Synthesis and Antitumor Activity of Novel Pyridoxine-Based Bioisosteric Analogs of trans-Stilbenes

Joint Authors

Pugachev, Mikhail V.
Shtyrlin, Yurii G.
Bondar, Oksana V.
Balakin, Konstantin V.
Pavelyev, Roman S.
Iksanova, Alfia G.
Nguyen, Thang T. N.
Bulatov, Timur M.

Source

Journal of Chemistry

Issue

Vol. 2017, Issue 2017 (31 Dec. 2017), pp.1-7, 7 p.

Publisher

Hindawi Publishing Corporation

Publication Date

2017-07-06

Country of Publication

Egypt

No. of Pages

7

Main Subjects

Chemistry

Abstract EN

A series of trans-6-phenylethenyl substituted pyridoxine derivatives, novel bioisosteric analogs of drugs based on trans-stilbene scaffold, were synthesized using the Wittig reaction of a bis-triphenylphosphonium pyridoxine derivative with various aromatic aldehydes.

Two compounds demonstrated high activity against the estrogen-dependent MCF-7 (breast cancer) cell line with IC50 in the range of 1.9–7.9 µM and very good selectivity for other studied normal and tumor cells, including the estrogen receptor negative MDA-MB-231 breast cancer cells.

The active compounds possessed an intense blue fluorescence, and this feature allowed us to effectively visualize them in cytoplasm and in nucleus.

The obtained results make the described chemotype a promising starting point for the development of new anticancer agents for the therapy of estrogen-dependent malignancies.

American Psychological Association (APA)

Pugachev, Mikhail V.& Nguyen, Thang T. N.& Bulatov, Timur M.& Pavelyev, Roman S.& Iksanova, Alfia G.& Bondar, Oksana V.…[et al.]. 2017. Synthesis and Antitumor Activity of Novel Pyridoxine-Based Bioisosteric Analogs of trans-Stilbenes. Journal of Chemistry،Vol. 2017, no. 2017, pp.1-7.
https://search.emarefa.net/detail/BIM-1172422

Modern Language Association (MLA)

Pugachev, Mikhail V.…[et al.]. Synthesis and Antitumor Activity of Novel Pyridoxine-Based Bioisosteric Analogs of trans-Stilbenes. Journal of Chemistry No. 2017 (2017), pp.1-7.
https://search.emarefa.net/detail/BIM-1172422

American Medical Association (AMA)

Pugachev, Mikhail V.& Nguyen, Thang T. N.& Bulatov, Timur M.& Pavelyev, Roman S.& Iksanova, Alfia G.& Bondar, Oksana V.…[et al.]. Synthesis and Antitumor Activity of Novel Pyridoxine-Based Bioisosteric Analogs of trans-Stilbenes. Journal of Chemistry. 2017. Vol. 2017, no. 2017, pp.1-7.
https://search.emarefa.net/detail/BIM-1172422

Data Type

Journal Articles

Language

English

Notes

Includes bibliographical references

Record ID

BIM-1172422