Design, synthesis, in vitro biological assessment and molecular modeling insights for novel 3-(naphthalen-1-yl)-4, 5-dihydropyrazoles as anticancer agents with …

WM Eldehna, MA El Hassab, ZM Elsayed, T Al-Warhi… - Scientific reports, 2022 - nature.com
Currently, the humanity is in a fierce battle against various health-related challenges
especially those associated with human malignancies. This created the urge to develop …

Novel 4-thiophenyl-pyrazole, pyridine, and pyrimidine derivatives as potential antitumor candidates targeting both EGFR and VEGFR-2; design, synthesis, biological …

SM Al-Muntaser, AA Al-Karmalawy, AM El-Naggar… - RSC …, 2023 - pubs.rsc.org
In this article, we continued our previous effort to develop new selective anticancer
candidates based on the basic pharmacophoric requirements of both EGFR and VEGFR-2 …

Novel 2-(5-Aryl-4, 5-dihydropyrazol-1-yl) thiazol-4-one as EGFR inhibitors: synthesis, biological assessment and molecular docking insights

T Al-Warhi, AM El Kerdawy, MA Said… - Drug Design …, 2023 - Taylor & Francis
Introduction Epidermal growth factor receptor (EGFR) regulates several cell functions which
include cell growth, survival, multiplication, differentiation, and apoptosis. Currently, EGFR …

The anticancer and EGFR-TK/CDK-9 dual inhibitory potentials of new synthetic pyranopyrazole and pyrazolone derivatives: X-ray crystallography, in vitro, and in silico …

A Musa, SK Ihmaid, DL Hughes, MA Said… - Journal of …, 2023 - Taylor & Francis
Abstract Treatment options for the management of breast cancer are still inadequate. This
inadequacy is attributed to the lack of effective targeted medications, often resulting in the …

New thiazole-based derivatives as EGFR/HER2 and DHFR inhibitors: Synthesis, molecular modeling simulations and anticancer activity

MA Sabry, MA Ghaly, AR Maarouf… - European Journal of …, 2022 - Elsevier
New series of thiazole and imidazo [2, 1-b] thiazole derivatives were synthesized and tested
for their in vitro anticancer activity. Compounds 27, 34, 39 and 42–44 showed the best …

Novel 1, 3, 5-triazine-based pyrazole derivatives as potential antitumor agents and EFGR kinase inhibitors: Synthesis, cytotoxicity, DNA binding, molecular docking …

MS Raghu, CBP Kumar, MK Prashanth… - New Journal of …, 2021 - pubs.rsc.org
We herein report the design and synthesis of new 1, 3, 5-triazine-based pyrazole derivatives
(5a–i) with anticancer activity targeting the epidermal growth factor (EGFR) tyrosine kinase …

Naproxen based 1, 3, 4-oxadiazole derivatives as EGFR inhibitors: Design, synthesis, anticancer, and computational studies

MM Alam, S Nazreen, ASA Almalki, AA Elhenawy… - Pharmaceuticals, 2021 - mdpi.com
A library of novel naproxen based 1, 3, 4-oxadiazole derivatives (8–16 and 19–26) has been
synthesized and screened for cytotoxicity as EGFR inhibitors. Among the synthesized …

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 …

Design, synthesis, and SAR studies of novel 4-methoxyphenyl pyrazole and pyrimidine derivatives as potential dual tyrosine kinase inhibitors targeting both EGFR …

AM El-Naggar, AMA Hassan, EB Elkaeed… - Bioorganic …, 2022 - Elsevier
Guided by the pharmacophoric features of both EGFR and VEGFR-2 antagonists, two novel
series of 4-methoxyphenyl pyrazole and pyrimidine derivatives [(4a-c) and (5a-c, 6, 7a-c, 8 …

Synthesis, structure‐activity relationship and in silico studies of novel pyrazolothiazole and thiazolopyridine derivatives as prospective antimicrobial and anticancer …

IMM Othman, MAM Gad‐Elkareem… - …, 2021 - Wiley Online Library
In our attempt to develop potential new drug candidates with promising dual antimicrobial
and anticancer activities, a series of pyrazolothiazole and thiazolopyridine analogues has …