Journal
MEDICINAL CHEMISTRY RESEARCH
Volume 28, Issue 12, Pages 2171-2183Publisher
SPRINGER BIRKHAUSER
DOI: 10.1007/s00044-019-02445-y
Keywords
Triterpenoids; Fusidic acid; Fusidane amines; Antitumor activity
Categories
Ask authors/readers for more resources
New 3-amino substituted derivatives, containing linear, aromatic, and heterocyclic fragments, as well as conjugates with biogenic amines-spermine and spermidine, were synthesized from 3,11-dioxo analogs of fusidic acid and its methyl ester. Antitumor activity of the compounds was studied in vitro towards the 60 cell lines of nine different types of human tumors of the NCI collection. Introduction of pyrrolidine, n-butylamine, benzylamine, and ethylenediamine substituents into the molecules were found to provide a pronounced selective effect on five cell lines of leukemia: HL-60, K-562, MOLT-4, RPMI-8226, and SR, inhibiting their growth from 70% to complete death of cancer cells. Methylfusidate derivative with a spermine fragment was shown to exhibit the widest spectrum of antiproliferative action among the obtained compounds, inhibiting the growth of leukemia, NSC lung cancer, colon cancer, and melanoma cell lines of 68-92%.
Authors
I am an author on this paper
Click your name to claim this paper and add it to your profile.
Reviews
Recommended
No Data Available