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  • Synthesis and evaluation of anticancer activity of new 9-acridinyl amino acid derivatives [Elektronski vir]
    Rupar, Jelena ...
    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 [micro]M), 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.
    Source: RSC medicinal chemistry [Elektronski vir]. - ISSN 2632-8682 (Vol. 11, iss. 3, 2020, str. 378-386)
    Type of material - e-article ; adult, serious
    Publish date - 2020
    Language - english
    COBISS.SI-ID - 4896625

    Link(s):

    https://pubs.rsc.org/en/content/articlelanding/2020/MD/C9MD00597H?utm_medium=email&utm_campaign=pub-MD-vol-11-issue-3&utm_source=toc-alert#!divAbstract

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    https://pubs.rsc.org/en/content/articlepdf/2020/md/c9md00597h

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