{"database":"biostudies-literature","file_versions":[],"scores":null,"additional":{"omics_type":["Unknown"],"volume":["30(5)"],"submitter":["Kandeel MM"],"funding":["STDF-RSG, Egypt"],"pubmed_abstract":["A series of indolinone-based derivatives were designed and synthesized using the hybrid pharmacophoric design approach as cytotoxic kinase inhibitors. The cytotoxic effects of the designed molecules were tested against MCF-7 and HepG-2 cell lines. Compounds <b>9</b> and <b>20</b> were the most cytotoxic, with IC<sub>50</sub> values against HepG-2 and MCF-7 cells ranging from 2.53 to 7.54 µM. Additionally, compounds <b>9</b> and <b>20</b> were also found to be slightly more cytotoxic than indirubin with 2.2-2.7-fold higher cytotoxicity with HepG-2 cells. CDK-2 and CDK-4 kinase enzyme inhibition assay showed that compound <b>9</b> had a higher inhibitory effect (4.8-fold) than indirubin against CDK-2 and comparable inhibition against CDK-4. Moreover, compound <b>20</b> displayed nanomolar in"],"journal":["Molecules (Basel, Switzerland)"],"pagination":["1105"],"full_dataset_link":["https://www.ebi.ac.uk/biostudies/studies/S-EPMC11901902"],"repository":["biostudies-literature"],"pubmed_title":["Design, Synthesis, and Cytotoxicity Evaluation of Novel Indolin-2-One Based Molecules on Hepatocellular Carcinoma HepG2 Cells as Protein Kinase Inhibitors."],"pmcid":["PMC11901902"],"pubmed_authors":["AbdElhameid MK","Al-Shorbagy MY","Kandeel MM","Adel M","Negmeldin AT"],"additional_accession":[]},"is_claimable":false,"name":"Design, Synthesis, and Cytotoxicity Evaluation of Novel Indolin-2-One Based Molecules on Hepatocellular Carcinoma HepG2 Cells as Protein Kinase Inhibitors.","description":"A series of indolinone-based derivatives were designed and synthesized using the hybrid pharmacophoric design approach as cytotoxic kinase inhibitors. The cytotoxic effects of the designed molecules were tested against MCF-7 and HepG-2 cell lines. Compounds <b>9</b> and <b>20</b> were the most cytotoxic, with IC<sub>50</sub> values against HepG-2 and MCF-7 cells ranging from 2.53 to 7.54 µM. Additionally, compounds <b>9</b> and <b>20</b> were also found to be slightly more cytotoxic than indirubin with 2.2-2.7-fold higher cytotoxicity with HepG-2 cells. CDK-2 and CDK-4 kinase enzyme inhibition assay showed that compound <b>9</b> had a higher inhibitory effect (4.8-fold) than indirubin against CDK-2 and comparable inhibition against CDK-4. Moreover, compound <b>20</b> displayed nanomolar in","dates":{"release":"2025-01-01T00:00:00Z","publication":"2025 Feb","modification":"2026-04-08T19:48:44.913Z","creation":"2025-04-04T09:08:14.277Z"},"accession":"S-EPMC11901902","cross_references":{"pubmed":["40076329"],"doi":["10.3390/molecules30051105"]}}