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

A new interesting article has been published in Bioorg Med Chem. 2018 Dec 1;26(22):5824-5837. doi: 10.1016/j.bmc.2018.10.031. Epub 2018 Oct 27. and titled:

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

Authors of this article are:

Pavelyev RS, Bondar OV, Nguyen TNT, Ziganshina AA, Al Farroukh M, Karwt R, Alekbaeva GD, Pugachev MV, Yamaleeva ZR, Kataeva ON, Balakin KV, Shtyrlin YG.

A summary of the article is shown below:

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.

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This article is a good source of information and a good way to become familiar with topics such as:

Anticancer activity;Dehydrozingerone;Drug discovery;Feruloyl methane;Pyridoxine;Vitamin B6

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