Quinazoline–tyrphostin as a new class of antitumor agents, molecular properties prediction, synthesis and biological testing

A new series of substituted quinazolin-4-(3H)-one-tyrphostin derivatives was prepared and screened for their cytotoxic activity against three tumor cell lines, namely human breast cancer cell line (MCF-7), human cervical cancer cell line (HeLa) and human hepatocellular liver carcinoma cell line (HepG2) using the colorimetric MTT assay. Among the current series, 10 compounds exhibited remarkable in vitro antiproliferative activity against the three tested cell lines with the IC50 values ranging from 0.009 to 0.015 mM. All the compounds showed suitable drug like characteristics according to Lipinski's rule.

General structures of the target compounds 4–23 and the model tyrphostin AG 99.Figure optionsDownload as PowerPoint slideHighlights
► Novel quinazoline–tyrphostin compounds with suitable drug like properties.
► Seven derivatives showed remarkable cytotoxic activity mostly as the standard drug.
► The reported compounds possessed moderate to good drug score.
► These compounds, are expected to present good bioavailability profile.