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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.
Afiliación
  • Abzianidze VV; Research Institute of Hygiene, Occupational Pathology and Human Ecology, Federal Medical Biological Agency, p/o Kuz'molovsky, Saint Petersburg 188663, Russian Federation. Electronic address: vvaavv@mail.ru.
  • Zakharenkova SA; Saint Petersburg State University of Industrial Technologies and Design, Saint Petersburg 198095, Russian Federation.
  • Moiseeva NI; N.N. Blokchin National Medical Research Center of Oncology, Moscow 115478, Russian Federation.
  • Beltyukov PP; Research Institute of Hygiene, Occupational Pathology and Human Ecology, Federal Medical Biological Agency, p/o Kuz'molovsky, Saint Petersburg 188663, Russian Federation.
  • Polukeev VA; Institute of Experimental Medicine, Saint Petersburg 197376, Russian Federation.
  • Dubrovskii YA; Research Institute of Hygiene, Occupational Pathology and Human Ecology, Federal Medical Biological Agency, p/o Kuz'molovsky, Saint Petersburg 188663, Russian Federation; Saint Petersburg State University, Institute of Chemistry, Saint Petersburg 198504, Russian Federation.
  • Kuznetsov VA; Research Institute of Hygiene, Occupational Pathology and Human Ecology, Federal Medical Biological Agency, p/o Kuz'molovsky, Saint Petersburg 188663, Russian Federation.
  • Trishin YG; Saint Petersburg State University of Industrial Technologies and Design, Saint Petersburg 198095, Russian Federation.
  • Mejia JE; Department of Chemistry and Biochemistry, Old Dominion University, 4541 Hampton Boulevard, Norfolk, VA 23529, United States.
  • Holder AA; Department of Chemistry and Biochemistry, Old Dominion University, 4541 Hampton Boulevard, Norfolk, VA 23529, United States. Electronic address: aholder@odu.edu.
Bioorg Med Chem Lett ; 29(1): 59-61, 2019 01 01.
Article en En | MEDLINE | ID: mdl-30447888
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 ±â€¯0.27 µM) was observed to be 11 times more active than PPA (IC50 = 6.5 ±â€¯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 ±â€¯0.05 µM) and A549 (IC50 = 100 ±â€¯7.0 µM) cell lines, respectively.
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Texto completo: 1 Colección: 01-internacional Banco de datos: MEDLINE Asunto principal: Compuestos Bicíclicos Heterocíclicos con Puentes / Antineoplásicos Límite: Humans Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2019 Tipo del documento: Article
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Texto completo: 1 Colección: 01-internacional Banco de datos: MEDLINE Asunto principal: Compuestos Bicíclicos Heterocíclicos con Puentes / Antineoplásicos Límite: Humans Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2019 Tipo del documento: Article