Design, synthesis, molecular modeling and antitumor evaluation of novel indolyl-pyrimidine derivatives with EGFR inhibitory activity
Scaffolds hybridization is a well-known drug design strategy for antitumor agents. Herein,
series of novel indolyl-pyrimidine hybrids were synthesized and evaluated in vitro and in …
series of novel indolyl-pyrimidine hybrids were synthesized and evaluated in vitro and in …
3-Substituted-2, 3-dihydrothiazole as a promising scaffold to design EGFR inhibitors
R El-Haggar, SF Hammad, RI Alsantali, MM Alrooqi… - Bioorganic …, 2022 - Elsevier
The overexpression of EGFR has been recognized as the driver mechanism in the
development of several human malignancies and the clinical use of EGFR inhibitors …
development of several human malignancies and the clinical use of EGFR inhibitors …
Antitumor evaluation and molecular docking study of substituted 2-benzylidenebutane-1, 3-dione, 2-hydrazonobutane-1, 3-dione and trifluoromethyl-1H-pyrazole …
IA Al-Suwaidan, NI Abdel-Aziz, AS El-Azab… - Journal of Enzyme …, 2015 - Taylor & Francis
Abstract A series of 2-(arylidene)-1-(4-chlorophenyl)-4, 4, 4-trifluorobutane-1, 3-diones (2–
4), 4-(arylidene)-3-(4-chlorophenyl)-5-(trifluoromethyl)-4 H-pyrazoles (5–7), 1-(4 …
4), 4-(arylidene)-3-(4-chlorophenyl)-5-(trifluoromethyl)-4 H-pyrazoles (5–7), 1-(4 …
Design, synthesis and evaluation of novel Se-alkylated pyrazoles and their cyclized analogs as potential anticancer agents
A simple multicomponent reaction (MCR) was utilized to synthesize a series of 5-alkylated
selanyl-1H-pyrazole derivatives 3a-d, 6a-d, and their 4-amino-5-substituted selenolo [2, 3-c] …
selanyl-1H-pyrazole derivatives 3a-d, 6a-d, and their 4-amino-5-substituted selenolo [2, 3-c] …
Novel thienopyrimidine derivatives as dual EGFR and VEGFR-2 inhibitors: design, synthesis, anticancer activity and effect on cell cycle profile
Aim: Design and synthesis of thienopyrimidine derivatives as dual EGFR and VEGFR-2
inhibitors. Material and methods: A series of novel 6, 7, 8, 9-tetrahydro-5 H-cyclohepta [4, 5] …
inhibitors. Material and methods: A series of novel 6, 7, 8, 9-tetrahydro-5 H-cyclohepta [4, 5] …
Design, synthesis and anticancer evaluation of thieno [2, 3-d] pyrimidine derivatives as dual EGFR/HER2 inhibitors and apoptosis inducers
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, 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 …
Synthesis and biological evaluation of compounds which contain pyrazole, thiazole and naphthalene ring as antitumor agents
JW Yuan, SF Wang, ZL Luo, HY Qiu, PF Wang… - Bioorganic & medicinal …, 2014 - Elsevier
A series of compounds which contain pyrazole, thiazole and naphthalene ring (1a–7a, 1b–
7b, 1c–7c, 1d–7d) were firstly synthesized and their anti-proliferative activity, EGFR …
7b, 1c–7c, 1d–7d) were firstly synthesized and their anti-proliferative activity, EGFR …
Synthesis, antitumor activities, and molecular modeling of 4-anilinoquinazoline derivatives as EGFR-TK inhibitors
AH Mohammed, RM Gomaa, MAA El-Sayed… - Pharmaceutical …, 2023 - Springer
New compounds of 4-anilino-6-substituted quinazoline were designed, synthesized, and
tested for their EGFR-TK and tumor growth inhibitory activities. The synthesized compounds …
tested for their EGFR-TK and tumor growth inhibitory activities. The synthesized compounds …
Design, synthesis, and antiproliferative activity of new 5-chloro-indole-2-carboxylate and pyrrolo [3, 4-b] indol-3-one derivatives as potent inhibitors of egfrt790m …
LH Al-Wahaibi, AF Mohammed, MH Abdelrahman… - Molecules, 2023 - mdpi.com
Mutant EGFR/BRAF pathways are thought to be crucial targets for the development of
anticancer drugs since they are over-activated in several malignancies. We present here the …
anticancer drugs since they are over-activated in several malignancies. We present here the …