Synthesis and Antiproliferative and Antimicrobial Activity of Methyl-6-Amino-3-Acyl-4-Aryl-5-Cyano-4H-Pyran-2-Carboxylates and their Derivatives

被引：18

作者：

Sheverdov, V. P. ^{[1
]}

Andreev, A. Yu. ^{[1
]}

Nasakin, O. E. ^{[1
]}

Gein, V. L. ^{[2
]}

机构：

[1] Ulyanov Chuvash State Univ, Cheboksary 428015, Russia

[2] Perm State Pharmaceut Acad, Perm 614990, Russia

来源：

PHARMACEUTICAL CHEMISTRY JOURNAL | 2014年 / 48卷 / 06期

关键词：

pyrans; decyclization; antitumor activity; methyl 2,4-dioxobutanoates; tumor cells; inhibition;

D O I：

10.1007/s11094-014-1114-7

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Antiproliferative and antimicrobial activity of methyl-6-amino-3-acyl-4-aryl-5-cyano-4H-pyran-2-carboxylates and their analogs that were synthesized from methyl-2,4-dioxobutanoates was studied. Studies of their antiproliferative activity at the USA National Cancer Institute under the program NCI 60 Cell One-Dose Screen found that methyl-6-amino-5-cyano-4-(furan-2-yl)-3-(3-methoxybenzoyl)-4H-pyran-2-carboxylate had the highest activity, greater than those of busulfan and cisplatin. Methyl-6-amino-3-acetyl-4-phenyl-5-cyano-4H-pyran-2-carboxylate had antimicrobial activity that was comparable with that of chloramine.

引用

页码：379 / 382

页数：4

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