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Synthesis and evaluation of anticancer activity of new 9-acridinyl amino acid derivatives

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Abstract

A series of eleven 9-acridinyl amino acid derivatives were synthesized using a two-step procedure. Cytotoxicity was tested on the K562 and A549 cancer cell lines and normal diploid cell line MRC5 using the MTT assay. Compounds 6, 7, 8 and 9 were the most active, with IC50 values comparable to or lower than that of chemotherapeutic agent amsacrine. 8 and 9 were especially effective in the A549 cell line (IC50 ≈ 6 μM), which is of special interest since amsacrine is not sufficiently active in lung cancer patients. Cell cycle analysis revealed that 7 and 9 caused G2/M block, amsacrine caused arrest in the S phase, while 6 and 8 induced apoptotic cell death independently of the cell cycle regulation. In comparison to amsacrine, 6, 7, 8, and 9 showed similar inhibitory potential towards topoisomerase II, whereas only 7 showed DNA intercalation properties. In contrast to amsacrine, 6, 7, 8 and 9 showed a lack of toxicity towards unstimulated normal human leucocytes.

Graphical abstract: Synthesis and evaluation of anticancer activity of new 9-acridinyl amino acid derivatives

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Article information


Submitted
31 Dec 2019
Accepted
19 Jan 2020
First published
14 Feb 2020

RSC Med. Chem., 2020, Advance Article
Article type
Research Article

Synthesis and evaluation of anticancer activity of new 9-acridinyl amino acid derivatives

J. Rupar, V. Dobričić, J. Grahovac, S. Radulović, Ž. Skok, J. Ilaš, M. Aleksić, J. Brborić and O. Čudina, RSC Med. Chem., 2020, Advance Article , DOI: 10.1039/C9MD00597H

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