New series of 4,6-diaryl pyrimidines: facile synthesis and antiproliferative activity as dual EGFR/VEGFR-2 inhibitors.

ABSTRACT:

Introduction

We developed and produced a new series of 4,6-diaryl-pyrimidines 9-29 as antiproliferative agents targeting EGFR/VEGFR-2.

Methods

The antiproliferative efficacy of the novel targets was assessed against a panel of 60 NCI cancer cell lines and four cancer cell lines in vitro.

Results and discussion

Compounds 14, 17, 19, 22, 25, and 29 demonstrated the greatest potency among the derivatives, with GI₅₀ values between 22 and 33 nM; compounds 22 and 29 exhibited the highest potency, with GI₅₀ values of 22 and 24 nM, respectively. We subsequently examined the most efficient derivatives as dual EGFR/VEGFR-2 inhibitors, finding that compounds 22 and 29 functi

SUBMITTER: Mostafa YA 

PROVIDER: S-EPMC11576293 | biostudies-literature | 2024

REPOSITORIES: biostudies-literature