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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

Maher, Mai ; Kassab, Asmaa E. ; Zaher, Ashraf F. ; Mahmoud, Zeinab

Journal of enzyme inhibition and medicinal chemistry, 2019-01, Vol.34 (1), p.532-546 [Periódico revisado por pares]

England: Taylor & Francis

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Título:
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
Autor: Maher, Mai ; Kassab, Asmaa E. ; Zaher, Ashraf F. ; Mahmoud, Zeinab
Assuntos: anticancer activity ; Antineoplastic Agents - chemical synthesis ; Antineoplastic Agents - chemistry ; Antineoplastic Agents - pharmacology ; apoptosis ; Apoptosis - drug effects ; Caspase 3 - metabolism ; caspase-3 ; cell cycle arrest profile ; Cell Cycle Checkpoints - drug effects ; Cell Proliferation - drug effects ; design ; Dose-Response Relationship, Drug ; Drug Design ; Drug Screening Assays, Antitumor ; EGFR ; ErbB Receptors - antagonists & inhibitors ; ErbB Receptors - metabolism ; ErbB2 ; Humans ; Molecular Structure ; Protein Kinase Inhibitors - chemical synthesis ; Protein Kinase Inhibitors - chemistry ; Protein Kinase Inhibitors - pharmacology ; Pyrazoles - chemical synthesis ; Pyrazoles - chemistry ; Pyrazoles - pharmacology ; Pyrazolo[3,4-d]pyrimidines ; Pyrimidines - chemical synthesis ; Pyrimidines - chemistry ; Pyrimidines - pharmacology ; Receptor, ErbB-2 - antagonists & inhibitors ; Receptor, ErbB-2 - metabolism ; Research Paper ; Structure-Activity Relationship ; synthesis ; Tumor Cells, Cultured
É parte de: Journal of enzyme inhibition and medicinal chemistry, 2019-01, Vol.34 (1), p.532-546
Notas: ObjectType-Article-1
SourceType-Scholarly Journals-1
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Descrição: 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 IC 50 value 5.53 μM, representing 2.2-fold more potency than Erlotinib. Regarding NCI-H460 cell line, compound 7d (IC 50 = 4.44 μM) was 1.9-fold more potent than Erlotinib. It inhibited EGFR and ErbB2 kinases at sub-micromolar level (IC 50 = 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.
Editor: England: Taylor & Francis
Idioma: Inglês

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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

Maher, Mai ; Kassab, Asmaa E. ; Zaher, Ashraf F. ; Mahmoud, Zeinab

England: Taylor & Francis

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