Abstract

NOVEL 4-ANILINOQUINAZOLINE DERIVATIVES AS EGFR AND VEGFR-2 INHIBITORS

Nilam Bhusare*, Dr Laxman Kawale, Dr. Mahesh Dumbare and Vaibhav Kharat

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Abstract

The 4-anilinoquinazoline has a basic pharmacophore for tyrosine kinase inhibitors activity. The approach of synthesis of the 4- anilinoquinazoline derivative is easy, so a variety of substitutions are possible with their versatile medicinal applications. The derivatives of 4-anilinoquinazoline are designed dual inhibitors of an EGFR and VEGFR-2. EGFR and VEGFR-2 follow the same downstream signalling pathway of inhibition resulting in a synergistic effect. Derivatives of 4-anilinoquinazoline have a wide range of applications in medicinal chemistry like colon cancer, non-small cell lung cancer, prostate cancer and breast cancer. Docking study of the 4- anilinoquinazoline compounds also shows some good interactions with receptors. Now a day, numerous 4-anilinoquinazoline derivatives are available in the market such as gefitinib, dacomitinib, erlotinib and vandetanib. In future, more possible improvements in the activity can be achieved with various pharmacophoric substitutions. In this review, we have highlighted the novel 4-anilinoquinazoline derivatives with their EGFR and VEGFR-2 tyrosine kinase inhibition activity.

Keywords: 4-anilinoquinazoline, EGFR, VEGFR-2, Tyrosine Kinase Inhibitor.