Kazan Federal University Digital Repository

Synthesis and in vitro antitumor activity of novel alkenyl derivatives of pyridoxine, bioisosteric analogs of feruloyl methane

Show simple item record

dc.contributor.author Pavelyev R.
dc.contributor.author Bondar O.
dc.contributor.author Nguyen T.
dc.contributor.author Ziganshina A.
dc.contributor.author Al Farroukh M.
dc.contributor.author Karwt R.
dc.contributor.author Alekbaeva G.
dc.contributor.author Pugachev M.
dc.contributor.author Yamaleeva Z.
dc.contributor.author Kataeva O.
dc.contributor.author Balakin K.
dc.contributor.author Shtyrlin Y.
dc.date.accessioned 2019-01-22T20:39:07Z
dc.date.available 2019-01-22T20:39:07Z
dc.date.issued 2018
dc.identifier.issn 0968-0896
dc.identifier.uri https://dspace.kpfu.ru/xmlui/handle/net/148138
dc.description.abstract © 2018 Elsevier Ltd Two series of novel pyridoxine-based azaheterocyclic analogs of feruloyl methane (Dehydrozingerone, DZG) were synthesized, and their biological activity against a panel of tumor and normal cell lines was evaluated in vitro. The most active compounds possessed expressed cytotoxic activity, which was comparable to cytotoxic activity of doxorubicin and significantly higher than that of DZG, and a remarkable selectivity for the studied cancer cell lines as compared to the normal cells. The leading compound and DZG initiated arrest of the cell cycle in the G2/M phase, preventing normal division and further transition of daughter cells to the G0/G1 phase. Similar to DZG, but with higher efficiency, the leading compound was able to inhibit migration activity and, therefore, invasiveness of tumor cells. It also increased concentration of reactive oxygen species in tumor cells, induced depolarization of mitochondrial membranes and initiated apoptosis accompanied by disruption of integrity of cytoplasmic cell membranes. By contrast to DZG, the leading compound did not possess antioxidant properties. The obtained data make the described chemotype a promising starting point for the development of new anticancer agents.
dc.relation.ispartofseries Bioorganic and Medicinal Chemistry
dc.subject Anticancer activity
dc.subject Dehydrozingerone
dc.subject Drug discovery
dc.subject Feruloyl methane
dc.subject Pyridoxine
dc.subject Vitamin B6
dc.title Synthesis and in vitro antitumor activity of novel alkenyl derivatives of pyridoxine, bioisosteric analogs of feruloyl methane
dc.type Article
dc.relation.ispartofseries-issue 22
dc.relation.ispartofseries-volume 26
dc.collection Публикации сотрудников КФУ
dc.relation.startpage 5824
dc.source.id SCOPUS09680896-2018-26-22-SID85056424097


Files in this item

This item appears in the following Collection(s)

  • Публикации сотрудников КФУ Scopus [24551]
    Коллекция содержит публикации сотрудников Казанского федерального (до 2010 года Казанского государственного) университета, проиндексированные в БД Scopus, начиная с 1970г.

Show simple item record

Search DSpace


Advanced Search

Browse

My Account

Statistics