Towards lead compounds as anti-cancer agents via new phaeosphaeride A derivatives |
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| Authors: | 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 |
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| Affiliation: | 1. Research Institute of Hygiene, Occupational Pathology and Human Ecology, Federal Medical Biological Agency, p/o Kuz’molovsky, Saint Petersburg 188663, Russian Federation;2. Saint Petersburg State University of Industrial Technologies and Design, Saint Petersburg 198095, Russian Federation;3. N.N. Blokchin National Medical Research Center of Oncology, Moscow 115478, Russian Federation;4. Institute of Experimental Medicine, Saint Petersburg 197376, Russian Federation;5. Saint Petersburg State University, Institute of Chemistry, Saint Petersburg 198504, Russian Federation;6. Department of Chemistry and Biochemistry, Old Dominion University, 4541 Hampton Boulevard, Norfolk, VA 23529, United States |
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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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| Keywords: | Natural products Phaeosphaeride A Anti-cancer agents Etoposide HEF cell line HCT-116 cell line Mercapto derivative Therapeutic index |
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