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 and synthesis of novel 2, 3-dihydropyrazino [1, 2-a] indole-1, 4-dione derivatives as antiproliferative EGFR and BRAFV600E dual inhibitors
Recent studies have shown additive and synergistic effects associated with the combination
of kinase inhibitors. BRAF V600E and EGFR are attractive targets for many diseases …
of kinase inhibitors. BRAF V600E and EGFR are attractive targets for many diseases …
Design, Synthesis, Antiproliferative Actions, and DFT Studies of New Bis–Pyrazoline Derivatives as Dual EGFR/BRAFV600E Inhibitors
Some new Bis-pyrazoline hybrids 8–17 with dual EGFR and BRAFV600E inhibitors have
been developed. The target compounds were synthesized and tested in vitro against four …
been developed. The target compounds were synthesized and tested in vitro against four …
Design, Synthesis, and Anti-Proliferative Action of Purine/Pteridine-Based Derivatives as Dual Inhibitors of EGFR and BRAFV600E
The investigation of novel EGFR and BRAFV600E dual inhibitors is intended to serve as
targeted cancer treatment. Two sets of purine/pteridine-based derivatives were designed …
targeted cancer treatment. Two sets of purine/pteridine-based derivatives were designed …
New Thiazolyl-Pyrazoline derivatives as potential dual EGFR/HER2 inhibitors: design, synthesis, anticancer activity evaluation and in silico study
A new series of thiazolyl-pyrazoline derivatives (4a–d, 5a–d 6a, b, 7a–d, 8a, b, and 10a, b)
have been designed and synthesized through the combination of thiazole and pyrazoline …
have been designed and synthesized through the combination of thiazole and pyrazoline …
Design, synthesis, and biological evaluation of indole-2-carboxamides as potential multi-target antiproliferative agents
LH Al-Wahaibi, AF Mohammed, MH Abdelrahman… - Pharmaceuticals, 2023 - mdpi.com
A small set of indole-based derivatives, IV and Va–I, was designed and synthesized.
Compounds Va–i demonstrated promising antiproliferative activity, with GI50 values ranging …
Compounds Va–i demonstrated promising antiproliferative activity, with GI50 values ranging …
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 …
Dual EGFR/HER2 inhibitors and apoptosis inducers: New benzo [g] quinazoline derivatives bearing benzenesulfonamide as anticancer and radiosensitizers
MM Ghorab, MS Alsaid, AM Soliman - Bioorganic Chemistry, 2018 - Elsevier
Dual targeting of EGFR and HER2 is a proven anticancer strategy for the treatment of solid
tumors. An array of new N-substituted-2-(4-oxo-3-(4-sulfamoylphenyl)-3, 4-dihydrobenzo [g] …
tumors. An array of new N-substituted-2-(4-oxo-3-(4-sulfamoylphenyl)-3, 4-dihydrobenzo [g] …
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 …
Design, synthesis, and docking studies of quinazoline analogues bearing aryl semicarbazone scaffolds as potent EGFR inhibitors
Two series of quinazoline derivatives bearing aryl semicarbazone scaffolds (9a–o and 10a–
o) were designed, synthesized and evaluated for the IC 50 values against four cancer cell …
o) were designed, synthesized and evaluated for the IC 50 values against four cancer cell …
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