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

Alexey Vladimirovich Trifonov, Almir Sabirovich Gazizov, Анипа Сейдалиевна Тапалова, Lyudmila K. Kibardina, Nurbol Orynbasaruly Appazov, Alexandra D. Voloshina, Аnastasiia S. Sapunova, Anna P. Luybina, Г. М. Абызбекова, Alexey B. Dobrynin

5 more authors

Igor A. Litvinov, Akerke K. Tauekel, Sholpan Yespenbetova, Alexander Romanovich Burilov, Michail A. Pudovik

2023

Full text Open access: Gold Metadata (CSL-JSON)
DOI 10.3390/ijms24129927
Data confidence 70 medium
How this score is calculated

It is built from checkable properties of the record itself: whether the article has a DOI, how many independent sources confirmed its data, whether the required fields are filled in, and how recent the latest confirmation is. Disagreement between sources and a missing identifier lower it. A value of 80 or above means the record was published without further checking; 60 to 79 means it is published at reduced confidence, with a manual check advisable. A record verified by an editor by hand is never pushed below 90 by a recalculation. This scores our data about the article, not the article itself.

Abstract

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.