Design, synthesis and anticancer evaluation of thieno [2, 3-d] pyrimidine derivatives as dual EGFR/HER2 inhibitors and apoptosis inducers
SA Elmetwally, KF Saied, IH Eissa, EB Elkaeed - Bioorganic chemistry, 2019 - Elsevier
Deregulation of many kinases is directly linked to cancer development and the tyrosine
kinase family is one of the most important targets in current cancer therapy regimens. In this …
kinase family is one of the most important targets in current cancer therapy regimens. In this …
Novel 4-(2-arylidenehydrazineyl) thienopyrimidine derivatives as anticancer EGFR inhibitors: Design, synthesis, biological evaluation, kinome selectivity and in silico …
HA Elsebaie, EA El-Bastawissy, KM Elberembally… - Bioorganic …, 2023 - Elsevier
The current study discovered fifteen new thieno [2, 3-d] pyrimidine derivatives with potential
anticancer action, including 5a-l, 6, and 7a-b. Results from the NCI screening revealed that …
anticancer action, including 5a-l, 6, and 7a-b. Results from the NCI screening revealed that …
Design, synthesis and biological evaluation of a new series of thiazolyl-pyrazolines as dual EGFR and HER2 inhibitors
Epidermal growth factor receptor (EGFR, also known as HER1) and HER2, prominent
members of receptor tyrosine kinase (RTK) superfamily, have been reported as diagnostic or …
members of receptor tyrosine kinase (RTK) superfamily, have been reported as diagnostic or …
Design, synthesis and anticancer evaluation of 1H-pyrazolo [3, 4-d] pyrimidine derivatives as potent EGFRWT and EGFRT790M inhibitors and apoptosis inducers
In our attempt to develop effective EGFR-TKIs, two series of 1H-pyrazolo [3, 4-d] pyrimidine
derivatives were designed and synthesized. All the newly synthesized compounds were …
derivatives were designed and synthesized. All the newly synthesized compounds were …
Discovery of new pyrimidine-5-carbonitrile derivatives as anticancer agents targeting EGFR WT and EGFR T790M
A new series of pyrimidine-5-carbonitrile derivatives has been designed as ATP mimicking
tyrosine kinase inhibitors of the epidermal growth factor receptor (EGFR). These compounds …
tyrosine kinase inhibitors of the epidermal growth factor receptor (EGFR). These compounds …
Design, synthesis, molecular docking and antiproliferative activity of some novel benzothiazole derivatives targeting EGFR/HER2 and TS
Multi-targeted anticancer drugs are in focus as a promising research topic. A new series of
benzothiazoles hybridized with pyrimidine moiety was designed and synthesized using the …
benzothiazoles hybridized with pyrimidine moiety was designed and synthesized using the …
New pyrimidine and pyrazole-based compounds as potential EGFR inhibitors: Synthesis, anticancer, antimicrobial evaluation and computational studies
IMM Othman, ZM Alamshany, NY Tashkandi… - Bioorganic …, 2021 - Elsevier
This study was focused on the synthesis of new pyrimidines 4a, b, 5a, b and pyrazoles 6a, b
as ATP mimicking tyrosine kinase inhibitors of the epidermal growth factor receptor (EGFR) …
as ATP mimicking tyrosine kinase inhibitors of the epidermal growth factor receptor (EGFR) …
New thiazole-based derivatives as EGFR/HER2 and DHFR inhibitors: Synthesis, molecular modeling simulations and anticancer activity
New series of thiazole and imidazo [2, 1-b] thiazole derivatives were synthesized and tested
for their in vitro anticancer activity. Compounds 27, 34, 39 and 42–44 showed the best …
for their in vitro anticancer activity. Compounds 27, 34, 39 and 42–44 showed the best …
Discovery of new 1H-pyrazolo[3,4-d]pyrimidine derivatives as anticancer agents targeting EGFRWT and EGFRT790M
Abstract New 1 H-pyrazolo [3, 4-d] pyrimidine derivatives were designed and synthesised to
act as epidermal growth factor receptor inhibitors (EGFRIs). The synthesised derivatives …
act as epidermal growth factor receptor inhibitors (EGFRIs). The synthesised derivatives …
Design, synthesis, biological evaluation, QSAR analysis and molecular modelling of new thiazol-benzimidazoles as EGFR inhibitors
AM Srour, NS Ahmed, SS Abd El-Karim… - Bioorganic & Medicinal …, 2020 - Elsevier
Heterocyclic rings such as thiazole and benzimidazole are considered as privileged
structures, since they constitute several FDA-approved drugs for cancer treatment. In this …
structures, since they constitute several FDA-approved drugs for cancer treatment. In this …
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