Document Type
Original Study
Subject Areas
Pharmaceutical Organic Chemistry
Keywords
benzo[h]quinolines, melanoma, CDK2, EGFR
Abstract
Background: Benzo[h]quinolines have attracted a lot of interest because of their biological characteristics, especially their capacity to impede cell proliferation, for this reason it is essential to utilize their high activity for new, powerful anti-cancer agents’ discovery. Objective: The main objectives are to synthesize de-novo benzo[h]quinolines and fused analogues then evaluate their anti-cancer activities. Methods: Our target compounds 1a-d were prepared through Knoevenagel condensation followed by Michael addition. Compounds 1a-d were further cyclized via reactions with different reagents particularly, formic acid, formamide, acetic anhydride and carbon disulfide to obtain fused derivatives 2-5 (a-d) respectively. Structures of the new synthesized derivatives were confirmed using elemental, IR, Mass, and 1H-NMR spectrum analysis. All the newly synthesized derivatives were selected by the National Cancer Institute (NCI) for single dose assay on 60 cell lines. Furthermore, docking study on Cyclin Dependent Kinase type 2 (CDK2) as well as Epidermal Growth Factor Receptor (EGFR) was performed Results: Among all tested compounds compound 1b and compound 4c exhibited the strongest activity especially against melanoma. Conclusion: Further investigations on the prepared compounds specifically, 1b and 4c are needed to get more promising agents.
How to Cite This Article
Khodair, Marwa A.; Mohamed, Mosaad S.; Awad, Samir M.; and El-Hameed, Rania H. Abd
(2024)
"Synthesis, anticancer activity and docking study of novel benzo[h]quinoline derivatives,"
Trends in advanced sciences and technology: Vol. 1:
Iss.
1, Article 12.
DOI: 10.62537/2974-444X.1012
Available at:
https://tast.researchcommons.org/journal/vol1/iss1/12
