New acetylenic derivatives of betulin and betulone, synthesis and cytotoxic activity.

Journal: Medicinal chemistry research : an international journal for rapid communications on design and mechanisms of action of biologically active agents
Published Date: Sep 1, 2016

Abstract

Betulin and its semisynthetic derivatives exhibit a cytotoxic activity toward various cancer cell lines. These compounds are a promising and potential anticancer candidates. A series of betulin derivatives was prepared and tested for the antiproliferative activity in vitro against T47D breast cancer, CCRF/CEM leukemia, HL-60 promyelocytic leukemia, SW707 colorectal, murine P388 leukemia, as well as BALB3T3 normal fibroblasts cell lines. Cisplatin and betulin were used as a reference compounds. Some derivatives of betulin showed a higher cytotoxic activity than the parent compound . Two derivatives ( and ) were 24-fold potent than betulin against the human promyelocytic leukemia cell line (HL-60), with an IC value of 0.3 µg/mL.

Authors

  • Ewa Bębenek
    Department of Organic Chemistry, Medical University of Silesia in Katowice, School of Pharmacy with the Division of Laboratory Medicine in Sosnowiec, 4 Jagiellońska Str., Sosnowiec, 41-200 Poland.
  • Monika Kadela-Tomanek
    Department of Organic Chemistry, Medical University of Silesia in Katowice, School of Pharmacy with the Division of Laboratory Medicine in Sosnowiec, 4 Jagiellońska Str., Sosnowiec, 41-200 Poland.
  • Elwira Chrobak
    Department of Organic Chemistry, Medical University of Silesia in Katowice, School of Pharmacy with the Division of Laboratory Medicine in Sosnowiec, 4 Jagiellońska Str., Sosnowiec, 41-200 Poland.
  • Joanna Wietrzyk
    Department of Experimental Oncology, Polish Academy of Sciences, Ludwik Hirszfeld Institute of Immunology and Experimental Therapy, 12 R. Weigla Str., Wrocław, 53-114 Poland.
  • Joanna Sadowska
    Department of Experimental Oncology, Polish Academy of Sciences, Ludwik Hirszfeld Institute of Immunology and Experimental Therapy, 12 R. Weigla Str., Wrocław, 53-114 Poland.
  • Stanisław Boryczka
    Department of Organic Chemistry, Medical University of Silesia in Katowice, School of Pharmacy with the Division of Laboratory Medicine in Sosnowiec, 4 Jagiellońska Str., Sosnowiec, 41-200 Poland.

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