Synthesis of dehydro-α-lapachones, α- and β-lapachones, and screening against cancer cell lines

Synthesis of dehydro-α-lapachones, α- and β-lapachones, and screening against cancer cell lines

14 new naphthoquinones were prepared and tested against human cancer cell lines PC-3 (prostate), HCT-116 (colon carcinoma), SNB-19 (glioblastoma), HL-60 (leukemia) and MCF-7 (breast), and a nontumor cell line L929 (murine fibroblasts) to determine cytotoxicity with the MTT assay. 8-OH-β-lapachones (...

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Veröffentlicht in:Medicinal chemistry research 2019-12, Vol.28 (12), p.2109-2117
Hauptverfasser: Moreira, Caroline dos S., Nicoletti, Caroline D., Pinheiro, Daniel P., de Moraes, Leonardo G. C., Futuro, Debora O., Ferreira, Vitor F., Pessoa, Claudia do Ó, da Rocha, David R.
Format: Artikel
Sprache:eng
Schlagworte:
60 APPLIED LIFE SCIENCES
Biochemistry
Biomedical and Life Sciences
Biomedicine
Biotechnology
Breast
CARCINOMAS
Cell Biology
Colon
Cytotoxicity
FIBROBLASTS
Glioblastoma
GLIOMAS
LARGE INTESTINE
LEUKEMIA
MAMMARY GLANDS
Original Research
Pharmacology/Toxicology
PROSTATE
Prostate cancer
Selectivity
SYNTHESIS
TOXICITY
Tumor cell lines
TUMOR CELLS
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Zusammenfassung:14 new naphthoquinones were prepared and tested against human cancer cell lines PC-3 (prostate), HCT-116 (colon carcinoma), SNB-19 (glioblastoma), HL-60 (leukemia) and MCF-7 (breast), and a nontumor cell line L929 (murine fibroblasts) to determine cytotoxicity with the MTT assay. 8-OH-β-lapachones ( 14a , 14c , 14d ) presented best results, showing low IC 50 values and high selectivity for HCT-116 and HL-60 tumor cells.
ISSN:1054-2523
1554-8120
DOI:10.1007/s00044-019-02439-w