Synthesis, biological evaluation and molecular modeling study of [1, 2, 4]-Triazolo [4, 3-c] quinazolines: New class of EGFR-TK inhibitors
Abstract New series of triazolo [4, 3-c] quinazolines were designed, synthesized and their
structures were elucidated using different spectroscopic techniques. They were evaluated …
structures were elucidated using different spectroscopic techniques. They were evaluated …
Design, synthesis, anticancer, and antibacterial evaluation of some quinazolinone‐based derivatives as DHFR inhibitors
Two series of quinazolinone derivatives were designed and synthesized as dihydrofolate
reductase (DHFR) inhibitors. All compounds were evaluated for their antibacterial and …
reductase (DHFR) inhibitors. All compounds were evaluated for their antibacterial and …
Novel sulfonyl thiazolyl-hydrazone derivatives as EGFR inhibitors: Design, synthesis, biological evaluation and molecular docking studies
TA Farghaly, EMH Abbas, AM Al-Soliemy, R Sabour… - Bioorganic …, 2022 - Elsevier
New hydrazonoyl-sulfonylthiazoles were designed and synthesized as EGFR inhibitors. The
new sulfonylthiazole derivatives were assessed in vitro to measure their effect on EGFR …
new sulfonylthiazole derivatives were assessed in vitro to measure their effect on EGFR …
Design, synthesis and antitumor activity of novel pyrazolo [3, 4-d] pyrimidine derivatives as EGFR-TK inhibitors
MA Abdelgawad, RB Bakr, OA Alkhoja… - Bioorganic chemistry, 2016 - Elsevier
Abstract A novel series of 2-(3, 6-dimethyl-1-phenyl-1H-pyrazolo [3, 4-d] pyrimidin-4-yloxy)-
N-(4-substitutedbenzylidene) acetohydrazide (12a–g) was prepared and their structures …
N-(4-substitutedbenzylidene) acetohydrazide (12a–g) was prepared and their structures …
Discovery of thiapyran-pyrimidine derivatives as potential EGFR inhibitors
Z Xiao, C Chu, L Zhou, Z Zhou, Q Zhang, F Yang… - Bioorganic & Medicinal …, 2020 - Elsevier
A series of novel thiapyran-pyrimidine derivatives (10a–10h, 11a–11g, 12a–12f, 13a–13f,
14a–14f) were synthesized and their antiproliferative activities were tested. Most of the target …
14a–14f) were synthesized and their antiproliferative activities were tested. Most of the target …
Novel 4-(2-arylidenehydrazineyl) thienopyrimidine derivatives as anticancer EGFR inhibitors: Design, synthesis, biological evaluation, kinome selectivity and in silico …
HA Elsebaie, EA El-Bastawissy, KM Elberembally… - Bioorganic …, 2023 - Elsevier
The current study discovered fifteen new thieno [2, 3-d] pyrimidine derivatives with potential
anticancer action, including 5a-l, 6, and 7a-b. Results from the NCI screening revealed that …
anticancer action, including 5a-l, 6, and 7a-b. Results from the NCI screening revealed that …
Design, synthesis, in vitro antiproliferative evaluation and in silico studies of new VEGFR-2 inhibitors based on 4-piperazinylquinolin-2 (1H)-one scaffold
Angiogenesis is essential in the growth of solid tumors which need oxygen and nutrients
supply to grow in size. The VEGF/VEGFR-2 signaling pathway plays an important role in …
supply to grow in size. The VEGF/VEGFR-2 signaling pathway plays an important role in …
Design, synthesis, and anti-cancer evaluation of new pyrido [2, 3-d] pyrimidin-4 (3H)-one derivatives as potential EGFRWT and EGFRT790M inhibitors and apoptosis …
HSA Elzahabi, ES Nossier, RA Alasfoury… - Journal of Enzyme …, 2022 - Taylor & Francis
A new series of pyrido [2, 3-d] pyrimidin-4 (3H)-one derivatives having the essential
pharmacophoric features of EGFR inhibitors has been designed and synthesised. Cell …
pharmacophoric features of EGFR inhibitors has been designed and synthesised. Cell …
New series of isoxazole derivatives targeting EGFR-TK: Synthesis, molecular modeling and antitumor evaluation
New series of isoxazole derivatives were synthesized and evaluated for in vitro antitumor
activity against HepG2, MCF-7 and HCT-116 cancer cells. Results showed that 4b and 25a …
activity against HepG2, MCF-7 and HCT-116 cancer cells. Results showed that 4b and 25a …
Synthesis, anticancer activity and molecular modeling studies of 1, 2, 4-triazole derivatives as EGFR inhibitors
HAM El-Sherief, BGM Youssif, SNA Bukhari… - European journal of …, 2018 - Elsevier
A series of novel compounds carrying 1, 2, 4-triazole scaffold were prepared and evaluated
for their antiproliferative activities against NCI 60 cell line. Compounds 10 (a, c), 11 (ad), and …
for their antiproliferative activities against NCI 60 cell line. Compounds 10 (a, c), 11 (ad), and …