Towards lead compounds as anti-cancer agents via new phaeosphaeride A derivatives

Victoria V. Abzianidze, Sofya A. Zakharenkova, Natalia I. Moiseeva, Petr P. Beltyukov, Valeriy A. Polukeev, Yaroslav A. Dubrovskii, Victor A. Kuznetsov, Yuri G. Trishin, Jennifer E. Mejia, Alvin A. Holder

Research output: Contribution to journalArticlepeer-review

2 Scopus citations

Abstract

New derivatives of phaeosphaeride A (PPA) were synthesized and characterized. Anti-tumor studies were carried out on the U937, HCT-116, PC3, MCF-7, A549, К562, NCI-H929, Jurkat, THP-1, RPMI8228 tumor cell lines, and on the HEF cell line. All the compounds synthesized were found to have better efficacy than PPA towards the tumor cell lines mentioned. Compound 6 (IC50 = 0.59 ± 0.27 µM) was observed to be 11 times more active than PPA (IC50 = 6.5 ± 0.30 µM) towards the NCI-H929 cell line, with a therapeutic index of 18. Compound 6 was determined to be over half and 16 times more active than etoposide towards the NCI-H929 (IC50 = 0.9 ± 0.05 µM) and A549 (IC50 = 100 ± 7.0 µM) cell lines, respectively.

Original languageEnglish
Pages (from-to)59-61
Number of pages3
JournalBioorganic and Medicinal Chemistry Letters
Volume29
Issue number1
DOIs
StatePublished - 1 Jan 2019

Scopus subject areas

  • Drug Discovery
  • Molecular Medicine
  • Molecular Biology
  • Biochemistry
  • Clinical Biochemistry
  • Pharmaceutical Science
  • Organic Chemistry

Keywords

  • Anti-cancer agents
  • Etoposide
  • HCT-116 cell line
  • HEF cell line
  • In vitro studies
  • Mercapto derivative
  • Natural products
  • Phaeosphaeride A
  • Therapeutic index
  • FLUORINE
  • NATURAL PHAEOSPHAERIDE

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