[HTML][HTML] Globally approved EGFR inhibitors: Insights into their syntheses, target kinases, biological activities, receptor interactions, and metabolism
Targeting the EGFR with small-molecule inhibitors is a confirmed valid strategy in cancer
therapy. Since the FDA approval of the first EGFR-TKI, erlotinib, great efforts have been …
therapy. Since the FDA approval of the first EGFR-TKI, erlotinib, great efforts have been …
A comprehensive review of recent advances in the biological activities of 1, 2, 4‐oxadiazoles
OM Hendawy - Archiv der Pharmazie, 2022 - Wiley Online Library
Nitrogen heterocycles play an essential role in medication development. The 1, 2, 4‐
oxadiazole heterocycle has been extensively studied, yielding a large variety of molecules …
oxadiazole heterocycle has been extensively studied, yielding a large variety of molecules …
Optimization and SAR investigation of novel 2, 3-dihydropyrazino [1, 2-a] indole-1, 4-dione derivatives as EGFR and BRAFV600E dual inhibitors with potent …
Using a single drug to treat cancer with dual-targeting is an unusual approach when
compared to other drug combinations. Dual-targeting agents were developed as a result of …
compared to other drug combinations. Dual-targeting agents were developed as a result of …
Novel pyrazole-based COX-2 inhibitors as potential anticancer agents: Design, synthesis, cytotoxic effect against resistant cancer cells, cell cycle arrest, apoptosis …
Novel differently substituted pyrazole derivatives were designed, synthesized and evaluated
for their anticancer activity. All compounds selectively inhibited COX-2 enzyme (IC 50 …
for their anticancer activity. All compounds selectively inhibited COX-2 enzyme (IC 50 …
Design and synthesis of new triarylimidazole derivatives as dual inhibitors of BRAFV600E/p38α with potential antiproliferative activity
Recent studies have shown that combining kinase inhibitors has additive and synergistic
effects. BRAF V600E and p38α have been extensively studied as potential therapeutic …
effects. BRAF V600E and p38α have been extensively studied as potential therapeutic …
Discovery of new pyrimido [5, 4-c] quinolines as potential antiproliferative agents with multitarget actions: Rapid synthesis, docking, and ADME studies
RA Mekheimer, SMR Allam, MA Al-Sheikh… - Bioorganic …, 2022 - Elsevier
A novel series of pyrimido [5, 4-c] quinoline derivatives variously substituted at positions 2
and 5 have been synthesized, in good to excellent yields, via rapid base-catalyzed …
and 5 have been synthesized, in good to excellent yields, via rapid base-catalyzed …
New 1, 3, 4‐oxadiazoles linked with the 1, 2, 3‐triazole moiety as antiproliferative agents targeting the EGFR tyrosine kinase
Abstract A series of 1, 3, 4‐oxadiazole‐1, 2, 3‐triazole hybrids bearing different
pharmacophoric moieties has been designed and synthesized. Their antiproliferative activity …
pharmacophoric moieties has been designed and synthesized. Their antiproliferative activity …
Structure-based design, synthesis and antiproliferative action of new quinazoline-4-one/chalcone hybrids as EGFR inhibitors
A new series of quinazoline-4-one/chalcone hybrids, 7–26, was synthesized in this study as
EGFR inhibitors with antiproliferative activity. Target compounds were synthesized and in …
EGFR inhibitors with antiproliferative activity. Target compounds were synthesized and in …
Novel piperine-carboximidamide hybrids: Design, synthesis, and antiproliferative activity via a multi-targeted inhibitory pathway
A new series of piperine-carboximidamide hybrids VIa-k was developed as a new cytotoxic
agent targeting EGFR, BRAF, and CDK2. The antiproliferative effect against four cancer cells …
agent targeting EGFR, BRAF, and CDK2. The antiproliferative effect against four cancer cells …
[HTML][HTML] Design and synthesis of new thiazolidinone/uracil derivatives as antiproliferative agents targeting EGFR and/or BRAFV600E
Thiourea derivatives of uracil were efficiently synthesized via the reaction of 5-aminouracil
with isothiocyanates. Then, we prepared uracil-containing thiazoles via condensation of …
with isothiocyanates. Then, we prepared uracil-containing thiazoles via condensation of …