Synthesis and cytotoxicity of novel 1-arylindolizines and 1-arylpyrrolo[2,1-a]isoquinolines

An efficient approach to the synthesis of indolizines and pyrrolo[2,1-a]isoquinolines based on a domino reaction is described. The reactivity of the derivatives and the structure-activity analysis are carried out in a number of the obtained compounds. We found a hit showing high cytotoxicity on tumor cells (IC50 = 5.92 ± 0.08 µM) whose cytotoxic effect is comparable to that of the known topoisomerase I inhibitor camptothecin. © 2021 Elsevier Ltd

Authors
Nevskaya A.A. 1 , Miftyakhova A.R. 1 , Anikina L.V. 2 , Borisova T.N. 1 , Varlamov A.V. 1 , Voskressensky L.G. 1
Journal
Tetrahedron Letters
Publisher
Elsevier Ltd
Language
English
Status
Published
Link
External link
DOI
10.1016/j.tetlet.2021.153552
Number
153552
Year
2021
Organizations
  • 1 Organic Chemistry Department, Peoples’ Friendship University of Russia (RUDN University), 6 Miklukho-Maklaya St., Moscow, 117198, Russian Federation
  • 2 Institute of Physiologically Active Compounds, Russian Academy of Sciences, 1 Severnyi Proezd, Chernogolovka, 142432, Russian Federation
Keywords
Cytotoxicity; Domino reactions; Indolizines; Pyrrolo[2,1-a]isoquinolines; Structure-activity relationship
Date of creation
16.12.2021
Date of change
16.12.2021
Short link
https://repository.rudn.ru/en/records/article/record/76852/
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