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 …
Therapeutic strategies of dual-target small molecules to overcome drug resistance in cancer therapy
J Ye, J Wu, B Liu - Biochimica et Biophysica Acta (BBA)-Reviews on …, 2023 - Elsevier
Despite some advances in targeted therapeutics of human cancers, curative cancer
treatment still remains a tremendous challenge due to the occurrence of drug resistance. A …
treatment still remains a tremendous challenge due to the occurrence of drug resistance. A …
Synthesis, biological evaluation, and molecular docking of novel azolylhydrazonothiazoles as potential anticancer agents
A novel set of thiazolylhydrazonothiazoles bearing an indole moiety were synthesized by
subjection reactions of carbothioamide derivative and hydrazonoyl chlorides (or α …
subjection reactions of carbothioamide derivative and hydrazonoyl chlorides (or α …
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 …
Design, synthesis, and biological evaluation of novel EGFR inhibitors containing 5-chloro-3-hydroxymethyl-indole-2-carboxamide scaffold with apoptotic …
New EGFR inhibitor series of fifteen 5-chloro-3-hydroxymethyl-indole-2-carboxamide
derivatives has been designed, synthesized, and tested for antiproliferative activity against a …
derivatives has been designed, synthesized, and tested for antiproliferative activity against a …
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 …
Design, synthesis, and biological evaluation of new pyrimidine-5-carbonitrile derivatives bearing 1, 3-thiazole moiety as novel anti-inflammatory EGFR inhibitors with …
A new series of pyrimidine-5-carbonitrile derivatives 8a-p carrying the 1, 3-thiazole moiety
has been designed and synthesized as novel anti-inflammatory EGFR inhibitors with cardiac …
has been designed and synthesized as novel anti-inflammatory EGFR inhibitors with cardiac …
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 …
Design, synthesis, and antibacterial evaluation of new quinoline-1, 3, 4-oxadiazole and quinoline-1, 2, 4-triazole hybrids as potential inhibitors of DNA gyrase and …
HA Hofny, MFA Mohamed, HAM Gomaa… - Bioorganic …, 2021 - Elsevier
DNA gyrase and topoisomerase IV (topo IV) inhibitors are among the most interesting
antibacterial drug classes without antibacterial pipeline representative. Twenty-four new …
antibacterial drug classes without antibacterial pipeline representative. Twenty-four new …
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 …