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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.
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页数:19
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