期刊
BIOORGANIC CHEMISTRY
卷 104, 期 -, 页码 -出版社
ACADEMIC PRESS INC ELSEVIER SCIENCE
DOI: 10.1016/j.bioorg.2020.104169
关键词
Domino reaction; DNA binding; Antiproliferative activity
资金
- Russian Science Foundation [18-73-00017]
- RUDN University Program 5-100
- Italian Ministry of Education, Universities and Research [201744BN5T_004]
- Russian Science Foundation [18-73-00017] Funding Source: Russian Science Foundation
An interaction of homophthalonitrile with salicylaldehydes proceeds as a novel domino reaction and results in the formation of nineteen 12H-chromeno[2,3-c]isoquinoline-5-amine derivatives. Four new bonds and two cycles are forged in a single synthetic operation, employing cheap and eco-friendly ammonium formate, acting both as a catalyst and a reducing agent. The in vitro cytotoxicity tests revealed antiproliferative activities against five human tumor cell lines, including the cisplatin-resistant ovarian carcinoma one (A2780cp8), with inhibitory potency data (IC50) in the low micromolar range in most cases. Molecular docking calculations and fluorescence quenching studies revealed possible binding properties with DNA of the active compounds.
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