Synthesis and biological evaluation of (S)-4-aminoquinazoline alcohols

被引：19

作者：

Cakici, Murat ^{[1
]}

Catir, Mustafa ^{[2
]}

Karabuga, Semistan ^{[3
]}

Kilic, Hamdullah ^{[1
]}

Ulukanli, Sabri ^{[4
]}

Gulluce, Medine ^{[5
]}

Orhan, Furkan ^{[5
]}

机构：

[1] Ataturk Univ, Fac Sci, Dept Chem, TR-25240 Erzurum, Turkey

[2] Erzincan Univ, Fac Arts & Sci, Dept Chem, TR-24100 Erzincan, Turkey

[3] Kills 7 Aral Univ, Fac Sci & Letters, Dept Chem, TR-79100 Kilis, Turkey

[4] Osmaniye Korkut Ata Univ, Fac Sci & Letters, Dept Chem, TR-80100 Osmaniye, Turkey

[5] Ataturk Univ, Fac Sci, Dept Biol, TR-25240 Erzurum, Turkey

来源：

TETRAHEDRON-ASYMMETRY | 2010年 / 21卷 / 16期

关键词：

MICROWAVE-ASSISTED SYNTHESIS; VITRO ANTITUMOR-ACTIVITY; 4-AMINOQUINAZOLINE DERIVATIVES; INHIBITORS; ALKALOIDS;

D O I：

10.1016/j.tetasy.2010.05.040

中图分类号：

O61 [无机化学];

学科分类号：

070301 ; 081704 ;

摘要：

A simple synthetic method for the preparation of enantiomerically pure (S)-4-aminoquinazoline alcohols from (S)-quinazolinone alcohols by key steps including chlorination, nucleophilic ipso substitution, and deacetylation is presented. Mutagenic and antimutagenic properties of the (S)-4-aminoquinazoline alcohols were investigated by using Salmonella typhimurium TA1535, and Escherichia colt WP2uvrA tester strains at 0.01, 0.1, and 1 mu g/plate concentrations. (S)-4-aminoquinazoline alcohols were found to be genotoxically safe at the tested concentrations. Among the tested (S)-4-aminoquinazoline alcohols, the best antimutagenic activity was obtained with a methyl derivative at 0.1 mu g/plate dose. (C) 2010 Elsevier Ltd. All rights reserved.

引用

页码：2027 / 2031

页数：5

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