Synthesis, Molecular Dynamics Simulation, and In-vitro Antitumor Activity of Quinazoline-2,4,6-triamine Derivatives as Novel EGFR Tyrosine Kinase Inhibitors.

ABSTRACT:

Background

Developing a potent and safe scaffold is challenging in anti-cancer drug discovery.

Objectives

The study focused on developing novel series of compounds based on the inhibition of epidermal growth factor receptor tyrosine kinase (EGFR-TK) as one of the most promising compounds in cancer therapy.

Methods

In this study, a novel series of quinazoline-2,4,6-triamine derivatives were designed and synthesized through intramolecular C-H activation reaction of para-nitro aniline, trichloroacetonitrile, and isocyanides employing a one-pot reaction.

Results

The in-vitro antitumor activities of the compounds which showed acceptable inhibitory effects were investigated against breast (MCF-7), lung (A-549), and colon (HT-29) cancer cell lines by emp

SUBMITTER: Nili Ahmadabadi M 

PROVIDER: S-EPMC10008000 | biostudies-literature | 2022 Dec

REPOSITORIES: biostudies-literature