Synthesis and Anticancer Evaluation of Novel 7-Aza-Coumarine-3-Carboxamides

被引：5

作者：

Trifonov, Alexey V. ^{[1
]}

Gazizov, Almir S. ^{[1
]}

Tapalova, Anipa S. ^{[2
]}

Kibardina, Lyudmila K. ^{[1
]}

Appazov, Nurbol O. ^{[2
]}

Voloshina, Alexandra D. ^{[1
]}

Sapunova, Anastasiia S. ^{[1
]}

Luybina, Anna P. ^{[1
]}

Abyzbekova, Gulmira M. ^{[2
]}

Dobrynin, Alexey B. ^{[1
]}

Litvinov, Igor A. ^{[1
]}

Tauekel, Akerke K. ^{[3
]}

Yespenbetova, Sholpan O. ^{[2
]}

Burilov, Alexander R. ^{[1
]}

Pudovik, Michail A. ^{[1
]}

机构：

[1] Russian Acad Sci, Arbuzov Inst Organ & Phys Chem, FRC Kazan Sci Ctr, Arbuzova Str 8, Kazan 420088, Russia

[2] Korkyt Ata Kyzylorda Univ, Aiteke Bi St 29A, Kyzylorda 120014, Kazakhstan

[3] Kazan Natl Res Technol Univ, Dept Oil Chem & Nanotechnol, Karl Marx Str 68, Kazan 420015, Russia

来源：

INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES | 2023年 / 24卷 / 12期

基金：

俄罗斯科学基金会;

关键词：

aza-coumarine; amides; cytotoxicity; selectivity; anti-tumor; OPTICAL-PROPERTIES; SCAFFOLD; DERIVATIVES; COUMARINS; AGENTS;

D O I：

10.3390/ijms24129927

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

Herein, we report the design and synthesis of novel 7-aza-coumarine-3-carboxamides via scaffold-hopping strategy and evaluation of their in vitro anticancer activity. Additionally, the improved non-catalytic synthesis of 7-azacoumarin-3-carboxylic acid is reported, which features water as the reaction medium and provides a convenient alternative to the known methods. The anticancer activity of the most potent 7-aza-coumarine-3-carboxamides against the HuTu 80 cell line is equal to that of reference Doxorubicin, while the selectivity towards the normal cell line is 9-14 fold higher.

引用

页数：19

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