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] |