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 …

HAM Gomaa, ME Shaker, SI Alzarea, OM Hendawy… - Bioorganic …, 2022 - Elsevier
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 …

Design and synthesis of novel 2, 3-dihydropyrazino [1, 2-a] indole-1, 4-dione derivatives as antiproliferative EGFR and BRAFV600E dual inhibitors

LH Al-Wahaibi, AM Gouda, OF Abou-Ghadir… - Bioorganic …, 2020 - Elsevier
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 …

Design, Synthesis, Antiproliferative Actions, and DFT Studies of New Bis–Pyrazoline Derivatives as Dual EGFR/BRAFV600E Inhibitors

LH Al-Wahaibi, HA Abou-Zied, EAM Beshr… - International Journal of …, 2023 - mdpi.com
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 …

Design, Synthesis, and Anti-Proliferative Action of Purine/Pteridine-Based Derivatives as Dual Inhibitors of EGFR and BRAFV600E

SA El-Kalyoubi, HAM Gomaa, EMN Abdelhafez… - Pharmaceuticals, 2023 - mdpi.com
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 …

New Thiazolyl-Pyrazoline derivatives as potential dual EGFR/HER2 inhibitors: design, synthesis, anticancer activity evaluation and in silico study

MM Fakhry, AA Mattar, M Alsulaimany, EM Al-Olayan… - Molecules, 2023 - mdpi.com
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 …

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 …

Design, synthesis and biological evaluation of a new series of thiazolyl-pyrazolines as dual EGFR and HER2 inhibitors

B Sever, MD Altıntop, MO Radwan, A Özdemir… - European journal of …, 2019 - Elsevier
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 …

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] …

Design and synthesis of new thiazolidinone/uracil derivatives as antiproliferative agents targeting EGFR and/or BRAFV600E

MB Alshammari, AA Aly, BGM Youssif, S Bräse… - Frontiers in …, 2022 - frontiersin.org
Thiourea derivatives of uracil were efficiently synthesized via the reaction of 5-aminouracil
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

Y Tu, C Wang, S Xu, Z Lan, W Li, J Han, Y Zhou… - Bioorganic & medicinal …, 2017 - Elsevier
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 …