Unknown

Dataset Information

0

Anticancer evaluation and molecular modeling of multi-targeted kinase inhibitors based pyrido[2,3-d]pyrimidine scaffold.

ABSTRACT: An efficient synthesis of substituted pyrido[2,3-d]pyrimidines was carried out and evaluated for in vitro anticancer activity against five cancer cell lines, namely hepatic cancer (HepG-2), prostate cancer (PC-3), colon cancer (HCT-116), breast cancer (MCF-7), and lung cancer (A-549) cell lines. Regarding HepG-2, PC-3, HCT-116 cancer cell lines, 7-(4-chlorophenyl)-2-(3-methyl-5-oxo-2,3-dihydro-1H-pyrazol-1-yl)-5-(p-tolyl)- pyrido[2,3-d]pyrimidin-4(3H)-one (5a) exhibited strong, more potent anticancer (IC50: 0.3, 6.6 and 7?µM) relative to the standard doxorubicin (IC50: 0.6, 6.8 and 12.8?µM), respectively. Kinase inhibitory assessment of 5a showed promising inhibitory activity against three kinases namely PDGFR ?, EGFR, and CDK4/cyclin D1 at two concentrations 50 and 100?µM in single measurements. Further, a molecular docking study for compound 5a was performed to verify the binding mode towards the EGFR and CDK4/cyclin D1 kinases.

SUBMITTER: Elzahabi HSA 

PROVIDER: S-EPMC6009920 | biostudies-literature | 2018 Dec

REPOSITORIES: biostudies-literature

Json Xml
altmetric image

Publications

Anticancer evaluation and molecular modeling of multi-targeted kinase inhibitors based pyrido[2,3-d]pyrimidine scaffold.

Elzahabi Heba S A HSA   Nossier Eman S ES   Khalifa Nagy M NM   Alasfoury Rania A RA   El-Manawaty May A MA  

Journal of enzyme inhibition and medicinal chemistry 20181201 1

An efficient synthesis of substituted pyrido[2,3-d]pyrimidines was carried out and evaluated for in vitro anticancer activity against five cancer cell lines, namely hepatic cancer (HepG-2), prostate cancer (PC-3), colon cancer (HCT-116), breast cancer (MCF-7), and lung cancer (A-549) cell lines. Regarding HepG-2, PC-3, HCT-116 cancer cell lines, 7-(4-chlorophenyl)-2-(3-methyl-5-oxo-2,3-dihydro-1H-pyrazol-1-yl)-5-(p-tolyl)- pyrido[2,3-d]pyrimidin-4(3H)-one (5a) exhibited strong, more potent antic  ...[more]

Similar Datasets

Unknown Scaffold-hopping identifies furano[2,3-d]pyrimidine amides as potent Notum inhibitors.
| S-EPMC6961116 | biostudies-literature
Unknown Synthesis and biological evaluation of pyrido[2,3-d]pyrimidine-2,4-dione derivatives as eEF-2K inhibitors.
| S-EPMC6473179 | biostudies-literature
Unknown Synthesis of Some Spiro Indeno[1,2-b]pyrido[2,3-d]Pyrimidine-5,3'-Indolines as New Urease Inhibitors.
| S-EPMC5242352 | biostudies-literature
Unknown Design, Synthesis and Docking Studies of Novel Macrocyclic Pentapeptides as Anticancer Multi-Targeted Kinase Inhibitors.
| S-EPMC6222410 | biostudies-literature
Unknown Design, synthesis, and molecular modeling of novel pyrido[2,3-d]pyrimidine analogues as antifolates; application of Buchwald-Hartwig aminations of heterocycles.
| S-EPMC3723128 | biostudies-literature
Unknown Design, Synthesis, Molecular Modeling Study and Biological Evaluation of New N'-Arylidene-pyrido [2,3-d]pyrimidine-5-carbohydrazide Derivatives as Anti-HIV-1 Agents.
| S-EPMC7393058 | biostudies-literature
Unknown N?-Aryl-6-substitutedphenylmethyl-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamines as receptor tyrosine kinase inhibitors.
| S-EPMC3276368 | biostudies-literature
Unknown Studies of Interaction Mechanism between Pyrido [3,4-<i>d</i>] Pyrimidine Inhibitors and Mps1.
| S-EPMC8401005 | biostudies-literature
Unknown Structure-activity correlations for three pyrido[2,3-d]pyrimidine antifolates binding to human and Pneumocystis carinii dihydrofolate reductase.
| S-EPMC4461351 | biostudies-literature
Transcriptomics Disparate anticancer activity of structurally similar multi-kinase inhibitors through cumulative differential effects on individual targets
2019-06-25 | GSE126850 | GEO