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
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
收藏
页数:19
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