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Novel pyrazolo[3,4-d]pyrimidines: design, synthesis, anticancer activity, dual EGFR/ErbB2 receptor tyrosine kinases inhibitory activity, effects on cell cycle profile and caspase-3-mediated apoptosis.
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- Author(s): Maher M;Maher M; Kassab AE; Kassab AE; Zaher AF; Zaher AF; Mahmoud Z; Mahmoud Z
- Source:
Journal of enzyme inhibition and medicinal chemistry [J Enzyme Inhib Med Chem] 2019 Dec; Vol. 34 (1), pp. 532-546.- Publication Type:
Journal Article- Language:
English - Source:
- Additional Information
- Source: Publisher: Taylor & Francis Country of Publication: England NLM ID: 101150203 Publication Model: Print Cited Medium: Internet ISSN: 1475-6374 (Electronic) Linking ISSN: 14756366 NLM ISO Abbreviation: J Enzyme Inhib Med Chem Subsets: MEDLINE
- Publication Information: Original Publication: Basingstoke, UK : Taylor & Francis, c2002-
- Subject Terms: Drug Design*; Antineoplastic Agents/*pharmacology ; Apoptosis/*drug effects ; Caspase 3/*metabolism ; Protein Kinase Inhibitors/*pharmacology ; Pyrazoles/*pharmacology ; Pyrimidines/*pharmacology ; Receptor, ErbB-2/*antagonists & inhibitors; Antineoplastic Agents/chemical synthesis ; Antineoplastic Agents/chemistry ; Cell Cycle Checkpoints/drug effects ; Cell Proliferation/drug effects ; Dose-Response Relationship, Drug ; Drug Screening Assays, Antitumor ; ErbB Receptors/antagonists & inhibitors ; ErbB Receptors/metabolism ; Humans ; Molecular Structure ; Protein Kinase Inhibitors/chemical synthesis ; Protein Kinase Inhibitors/chemistry ; Pyrazoles/chemical synthesis ; Pyrazoles/chemistry ; Pyrimidines/chemical synthesis ; Pyrimidines/chemistry ; Receptor, ErbB-2/metabolism ; Structure-Activity Relationship ; Tumor Cells, Cultured
- Abstract: A series of novel pyrazolo[3,4-d]pyrimidines was synthesised. Twelve synthesised compounds were evaluated for their anticancer activity against 60 human tumour cell lines by NCI (USA). Compound 7d proved prominent anticancer activity. It showed 1.6-fold more potent anti-proliferative activity against OVCAR-4 cell line with IC
50 = 1.74 μM. It also exhibited promising potent anticancer activity against ACHN cell line with IC50 value 5.53 μM, representing 2.2-fold more potency than Erlotinib. Regarding NCI-H460 cell line, compound 7d (IC50 = 4.44 μM) was 1.9-fold more potent than Erlotinib. It inhibited EGFR and ErbB2 kinases at sub-micromolar level (IC50 = 0.18 and 0.25 µM, respectively). Dual inhibition of EGFR and ErbB2 caused induction of apoptosis which was confirmed by a significant increase in the level of active caspase-3 (11-fold). It showed accumulation of cells in pre-G1 phase and cell cycle arrest at G2/M phase. - References: Int J Biochem Cell Biol. 1999 Jun;31(6):637-43. (PMID: 10404636)
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Science. 1998 Jul 24;281(5376):533-8. (PMID: 9677190) - Contributed Indexing: Keywords: EGFR; ErbB2; Pyrazolo[3,4-d]pyrimidines; anticancer activity; apoptosis; caspase-3; cell cycle arrest profile; design; synthesis
- Accession Number: 0 (Antineoplastic Agents)
0 (Protein Kinase Inhibitors)
0 (Pyrazoles)
0 (Pyrimidines)
EC 2.7.10.1 (EGFR protein, human)
EC 2.7.10.1 (ErbB Receptors)
EC 2.7.10.1 (Receptor, ErbB-2)
EC 3.4.22.- (CASP3 protein, human)
EC 3.4.22.- (Caspase 3) - Publication Date: Date Created: 20190129 Date Completed: 20190507 Latest Revision: 20200225
- Publication Date: 20240104
- Accession Number: PMC6352943
- Accession Number: 10.1080/14756366.2018.1564046
- Accession Number: 30688116
- Source:
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