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

Результат исследований: Научные публикации в периодических изданияхстатьянаучнаярецензирование

1 цитирование (Scopus)

Выдержка

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.

Язык оригиналаанглийский
ЖурналBioorganic and Medicinal Chemistry Letters
DOI
СостояниеПринято в печать - 1 янв 2018

Предметные области Scopus

  • Биохимия
  • Молекулярная медицина
  • Молекулярная биология
  • Фармация
  • Поиск новых лекарств
  • Клиническая биохимия
  • Органическая химия

Цитировать

Abzianidze, V. V., Zakharenkova, S. A., Moiseeva, N. I., Beltyukov, P. P., Polukeev, V. A., Dubrovskii, Y. A., ... Holder, A. A. (Принято в печать). 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. В: Bioorganic and Medicinal Chemistry Letters. 2018.
@article{5f67dd2b62fa4c49a95a25c3cbc91a26,
title = "Towards lead compounds as anti-cancer agents via new phaeosphaeride A derivatives",
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",
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.}",
year = "2018",
month = "1",
day = "1",
doi = "10.1016/j.bmcl.2018.11.003",
language = "English",
journal = "Bioorganic and Medicinal Chemistry Letters",
issn = "0960-894X",
publisher = "Elsevier",

}

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.

В: Bioorganic and Medicinal Chemistry Letters, 01.01.2018.

Результат исследований: Научные публикации в периодических изданияхстатьянаучнаярецензирование

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.

KW - Anti-cancer agents

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

UR - http://www.scopus.com/inward/record.url?scp=85056508587&partnerID=8YFLogxK

U2 - 10.1016/j.bmcl.2018.11.003

DO - 10.1016/j.bmcl.2018.11.003

M3 - Article

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

SN - 0960-894X

ER -