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New Conjugates of Daunorubicin with Sesquiterpene Lactones and Their Biological Activity
Author(s) -
Pukhov Sergey A.,
Semakov Alexey V.,
Globa Anastasiya A.,
Anikina Lada V.,
Afanasyeva Svetlana V.,
Yandulova Ekaterina Y.,
Aleksandrova Yulia R.,
Neganova Margarita E.,
Klochkov Sergey G.
Publication year - 2021
Publication title -
chemistryselect
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.437
H-Index - 34
ISSN - 2365-6549
DOI - 10.1002/slct.202102244
Subject(s) - daunorubicin , sesquiterpene , cell cycle , apoptosis , conjugate , jurkat cells , chemistry , toxicity , hl60 , cell culture , cell cycle checkpoint , flow cytometry , viability assay , anthracycline , pharmacology , stereochemistry , biochemistry , biology , microbiology and biotechnology , leukemia , immunology , organic chemistry , t cell , mathematical analysis , genetics , mathematics , immune system , cancer , breast cancer
New conjugates of daunorubicin with sesquiterpene lactones at the 3′‐amino group of anthracycline were synthesized and their effect on the viability of cell lines (HL60, Jurkat, K562, and A549) was assessed using a resazurin test. The effect on the cell cycle and apoptosis by flow cytometry was studied. The following natural lactones were used for modification: telekin, isotelekin, reynosin, costunolide, dehydrocostuslactone, santamarine and epoxyisoalantolactone. The synthesized conjugates are characterized by a general high toxicity (8…0.14 μM) in relation to tumor cell lines (in some cases, higher than the toxicity of the initial antibiotic), as well as a comparable effect on the cell cycle (arrest in the G2/M‐phase) with a relatively low the effect on the initiation of apoptosis at concentrations close to the IC 50 .