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

2 Citations (Scopus)

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
JournalBioorganic and Medicinal Chemistry Letters
DOIs
Publication statusAccepted/In press - 1 Jan 2018

Fingerprint

Lead compounds
Inhibitory Concentration 50
Cells
Derivatives
Tumors
Tumor Cell Line
Cell Line
Neoplasms
Etoposide
phaeosphaeride A

Scopus subject areas

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

Cite this

Abzianidze, V. V., Zakharenkova, S. A., Moiseeva, N. I., Beltyukov, P. P., Polukeev, V. A., Dubrovskii, Y. A., ... Holder, A. A. (Accepted/In press). Towards lead compounds as anti-cancer agents via new phaeosphaeride A derivatives. Bioorganic and Medicinal Chemistry Letters. https://doi.org/10.1016/j.bmcl.2018.11.003
Abzianidze, Victoria V. ; Zakharenkova, Sofya A. ; Moiseeva, Natalia I. ; Beltyukov, Petr P. ; Polukeev, Valeriy A. ; Dubrovskii, Yaroslav A. ; Kuznetsov, Victor A. ; Trishin, Yuri G. ; Mejia, Jennifer E. ; Holder, Alvin A. / Towards lead compounds as anti-cancer agents via new phaeosphaeride A derivatives. In: Bioorganic and Medicinal Chemistry Letters. 2018.
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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.",
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Abzianidze, VV, Zakharenkova, SA, Moiseeva, NI, Beltyukov, PP, Polukeev, VA, Dubrovskii, YA, Kuznetsov, VA, Trishin, YG, Mejia, JE & Holder, AA 2018, 'Towards lead compounds as anti-cancer agents via new phaeosphaeride A derivatives', Bioorganic and Medicinal Chemistry Letters. https://doi.org/10.1016/j.bmcl.2018.11.003

Towards lead compounds as anti-cancer agents via new phaeosphaeride A derivatives. / Abzianidze, Victoria V.; Zakharenkova, Sofya A.; Moiseeva, Natalia I.; Beltyukov, Petr P.; Polukeev, Valeriy A.; Dubrovskii, Yaroslav A.; Kuznetsov, Victor A.; Trishin, Yuri G.; Mejia, Jennifer E.; Holder, Alvin A.

In: Bioorganic and Medicinal Chemistry Letters, 01.01.2018.

Research output

TY - JOUR

T1 - Towards lead compounds as anti-cancer agents via new phaeosphaeride A derivatives

AU - Abzianidze, Victoria V.

AU - Zakharenkova, Sofya A.

AU - Moiseeva, Natalia I.

AU - Beltyukov, Petr P.

AU - Polukeev, Valeriy A.

AU - Dubrovskii, Yaroslav A.

AU - Kuznetsov, Victor A.

AU - Trishin, Yuri G.

AU - Mejia, Jennifer E.

AU - Holder, Alvin A.

PY - 2018/1/1

Y1 - 2018/1/1

N2 - 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.

AB - 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.

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KW - Etoposide

KW - HCT-116 cell line

KW - HEF cell line

KW - In vitro studies

KW - Mercapto derivative

KW - Natural products

KW - Phaeosphaeride A

KW - Therapeutic index

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U2 - 10.1016/j.bmcl.2018.11.003

DO - 10.1016/j.bmcl.2018.11.003

M3 - Article

AN - SCOPUS:85056508587

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

SN - 0960-894X

ER -