Design, synthesis and biological evaluation of novel quinazoline derivatives as potential antitumor agents: molecular...

Area of Science:

• Medicinal Chemistry
• Oncology
• Molecular Pharmacology

Background:

• Epidermal Growth Factor Receptor (EGFR) is a key target in cancer therapy, especially in breast carcinoma.
• Quinazoline derivatives are a known class of compounds with potential anticancer properties.

Purpose of the Study:

• To synthesize novel quinazoline derivatives.
• To evaluate their antitumor activity against various human cancer cell lines.
• To investigate their potential as EGFR inhibitors.

Main Methods:

• Synthesis of 27 novel quinazoline derivatives.
• In vitro antitumor activity testing against human liver (HEPG2), breast (MCF-7), and cervix (HELA) cancer cell lines.
• In silico molecular docking into the ATP binding site of EGFR.

Main Results:

• All tested compounds exhibited potent and selective antitumor activity against MCF-7 cells (IC50: 3.35-6.81 μg/ml).
• Compounds 5, 9, 15, 18, and 20 displayed broad-spectrum activity against HEPG2, MCF-7, and HELA cells (IC50: 3.35-5.59 μg/ml).
• Docking studies suggested analogous binding modes to known EGFR inhibitors.

Conclusions:

• Novel quinazoline derivatives possess significant antitumor potential, especially against EGFR-expressing breast cancer.
• These compounds represent promising candidates for further development as anticancer agents.
• The findings support the role of EGFR as a therapeutic target for these novel compounds.