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

doi:10.1016/j.bmcl.2018.11.003

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 journal › Article › peer-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 language	English
Pages (from-to)	59-61
Number of pages	3
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	29
Issue number	1
DOIs	https://doi.org/10.1016/j.bmcl.2018.11.003
State	Published - 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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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. 2019 ; Vol. 29, No. 1. pp. 59-61.

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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.",

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",

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

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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, Vol. 29, No. 1, 01.01.2019, p. 59-61.

Research output: Contribution to journal › Article › peer-review

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

AU - Abzianidze, Victoria V.

AU - Zakharenkova, Sofya A.

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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.

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