SYNTHESIS AND ANTIPROLIFERATIVE ACTIVITY OF SALICYLIDENEHYDRAZONES BASED ON INDOLE-2(3)-CARBOXYLIC ACIDS

Authors

  • Андрей Г. Васин Gause Institute of New Antibiotics, 11 B. Pirogovskaya St., Moscow 119021, Russia Mendeleev University of Chemical Technology of Russia, 9 Miusskaya Sq., Moscow 125190, Russia
  • Любовь Г. Деженкова Gause Institute of New Antibiotics, 11 B. Pirogovskaya St., Moscow 119021, Russia
  • Иван В. Иванов Gause Institute of New Antibiotics, 11 B. Pirogovskaya St., Moscow 119021, Russia
  • Александр М. Щербаков N. N. Blokhin Russian Cancer Research Center 24 Kashirskoe shosse, Moscow 115422, Russia
  • Андрей Е. Щекотихин Gause Institute of New Antibiotics, 11 B. Pirogovskaya St., Moscow 119021, Russia

DOI:

https://doi.org/10.1007/5639

Keywords:

hydrazones, indole-2(3)-carboxylic acids, salicylic aldehyde, antiproliferative activity.

Abstract

A series of indole-2(3)-carboxylic acid hydrazones were synthesized and their antiproliferative activity was studied for the K562 leukemia, MCF7 breast adenocarcinoma, and HCT116 colon carcinoma cell lines and resistant HCT116p53KO subline in order to preliminary screen biological properties and to reveal the role of the aldehyde fragment and heterocycle in the ability of compounds to inhibit tumor growth. A number of derivatives have been identified that inhibit the growth of tumor cells in submicromolar concentrations, promising for further optimization and in-depth study of antitumor properties.

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Published

2020-07-10

Issue

Vol. 56 No. 6 (2020): Heterocyclic сompounds in medicinal chemistry

Section

Original Papers