Design, synthesis and biological evaluation of novel 3, 4-dihydro-2H-[1, 4] oxazino [2, 3-f] quinazolin derivatives as EGFR-TKIs

X Qin, P Liu, Y Li, L Hu, Y Liao, T Cao… - Bioorganic & Medicinal …, 2023 - Elsevier
Starting with our previously reported work, a novel series of 3, 4-dihydro-2H-[1, 4] oxazino [2,
3-f] quinazolin-derivatives were designed, synthesized and evaluated as potent EGFR …

In silico and in vitro studies of novel 7-azaindole and 7-azaisatin derivatives as potent anticancer agents

S Rekulapally, R Jarapula, K Gangarapu… - Medicinal Chemistry …, 2015 - Springer
A series of novel 7-azaindole (1a–j) and 7-azaisatin (2a–j) derivatives were screened for
their in vitro breast, lung and liver cytotoxic activities against MCF-7, A549 and HEPG2 cell …

Design, synthesis, and antiproliferative activities of novel substitutedhydrazone/triazolo-linked quinazoline derivatives

A El-Malah, AM Malebari, AN Khayyat… - Journal of Molecular …, 2024 - Elsevier
A series of novel hydrazonoquinazolines and triazoloquinazolines analogues of Erlotinib
were synthesized and evaluated for their antiproliferative as well as EGFR kinase inhibitory …

Synthesis of Quinoline‐Thiazolidine‐2, 4‐dione Coupled Pyrazoles as in vitro EGFR Targeting Anti‐Breast Cancer Agents and Their in silico Studies

M Bangaru, S Kumar Nukala, PK Kannekanti… - …, 2023 - Wiley Online Library
The synthesis of some new quinoline‐thiazolidine‐2, 4‐dione coupled pyrazoles (7 a–7 n)
via Knoevengal condensation, N‐alkynylation and tandem one‐pot Sonogashira coupling …

Novel quinoline-3-carboxamides (Part 2): Design, optimization and synthesis of quinoline based scaffold as EGFR inhibitors with potent anticancer activity

RM Aly, RAT Serya, AM El-Motwally, A Esmat… - Bioorganic …, 2017 - Elsevier
EGFR has a key role in cell growth. Its mutation and overexpression share in epithelial
malignancies and tumor growth. Quinazoline and quinoline derivatives are common …

Synthesis, molecular docking, in silico ADME, and EGFR kinase inhibitor activity studies of some new benzimidazole derivatives bearing thiosemicarbazide, triazole …

I Celik, G Ayhan‐Kılcıgil, A Karayel… - Journal of …, 2022 - Wiley Online Library
Epidermal growth factor receptor (EGFR), one of the important targets in the development of
the anticancer compound, is a member of the ErbB receptor tyrosine kinase receptor family …

Structure-based virtual screening, molecular docking, molecular dynamics simulation, and metabolic reactivity studies of quinazoline derivatives for their anti-EGFR …

AA Shah, S Ahmad, MK Yadav, K Raza… - Current Medicinal …, 2024 - ingentaconnect.com
Background: Epidermal growth factor receptor (EGFR/HER-1) and its role in tumor
development and progression through the mechanism of tumor angiogenesis is prevalent in …

Design, synthesis, and biological evaluation of novel EGFR inhibitors containing 5-chloro-3-hydroxymethyl-indole-2-carboxamide scaffold with apoptotic …

FAM Mohamed, HAM Gomaa, OM Hendawy, AT Ali… - Bioorganic …, 2021 - Elsevier
New EGFR inhibitor series of fifteen 5-chloro-3-hydroxymethyl-indole-2-carboxamide
derivatives has been designed, synthesized, and tested for antiproliferative activity against a …

Discovery and Anticancer Activity of Novel 1,3,4-Thiadiazole- and Aziridine-Based Indolin-2-ones via In Silico Design Followed by Supramolecular Green Synthesis

PJ Chaudhari, SB Bari, SJ Surana, AA Shirkhedkar… - ACS …, 2022 - ACS Publications
Three crucial anticancer scaffolds, namely indolin-2-one, 1, 3, 4-thiadiazole, and aziridine,
are explored to synthesize virtually screened target molecules based on the c-KIT kinase …

Design and synthesis of novel pyrazolopyrimidine candidates as promising EGFR-T790M inhibitors and apoptosis inducers

AA Gaber, M Sharaky, AA Elmaaty… - Future Medicinal …, 2023 - Taylor & Francis
Aim: Our objective was to design and synthesize a new range of pyrazolopyrimidines while
maintaining the key pharmacophoric features of EGFR tyrosine kinase inhibitors. Materials & …