AZIRIDINE-2-CARBOXYLIC ACID DERIVATIVES AND ITS OPEN-RING ISOMERS AS A NOVEL PDIA1 INHIBITORS

Authors

  • Irena Leite Latvian Institute of Organic Synthesis, 21 Aizkraukles St., Riga, LV-1006, Latvia
  • Victor Andrianov Latvian Institute of Organic Synthesis, 21 Aizkraukles St., Riga, LV-1006, Latvia
  • Diana Zelencova-Gopejenko Latvian Institute of Organic Synthesis, 21 Aizkraukles St., Riga, LV-1006, Latvia
  • Einars Loza Latvian Institute of Organic Synthesis, 21 Aizkraukles St., Riga, LV-1006, Latvia
  • Iveta Kazhoka-Lapsa Latvian Institute of Organic Synthesis, 21 Aizkraukles St., Riga, LV-1006, Latvia
  • Ilona Domracheva Latvian Institute of Organic Synthesis, 21 Aizkraukles St., Riga, LV-1006, Latvia
  • Marta Stojak Jagiellonian Centre for Experimental Therapeutics (JCET), Jagiellonian University, 14 Bobrzynskiego St., 30-348 Krakow, Poland
  • Stefan Chlopicki Jagiellonian Centre for Experimental Therapeutics (JCET), Jagiellonian University, 14 Bobrzynskiego St., 30-348 Krakow, Poland
  • Ivars Kalvins Latvian Institute of Organic Synthesis, 21 Aizkraukles St., Riga, LV-1006, Latvia

DOI:

https://doi.org/10.1007/6261

Keywords:

aziridine-2-carboxylic acid, DFT calculation, isomerisation, PDIA1 inhibitors.

Abstract

Acyl derivatives of aziridine-2-carboxylic acid have been synthesized and tested as PDIA1 inhibitors. Calculations of charge value and distribution in aziridine ring system and some alkylating agents were performed. For the first time was found that acyl derivatives of aziridine-2-carboxylic acid are weak to moderately active PDIA1 inhibitors.

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Published

2021-11-26

Issue

Vol. 57 No. 11 (2021)

Section

Original Papers