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 |
|---|---|
| Journal | Bioorganic and Medicinal Chemistry Letters |
| DOIs | |
| Publication status | Accepted/In press - 1 Jan 2018 |
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Scopus subject areas
- Biochemistry
- Molecular Medicine
- Molecular Biology
- Pharmaceutical Science
- Drug Discovery
- Clinical Biochemistry
- Organic Chemistry
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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, 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.
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
AN - SCOPUS:85056508587
JO - Bioorganic and Medicinal Chemistry Letters
JF - Bioorganic and Medicinal Chemistry Letters
SN - 0960-894X
ER -