An outlook of docking analysis and structure-activity relationship of pyrimidine-based analogues as EGFR inhibitors against non-small cell lung cancer (NSCLC)
Almost 80% of lung cancer diagnoses each year correspond to non-small cell lung cancer
(NSCLC). The percentage of NSCLC with EGFR overexpression ranges from 40% to 89 …
(NSCLC). The percentage of NSCLC with EGFR overexpression ranges from 40% to 89 …
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 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 …
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 …
Design, synthesis, molecular modeling and anti-proliferative evaluation of novel quinoxaline derivatives as potential DNA intercalators and topoisomerase II inhibitors
Abstract New series of [1, 2, 4] triazolo [4, 3-a] quinoxaline and bis ([1, 2, 4] triazolo)[4, 3-a:
3′, 4′-c] quinoxaline derivatives have been designed, synthesized and biologically …
3′, 4′-c] quinoxaline derivatives have been designed, synthesized and biologically …
Discovery of new 1H-pyrazolo[3,4-d]pyrimidine derivatives as anticancer agents targeting EGFRWT and EGFRT790M
AA Gaber, M Sobhy, A Turky… - Journal of Enzyme …, 2022 - Taylor & Francis
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, and anti-cancer evaluation of new pyrido [2, 3-d] pyrimidin-4 (3H)-one derivatives as potential EGFRWT and EGFRT790M inhibitors and apoptosis …
HSA Elzahabi, ES Nossier, RA Alasfoury… - Journal of Enzyme …, 2022 - Taylor & Francis
A new series of pyrido [2, 3-d] pyrimidin-4 (3H)-one derivatives having the essential
pharmacophoric features of EGFR inhibitors has been designed and synthesised. Cell …
pharmacophoric features of EGFR inhibitors has been designed and synthesised. Cell …
Design, synthesis, anticancer activity and molecular docking of novel 1H-benzo [d] imidazole derivatives as potential EGFR inhibitors
CE Theodore, G Sivaiah, SBB Prasad… - Journal of Molecular …, 2023 - Elsevier
Here, we present the design, synthesis, and evaluation of a new series of 1H-benzo [d]
imidazole derivatives (10a–j) to determine their anticancer efficacy. The MCF-7 and HCT116 …
imidazole derivatives (10a–j) to determine their anticancer efficacy. The MCF-7 and HCT116 …
ADMET profiling of geographically diverse phytochemical using chemoinformatic tools
Aim: Phytocompounds are important due to their uniqueness, however, only few reach the
development phase due to their poor pharmacokinetics. Therefore, preassessing the …
development phase due to their poor pharmacokinetics. Therefore, preassessing the …
Identification of vinyl sulfone derivatives as EGFR tyrosine kinase inhibitor: in vitro and in silico studies
T Aiebchun, P Mahalapbutr, A Auepattanapong… - Molecules, 2021 - mdpi.com
Epidermal growth factor receptor (EGFR), overexpressed in many types of cancer, has been
proved as a high potential target for targeted cancer therapy due to its role in regulating …
proved as a high potential target for targeted cancer therapy due to its role in regulating …