Document Type

Article

Publication Date

11-2018

DOI

10.3390/molecules23113043

Publication Title

Molecules

Volume

23

Issue

11

Pages

3043 (9 pages)

Abstract

New derivatives of phaeosphaeride A (PPA) were synthesized and characterized. Anti-tumor activity studies were carried out on the HCT-116, PC3, MCF-7, A549, К562, NCI-Н929, Jurkat, THP-1, RPMI8228 tumor cell lines, and on the HEF cell line. All of the compounds synthesized were found to have better efficacy than PPA towards the tumor cell lines mentioned. Compound 6 was potent against six cancer cell lines, HCT-116, PC-3, K562, NCI-H929, Jurkat, and RPMI8226, showing a 47, 13.5, 16, 4, 1.5, and 7-fold increase in anticancer activity comparative to those of etoposide, respectively. Compound 1 possessed selectivity toward the NCI-H929 cell line (IC50 = 1.35 ± 0.69 μM), while product 7 was selective against three cancer cell lines, HCT-116, MCF-7, and NCI-H929, each having IC50 values of 1.65 μM, 1.80 μM and 2.00 μM, respectively.

Comments

© 2018 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license.

Original Publication Citation

Abzianidze, V., Beltyukov, P., Zakharenkova, S., Moiseeva, N., Mejia, J., Holder, A., . . . Kuznetsov, V. (2018). Synthesis and biological evaluation of phaeosphaeride a derivatives as antitumor agents. Molecules, 23(11), 3043. doi:10.3390/molecules23113043

ORCID

0000-0001-9618-5297 (Holder)

Download

Share

COinS