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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

[5557]

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

[6163]

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]