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Table 1 Drugs tested in this study, with previous reports of increased or decreased effect in hypoxia

From: Effects of hypoxia on human cancer cell line chemosensitivity

Drug Type of drug Effect in hypoxia References
5-FU Antimetabolite pyrimidine analog Less effective in hypoxia in mammary tumor and gastric cancer cell lines [37, 38]
Acriflavine Antiseptic Inhibition of HIF dimerization in a kidney cancer cell line [39]
Bortezomib Proteasome inhibitor VEGF inhibitor in endothelial cells from myeloma patients, repress HIF-1α activity in multiple myeloma and liver cancer cell lines [40, 41]
Cisplatin Platinum compound Less effective in hypoxia in testicular germ cell tumor and gastric cancer cell lines [35, 38]
Downregulate HIF in human ovarian cancer cell lines [42]
Digitoxin Cardiac glycoside HIF-1 inhibition in hepatoblastoma cell line [43]
Digoxin Cardiac glycoside HIF-1 inhibition in prostate cancer, hepatoblastoma and lymphoma cell lines [43]
Docetaxel Mitosis inhibitor, taxane HIF-1 inhibition in ovarian and breast cancer cell lines [44]
Activity unchanged in prostate and ovarian cancer cell lines [42, 45]
Doxorubicin Antracycline, topoisomerase II inhibitor Inhibition of HIF activation in human ovarian cancer cell lines [42]
Less effective in hypoxia in murine sarcoma cell lines [46]
Etoposide Mitosis inhibitor, epipodo-phyllotoxin Less effective in hypoxia in testicular germ cell tumor, breast, prostatic and hepatic cell lines [35, 47, 48]
Gemcitabine Pyrimidine analog Less effective in hypoxia in testicular germ cell tumor and pancreatic cell lines [35, 49, 50]
Irinotecan Topoisomerase I inhibitor The metabolite SN38 inhibits HIF-1α and VEGF in glioma cell lines [51]
Melphalan Alkylating mustard analog Enhanced effect in hypoxia in an animal model and in multiple myeloma cell lines [52, 53]
Mitomycin c Quinone antibiotics Bioreductive in hypoxia in murine sarcoma and mammary cell lines [46, 54]
Less effective in hypoxia in testicular germ cell tumor cell lines [35]
Rapamycin Oral macrolide, mTOR-inhibitor Inhibits mTOR, downregulate VEGF, degrades HIF-1 in prostate cancer, hematopoietic and colon cancer cell lines [55–57]
Sorafenib Multikinase inhibitor VEGFR and PDGFR inhibitor in hepatocellular carcinoma [58]
Thalidomide Anti-inflammatory Angiogenesis inhibitor in CAM-assay and human endothelial cells [59, 60]
Tirapazamine Bioreductive prodrug Reactive radical cause DNA- breaks in several hypoxic human and animal cell lines [61–63]
Topotecan Topoisomerase I inhibitor Inhibit HIF-1α expression in glioblastoma cell lines and tumor biopsies [64, 65]
Vincristine Vinca alkaloid Inhibit HIF-1α expression in ovarian and breast cancer cell lines [44]
Less effective in hypoxia in gastric cancer cells [66]
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BMC Cancer

ISSN: 1471-2407

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