a was the most intriguing, with an IC 50 value of 97.1 μM [151] …”

Palladium-Mediated Synthesis of 2-([Biphenyl]-4-yloxy)quinolin-3-carbaldehydes through Suzuki–Miyaura Cross-Coupling and Their in Silico Breast Cancer Studies on the 3ERT Protein

“…The recent literature shows evidently that quinoline-based compounds are widely used for anticancer treatment, especially breast cancer . Quinolone-based compounds recently reported by Govindarao et al are found to act against breast cancer cells . Kardile et al reported the in vitro screening, molecular docking, and absorption, distribution, metabolism, and excretion (ADME) predictions of quinolone derivatives .…”

“… 3 Quinolone-based compounds recently reported by Govindarao et al are found to act against breast cancer cells. 4 Kardile et al reported the in vitro screening, molecular docking, and absorption, distribution, metabolism, and excretion (ADME) predictions of quinolone derivatives. 5 The derivatives with a quinoline core are also known as potent tubulin assembly inhibitors, 6 mutant epidermal growth factor receptor (EGFR) inhibitors targeting resistance in lung cancer cells, 7 anti-tubulin agents targeting the colchicine binding site, 8 potential anti-hepatoma agents, 9 and various other anticancer activities; 10 − 13 hence, we intend to synthesize new quinoline derivatives and screen them for their activity against the breast cancer 3ERT protein.…”

Recent advances in chemistry and therapeutic potential of functionalized quinoline motifs – a review

“…Furthermore, functionalized quinoline moieties are highly essential pharmacophoric motifs with undeniable therapeutic propensity owing to their numerous reported biological and pharmacological activities, which include anticancer, 13 antimicrobial, 14 anti-inflammatory, 15 antioxidant, 16 antitubercular, 17 antimalarial, 18 anti-leishmanial, 19 antiprotozoal, 20 anti-HIV, 21 and DNA binding 22 among others. However, the previous review by Sharma and coworkers only highlighted the anti-cancer activities of quinoline derivatives, 2 while the review by Martins and coworkers focused on the quinoline heterocycle as a tool box in nanomedicine.…”