title: New acetylenic derivatives of betulin and betulone, synthesis and cytotoxic activity.
abstract: Betulin1and 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 betulin1were used as a reference compounds. Some derivatives of betulin showed a higher cytotoxic activity than the parent compound1. Two derivatives (5and17) were 24-fold potent than betulin1against the human promyelocytic leukemia cell line (HL-60), with an IC50value of 0.3 µg/mL.
authors.affiliation: 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.
authors.forename: Ewa
authors.initials: E
authors.lastname: Bębenek
authors.affiliation: 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.
authors.forename: Monika
authors.initials: M
authors.lastname: Kadela-Tomanek
authors.affiliation: 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.
authors.forename: Elwira
authors.initials: E
authors.lastname: Chrobak
authors.affiliation: Department of Experimental Oncology, Polish Academy of Sciences, Ludwik Hirszfeld Institute of Immunology and Experimental Therapy, 12 R. Weigla Str., Wrocław, 53-114 Poland.
authors.forename: Joanna
authors.initials: J
authors.lastname: Wietrzyk
authors.affiliation: Department of Experimental Oncology, Polish Academy of Sciences, Ludwik Hirszfeld Institute of Immunology and Experimental Therapy, 12 R. Weigla Str., Wrocław, 53-114 Poland.
authors.forename: Joanna
authors.initials: J
authors.lastname: Sadowska
authors.affiliation: 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.
authors.forename: Stanisław
authors.initials: S
authors.lastname: Boryczka
keywords: Betulin; Betulone; Cytotoxic activity; Lipophilicity; Synthesis