Aisha A. Alsfouk (Data curation Funding acquisition Methodology Validation Writing – original draft) , Benson M. Kariuki (Data curation Formal analysis Investigation Methodology Resources Software Validation Visualization Writing – original draft) , Asmaa Saleh (Data curation Funding acquisition Project administration Validation Visualization Writing – original draft) , Aladdin M. Srour (Conceptualization Investigation Methodology Supervision Validation Visualization Writing – original draft Writing – review & editing)
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引用次数: 0
Abstract
Three novel 4-piperidone-based derivatives (3a–c) were synthesized utilizing the base-catalyzed condensation method (KOH/EtOH) with aromatic aldehydes (2a–c) featuring secondary amine rings, specifically piperidine, morpholine, and methyl piperazine. The three newly synthesized derivatives were characterized through X-ray crystallography, and their anti-proliferative effects were assessed against three different human cancer cell lines: breast carcinoma (MCF-7), liver cancer (HepG-2), and colorectal carcinoma (HCT-116), along with a normal cell line (RPE1), following the MTT assay procedure. Among them, compound 3c demonstrated the highest efficacy against all tested cell lines, demonstrating IC50 = 1.07 ± 0.04 μM for MCF-7 and 2.55 ± 0.07 μM for HepG-2, compared to the standard reference, Doxorubicin, which had IC50 = 5.38 ± 0.05 μM and 4.25 ± 0.01 μM, respectively. Moreover, a molecular docking study confirmed the stable interaction of compound 3c within the ATP binding site of human cyclin-dependent kinase 2 (CDK2). This study introduces three promising intermediates for further research in medicinal chemistry.
期刊介绍:
Synthetic Communications presents communications describing new methods, reagents, and other synthetic work pertaining to organic chemistry with sufficient experimental detail to permit reported reactions to be repeated by a chemist reasonably skilled in the art. In addition, the Journal features short, focused review articles discussing topics within its remit of synthetic organic chemistry.