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

被引：49

作者：

Alafeefy, Ahmed M. ^{[1
]}

Alqasoumi, Saleh I. ^{[2
]}

Ashour, Abdelkader E. ^{[3
]}

Masand, Vijay ^{[4
]}

Al-Jaber, Nabila A. ^{[5
,6
]}

Ben Hadda, Taibi ^{[7
]}

Mohamed, Menshawy A. ^{[1
,8
]}

机构：

[1] Salman Bin Abdulaziz Univ, Coll Pharm, Dept Pharmaceut Chem, Alkharj 11942, Saudi Arabia

[2] King Saud Univ, Coll Pharm, Dept Pharmacognosy, Riyadh 11451, Saudi Arabia

[3] King Saud Univ, Coll Pharm, Dept Pharmacol & Toxicol, Riyadh 11451, Saudi Arabia

[4] Vidya Bharati Coll, Dept Chem, Amravati 444602, Maharashtra, India

[5] King Saud Univ, Coll Sci, Dept Chem, Women Students Med Studies Sect, Riyadh 11495, Saudi Arabia

[6] King Saud Univ, Coll Sci, Dept Chem, Sci Sect, Riyadh 11495, Saudi Arabia

[7] Univ Mohammed Premier, Fac Sci, Lab Chim Mat, Oujda 60000, Morocco

[8] Al Azhar Univ, Fac Pharm, Dept Organ Chem, Cairo 11884, Egypt

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2012年 / 53卷

关键词：

Quinazolin-4-(3H)-one; Tyrphostin; MTT assay; Cytotoxicity; POM analysis; SULFONAMIDE; DESIGN;

D O I：

10.1016/j.ejmech.2012.03.044

中图分类号：

R914 [药物化学];

学科分类号：

100705 [微生物与生化药学];

摘要：

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. (C) 2012 Elsevier Masson SAS. All rights reserved.

引用

页码：133 / 140

页数：8

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