A Green Mechanochemical One-Pot Three-Component Domino Reaction Synthesis of Polysubstituted Azoloazines Containing Benzofuran Moiety: Cytotoxic Activity Against HePG2 Cell Lines

被引：3

作者：

Mokhtar, Mohamed ^{[1
,2
]}

Saleh, Tamer S. ^{[2
,3
]}

Ahmed, Nesreen S. ^{[1
,2
]}

Al-Bogami, Abdullah S. ^{[3
]}

机构：

[1] King Abdulaziz Univ, Fac Sci, Chem Dept, POB 80203, Jeddah 21589, Saudi Arabia

[2] Natl Res Ctr, Dept Med Chem, Phys Chem Dept, Green Chem Dept, Cairo, Egypt

[3] Univ Jeddah, Fac Sci, Chem Dept, Jeddah, Saudi Arabia

来源：

POLYCYCLIC AROMATIC COMPOUNDS | 2020年 / 40卷 / 03期

关键词：

Azoloazines; ball milling; benzofuran; cytotoxic activity; green protocol; magadiite; ULTRASOUND PROMOTED SYNTHESIS; MULTICOMPONENT SYNTHESES; SUBSTITUTED PYRAZOLES; HETEROCYCLES; DERIVATIVES; TRANSITION; INHIBITORS; TOXICITY;

D O I：

10.1080/10406638.2018.1464036

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

A one-pot procedure for the synthesis of azolopyrimidine derivatives by a three-component reaction of beta-ketosulfone, aldehyde, and 2-aminoben-zimidazole over synthetic magadiite clay (SMC-H) under ball milling in the absence of any solvent and additive has been developed. The catalyst was re-used for consequent reactions. The novel manufactured compounds were verified for HePG2 cell development inhibition. A pronounced inhibitory effect on the growth of HePG2 cell line was recorded. This protocol offers a broad scope for an access to a variety of diversely substituted azolopyrimidines of high inhibition activity against HePG2 cell line. The use of non-hazardous organic solvent, ball milling, cost efficiency, recyclability of the catalyst up to six runs without appreciable loss of activity, and high yields of products make this procedure greener.

引用

页码：594 / 608

页数：15

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