NEW 3,4-BIS(INDOL-1-YL)MALEIMIDES AS PROTEIN KINASE INHIBITORS

Authors

  • Алексей А. Панов Gause Institute of New Antibiotics, 11 Build. 1 B. Pirogovskaya St., Moscow 119021, Russia;
  • Сергей А. Лакатош Gause Institute of New Antibiotics, 11 Build. 1 B. Pirogovskaya St., Moscow 119021, Russia;
  • Михаэль Х. Г. Куббутат ProQinase GmbH, Tumor Biology Centre in Freiburg, 117 Breisacher St., Freiburg 79106, Germany
  • Любовь Г. Деженкова N. N. Blokhin Russian Cancer Research Center, 24 Build. 2 Kashirskoye Shosse, Moscow 115478, Russia
  • Франк Тотцке ProQinase GmbH, Tumor Biology Centre in Freiburg, 117 Breisacher St., Freiburg 79106, Germany
  • Кристоф Шехтеле ProQinase GmbH, Tumor Biology Centre in Freiburg, 117 Breisacher St., Freiburg 79106, Germany

DOI:

https://doi.org/10.1007/5160

Keywords:

indole, indolylmaleimides, antitumor drugs, protein kinases, protein kinase inhibitors.

Abstract

Several previously unknown derivatives of 3,4-bis(indol-1-yl)maleimide, as well as 3-(2,3-dihydroindol-1-yl)-4-(indol-1-yl)maleimide were synthesized as potential analogs for a known series of protein kinase inhibitors BIS I, IV, IX containing the structural motif of 3,4-bis(indol-3-yl)maleimide. The activity of these synthesized compounds was characterized with regard to several human protein kinases and their cytotoxicity was determined.

Author Biographies

Алексей А. Панов, Gause Institute of New Antibiotics, 11 Build. 1 B. Pirogovskaya St., Moscow 119021, Russia;

м.н.с Лаборатории Химической Трансформации Антибиотиков

Михаэль Х. Г. Куббутат, ProQinase GmbH, Tumor Biology Centre in Freiburg, 117 Breisacher St., Freiburg 79106, Germany

Head of Biochemical Drug Discovery & Head of Drug Development

Любовь Г. Деженкова, N. N. Blokhin Russian Cancer Research Center, 24 Build. 2 Kashirskoye Shosse, Moscow 115478, Russia

с.н.с. Лаборатории Химической Трансформации Антибиотиков

Кристоф Шехтеле, ProQinase GmbH, Tumor Biology Centre in Freiburg, 117 Breisacher St., Freiburg 79106, Germany

CEO of ProQinase

Published

2019-11-12

Issue

Section

Original Papers