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1. Full Text Tumor-Penetrating Nanoparticles for Enhanced Anticancer Activity of Combined Photodynamic and Hypoxia-Activated Therapy
by Wang, Yazhe and Xie, Ying and Li, Jing and Peng, Zheng-Hong and Sheinin, Yuri and Zhou, Jianping and Oupický, David
ACS Nano, ISSN 1936-0851, 02/2017, Volume 11, Issue 2, pp. 2227 - 2238
Poor tumor penetration is a major challenge for the use of nanoparticles in anticancer therapy. Moreover, the inability to reach hypoxic tumor cells that are... 
hypoxia | cancer | nanoparticles | tumor penetration | iRGD | photodynamic therapy | DRUG-DELIVERY | COMBINATION THERAPY | MATERIALS SCIENCE, MULTIDISCIPLINARY | TISSUE | CHEMISTRY, PHYSICAL | TIRAPAZAMINE | NANOSCIENCE & NANOTECHNOLOGY | CHEMISTRY, MULTIDISCIPLINARY | CANCER-THERAPY | PEPTIDE | BREAST-CANCER | MICROENVIRONMENT | EFFICIENT | POLYMER HYBRID NANOPARTICLES | Prodrugs - administration & dosage | Hypoxia - drug therapy | Injections, Intravenous | Photosensitizing Agents - chemistry | Reactive Oxygen Species - metabolism | Nanoparticles - chemistry | Apoptosis - drug effects | Prodrugs - chemistry | Antineoplastic Agents - administration & dosage | Indocyanine Green - pharmacology | Photochemotherapy | Drug Delivery Systems | Tirapazamine - chemistry | Photosensitizing Agents - administration & dosage | Tissue Distribution | Indocyanine Green - chemistry | Photosensitizing Agents - pharmacology | Antineoplastic Agents - pharmacology | Molecular Structure | Tumor Cells, Cultured | Indocyanine Green - administration & dosage | Tirapazamine - administration & dosage | Tirapazamine - pharmacology | Antineoplastic Agents - chemistry | Reactive Oxygen Species - analysis | Animals | Cell Proliferation - drug effects | Mice | Nanoparticles - administration & dosage | Prodrugs - pharmacology | Drug Screening Assays, Antitumor | Nanoparticles | Drugs | Therapy | Drug delivery systems | Photodynamic therapy | Penetration | Tumors | Anticancer properties | Hypoxia | Tumor Penetration | Photodynamic Therapy | Cancer
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2. Full Text Kinetics of Flavoenzyme-Catalyzed Reduction of Tirapazamine Derivatives: Implications for Their Prooxidant Cytotoxicity
by Nemeikaitė-Čėnienė and Šarlauskas and Jonušienė and Marozienė and Misevičienė and Yantsevich and Čėnas
International Journal of Molecular Sciences, ISSN 1422-0067, 09/2019, Volume 20, Issue 18, p. 4602
Derivatives of tirapazamine and other heteroaromatic N-oxides (ArN→O) exhibit promising antibacterial, antiprotozoal, and tumoricidal activities. Their action... 
reductive activation | oxidative stress | cytotoxicity | tirapazamine
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3. Full Text Putative electron-affinic radiosensitizers and markers of hypoxic tissue: Synthesis and preliminary in vitro biological characterization of C3-amino-substituted benzotriazine dioxides (BTDOs)
by Elsaidi, Hassan RH and Yang, Xiao-Hong and Ahmadi, Fatemeh and Weinfeld, Michael and Wiebe, Leonard I and Kumar, Piyush
European Journal of Medicinal Chemistry, ISSN 0223-5234, 03/2019, Volume 165, pp. 216 - 224
The redox characteristics of 1,2,4-benzotriazine-1,4-dioxides (BTDOs) make them potential radiosensitizing agents for hypoxic cells in solid human cancers.... 
Benzotriazine-1-monoxides (BTMOs) | Tumor hypoxia | Benzotriazine-1,4-dioxides (BTDOs) | Radiosensitization | Tirapazamine | Hypoxia-selective benzotriazines | 1,2,4-BENZOTRIAZINE 1,4-DIOXIDES | DESIGN | CHEMISTRY, MEDICINAL | ANALOGS | TOXICITY | N-OXIDES | EXTRAVASCULAR TRANSPORT | CHEMISTRY | REDUCTION POTENTIALS | CELL | Tirapazamine - therapeutic use | Oxidation-Reduction | Triazines - therapeutic use | Humans | Tirapazamine - analogs & derivatives | Oxides | Structure-Activity Relationship | Animals | Triazines - chemical synthesis | Biomarkers | Hypoxia | Triazines - chemistry | Radiation-Sensitizing Agents - chemistry
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4. Full Text Targeting the hypoxic fraction of tumours using hypoxia-activated prodrugs Cytotoxic Reviews Godefridus J. Peters and Eric Raymond
by Phillips, Roger M
Cancer Chemotherapy and Pharmacology, ISSN 0344-5704, 03/2016, Volume 77, Issue 3, pp. 441 - 457
AQ4N | Hypoxia-activated prodrugs | Bioreductive drugs | PR-104 | Hypoxia | Tirapazamine | EO9 | TH-302 | TH-4000
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5. Full Text Simultaneous Assay of Oxygen-Dependent Cytotoxicity and Genotoxicity of Anticancer Drugs on an Integrated Microchip
by Li, Lili and Li, Yaqiong and Shao, Zixing and Luo, Guoan and Ding, Mingyu and Liang, Qionglin
Analytical Chemistry, ISSN 0003-2700, 10/2018, Volume 90, Issue 20, pp. 11899 - 11907
Oxygen deprivation is a common feature in a variety Pyrogallo of cancer tissues and associated with tumor progression, acquisition of antiapoptotic potential,... 
PLATFORM | ADHESION | CHEMISTRY, ANALYTICAL | CHIP | TUMOR HYPOXIA | SOLID TUMORS | 3-DIMENSIONAL CELL-CULTURE | GRADIENT | CHEMOTHERAPY | MICROFLUIDICS | DROPLETS | A549 Cells | Cell Survival - drug effects | Optical Imaging | Oxygen - pharmacology | Apoptosis - drug effects | DNA, Neoplasm - metabolism | Humans | Microfluidic Analytical Techniques - instrumentation | Tirapazamine - pharmacology | Structure-Activity Relationship | Antineoplastic Agents - chemistry | DNA, Neoplasm - drug effects | Oxygen - metabolism | Tirapazamine - chemistry | Dose-Response Relationship, Drug | Bleomycin - chemistry | Mutagenicity Tests | Bleomycin - pharmacology | Antineoplastic Agents - pharmacology | Cell Proliferation - drug effects | DNA Damage | DNA, Neoplasm - genetics | Tumor Cells, Cultured | Drug Screening Assays, Antitumor | Drugs | Silicone resins | Toxicity | DNA damage | Genotoxicity | Cytotoxicity | Assaying | Polydimethyl siloxanes | Mimicry | Antitumor agents | Tirapazamine | Deoxyribonucleic acid--DNA | Oxygen | Deprivation | Cultivation | Studies | DNA microarrays | Response time | Hypoxia | Drug discovery | Combinatorial analysis | Microfluidics | Cancer | Tumors | Apoptosis | Index Medicus
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6. Full Text P 084 - Therapeutic assessment of tirapazamine-induced oxidative stress on gastric cancers
by Chang, Jungshan and Ajnai, Giimel and Lin, Pao-Ying
Free Radical Biology and Medicine, ISSN 0891-5849, 07/2017, Volume 108, pp. S46 - S46
Catalase | Gold nanoparticles | Glutathione S-transferase P | Tirapazamine
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7. Full Text Functional CRISPR and shRNA Screens Identify Involvement of Mitochondrial Electron Transport in the Activation of Evofosfamide
by Hunter, Francis W and Devaux, Jules B L and Meng, Fanying and Hong, Cho Rong and Khan, Aziza and Tsai, Peter and Ketela, Troy W and Sharma, Indumati and Kakadia, Purvi M and Marastoni, Stefano and Shalev, Zvi and Hickey, Anthony J R and Print, Cristin G and Bohlander, Stefan K and Hart, Charles P and Wouters, Bradly G and Wilson, William R
Molecular pharmacology, ISSN 0026-895X, 06/2019, Volume 95, Issue 6, pp. 638 - 651
Evofosfamide (TH-302) is a hypoxia-activated DNA-crosslinking prodrug currently in clinical development for cancer therapy. Oxygen-sensitive activation of... 
PRODRUG EVOFOSFAMIDE | THERAPY | PRECLINICAL MODELS | IN-VIVO | DOXORUBICIN | TIRAPAZAMINE | PHARMACOLOGY & PHARMACY | HYPOXIA | IDENTIFICATION | COMBINATION | TH-302
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8. Full Text Development of [131 I]I-EOE-TPZ and [131 I]I-EOE-TPZMO: Novel tirapazamine (TPZ)-based radioiodinated pharmaceuticals for application in theranostic management of hypoxia
by Elsaidi, Hassan and Ahmadi, Fatemeh and Wiebe, Leonard I and Kumar, Piyush
Pharmaceuticals, ISSN 1424-8247, 03/2019, Volume 12, Issue 1, p. 3
: Benzotriazine-1,4-dioxides (BTDOs) such as tirapazamine (TPZ) and its derivatives act as radiosensitizers of hypoxic tissues. The benzotriazine-1-monoxide... 
Benzotriazine-1-monoxide (BTMO) | Tirapazamine (TPZ) | Benzotriazine-1,4-dioxide (BTDO) | Hypoxia | Radiosensitizer | Radioiodination | SR 4317 | radioiodination | hypoxia | benzotriazine-1,4-dioxide (BTDO), benzotriazine-1-monoxide (BTMO), tirapazamine (TPZ), SR 4317 | radiosensitizer
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9. Full Text Quinoxaline 1,4-di-N-oxides: Biological activities and mechanisms of actions
by Cheng, Guyue and Sa, Wei and Cao, Chen and Guo, Liangliang and Hao, Haihong and Liu, Zhenli and Wang, Xu and Yuan, Zonghui
Frontiers in Pharmacology, ISSN 1663-9812, 03/2016, Volume 7
Quinoxaline 1,4-di-N-oxides (QdNOs) have manifold biological properties, including antimicrobial, antitumoral, antitrypanosomal and... 
Antimicrobial | Antitumoral | Structure-activity relationship | Antiinflammatory | Quinoxaline 1 | Antioxidant | Antiprotozoal | 4-di-N-oxides | Mode of action | antimicrobial | antioxidant | CHLOROQUINOXALINE SULFONAMIDE CQS | mode of action | DNA-BASE DAMAGE | antiprotozoal | PROTEIN CROSS-LINKS | 3-AMINO-1,2,4-BENZOTRIAZINE 1,4-DIOXIDE TIRAPAZAMINE | OLAQUINDOX IN-VITRO | MYCOBACTERIUM-TUBERCULOSIS AGENTS | HYPOXIA-INDUCIBLE FACTOR-1-ALPHA | quinoxaline 1,4-di-N-oxides | PHARMACOLOGY & PHARMACY | antitumoral | SELECTIVE THERAPEUTIC AGENTS | antiinflammatory | ANTICANCER DRUG TIRAPAZAMINE | structure-activity relationship | ANTI-TRYPANOSOMA-CRUZI
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10. Full Text Pretreatment F-18-FAZA PET predicts success of hypoxia-directed radiochemotherapy using tirapazamine
by Beck, R and Roper, B and Carlsen, JM and Huisman, MC and Lebschi, JA and Andratschke, N and Picchio, M and Souvatzoglou, M and Machulla, HJ and Piert, M
JOURNAL OF NUCLEAR MEDICINE, ISSN 0161-5505, 06/2007, Volume 48, Issue 6, pp. 973 - 980
We evaluated the predictive value of PET using the hypoxia tracer F-18-fluoroazomycin arabinoside (F-18-FAZA) for success of radiotherapy in combination with... 
FAZA | tirapazamine | RADIATION ONCOLOGY | tumor hypoxia | PHASE-II | EMT6 | CHEMOTHERAPEUTIC DRUGS | ADVANCED HEAD | NECK-CANCER | CELL LUNG-CANCER | radiochemotherapy | POSITRON-EMISSION-TOMOGRAPHY | RADIOTHERAPY | CONCURRENT TIRAPAZAMINE | RADIOLOGY, NUCLEAR MEDICINE & MEDICAL IMAGING
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11. Full Text Monitoring and Targeting Anti-VEGF Induced Hypoxia within the Viable Tumor by 19F–MRI and Multispectral Analysis
by Shi, Yunzhou and Oeh, Jason and Hitz, Anna and Hedehus, Maj and Eastham-Anderson, Jeffrey and Peale, Franklin V and Hamilton, Patricia and O'Brien, Thomas and Sampath, Deepak and Carano, Richard A.D
Neoplasia, ISSN 1476-5586, 11/2017, Volume 19, Issue 11, pp. 950 - 959
The effect of anti-angiogenic agents on tumor oxygenation has been in question for a number of years, where both increases and decreases in tumor pO have been... 
Angiogenesis | Prodrugs | Magnetic resonance imaging | Xenografts | Clinical trials | Hypoxia | Tirapazamine | Oxygenation | Vascular endothelial growth factor | Tumors | Structure-function relationships | Cancer
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12. Synthesis, preferentially hypoxic apoptosis and anti-angiogenic activity of 3- amino-1,2,4-benzotriazine-1,4-dioxide bearing alkyl linkers with a 3-amino-1,2,4- benzotriazine-1-oxide moiety
by Lee, Chun-I and Huang, Chien-Ming and Huang, Wen-Hsin and Lee, An-Rong
Anti-Cancer Agents in Medicinal Chemistry, ISSN 1871-5206, 2014, Volume 14, Issue 10, pp. 1428 - 1446
3-(Aminoalkylamino)-1,2,4-benzotriazine-1,4-dioxide-extended derivatives were synthesized by the structural modification of... 
Bioreductive agent | 3-amino-1,2,4-benzotriazine-1,4-dioxide (tirapazamine) | Hypoxic cytotoxin | Anti-angiogensis | Apoptosis | CELLS | 1,2,4-BENZOTRIAZINE 1,4-DIOXIDES | CHEMISTRY, MEDICINAL | TUMOR HYPOXIA | bioreductive agent | ANALOGS | VASCULAR DYSFUNCTION | CYTOTOXIN TIRAPAZAMINE | apoptosis | SR-4233 | hypoxic cytotoxin | AGENT | ONCOLOGY | BIOREDUCTIVE DRUGS | DERIVATIVES
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13. Full Text Application of Suzuki–Miyaura and Buchwald–Hartwig Cross‐coupling Reactions to the Preparation of Substituted 1,2,4‐Benzotriazine 1‐Oxides Related to the Antitumor Agent Tirapazamine
by Sarkar, Ujjal and Hillebrand, Roman and Johnson, Kevin M and Cummings, Andrea H and Phung, Ngoc Linh and Rajapakse, Anuruddha and Zhou, Haiying and Willis, Jordan R and Barnes, Charles L and Gates, Kent S
Journal of Heterocyclic Chemistry, ISSN 0022-152X, 01/2017, Volume 54, Issue 1, pp. 155 - 160
Many 1,2,4‐benzotriazine 1,4‐dioxides display the ability to selectively kill the oxygen‐poor cells found in solid tumors. As a result, there is a desire for... 
N‐oxides | hypoxia selective anticancer agent | N-oxides | DNA STRAND CLEAVAGE | 1,4-DI-N-OXIDE | 3-AMINO-1,2,4-BENZOTRIAZINE 1,4-DIOXIDE TIRAPAZAMINE | EXTRAVASCULAR TRANSPORT | CYTOTOXIN TIRAPAZAMINE | CHEMISTRY, ORGANIC | REDUCTION CHEMISTRY | BASE DAMAGE | N-OXIDES | HYPOXIA | DERIVATIVES | Antimitotic agents | Antineoplastic agents | Oxides
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14. Full Text Artificial anaerobic cell dormancy for tumor gaseous microenvironment regulation therapy
by Chen, Chen and Su, Weiwei and Liu, Yanyan and Zhang, Jiawen and Zuo, Changjing and Yao, Zhenwei and Bu, Wenbo
Biomaterials, ISSN 0142-9612, 04/2019, Volume 200, pp. 48 - 55
Oxygen is known as an irreplaceable gas in the lives of most eukaryotic cells, yet researchers underestimate its importance, as in the case in many studies of... 
Hypoxia | Cell dormancy | Gaseous microenvironment regulation | Controlled drug release | Anaerobic | MATERIALS SCIENCE, BIOMATERIALS | ENGINEERING, BIOMEDICAL | TIRAPAZAMINE | CANCER | Green chemistry | Ceramics | Ceramic materials | Green technology | Tumors
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15. Full Text Drug testing and flow cytometry analysis on a large number of uniform sized tumor spheroids using a microfluidic device
by Patra, Bishnubrata and Peng, Chien-Chung and Liao, Wei-Hao and Lee, Chau-Hwang and Tung, Yi-Chung
Scientific Reports, ISSN 2045-2322, 02/2016, Volume 6, Issue 1, p. 21061
Three-dimensional (3D) tumor spheroid possesses great potential as an in vitro model to improve predictive capacity for pre-clinical drug testing. In this... 
APOPTOSIS | RESVERATROL | HEPATOCELLULAR-CARCINOMA | ACTIVATION | CISPLATIN | MULTIDISCIPLINARY SCIENCES | NITRIC-OXIDE | RESISTANCE | TIRAPAZAMINE | CELL-CULTURE | MODEL | Microfluidic Analytical Techniques - methods | Spheroids, Cellular - drug effects | Flow Cytometry | Cell Culture Techniques | Humans | Drug Screening Assays, Antitumor | Flow cytometry | Cell culture | Resveratrol | Hepatocellular carcinoma | Drug screening | Tirapazamine | Drug testing | Cisplatin | Microfluidics | Spheroids
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16. Full Text Exploiting the Inherent Photophysical Properties of the Major Tirapazamine Metabolite in the Development of Profluorescent Substrates for Enzymes That Catalyze the Bioreductive Activation of Hypoxia-Selective Anticancer Prodrugs
by Shen, Xiulong and Laber, Charles H and Sarkar, Ujjal and Galazzi, Fabio and Johnson, Kevin M and Mahieu, Nathaniel G and Hillebrand, Roman and Fuchs-Knotts, Tarra and Barnes, Charles L and Baker, Gary A and Gates, Kent S
Journal of Organic Chemistry, ISSN 0022-3263, 03/2018, Volume 83, Issue 6, pp. 3126 - 3131
Hypoxia-selective cytotoxins (HSCs) seek to exploit the oxygen poor nature of tumor tissue for therapeutic gain. Typically, HSCs require activation by... 
DNA STRAND CLEAVAGE | ANTITUMOR AGENTS | 3-AMINO-1,2,4-BENZOTRIAZINE 1,4-DIOXIDE TIRAPAZAMINE | 1,2,4-BENZOTRIAZINE 1,4-DIOXIDES | ENZYMATIC CONVERSION | TUMOR HYPOXIA | P450 REDUCTASE | CHEMISTRY, ORGANIC | SR-4233 | ONE-ELECTRON REDUCTASES | CANCER-THERAPY
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17. Full Text Transferring oxygen isotopes to 1,2,4-benzotriazine 1-oxides forming the corresponding 1,4-dioxides by using the HOF·CH 3CN complex
by Gatenyo, Julia and Johnson, Kevin and Rajapakse, Anuruddha and Gates, Kent S and Rozen, Shlomo
Tetrahedron, ISSN 0040-4020, 10/2012, Volume 68, Issue 43, pp. 8942 - 8944
Heterocyclic benzotriazine N-oxides are an interesting class of experimental anticancer and antibacterial agents. Analogs with O incorporated into the N-oxide... 
HOF·CH | O isotope | N-oxide | Oxygen transfer | Tirapazamine
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18. Full Text Selective tumor hypoxia targeting by hypoxia-activated prodrug TH-302 inhibits tumor growth in preclinical models of cancer
by Sun, Jessica D and Liu, Qian and Wang, Jingli and Ahluwalia, Dharmendra and Ferraro, Damien and Wang, Yan and Duan, Jian-Xin and Ammons, W. Steve and Curd, John G and Matteucci, Mark D and Hart, Charles P
Clinical Cancer Research, ISSN 1078-0432, 02/2012, Volume 18, Issue 3, pp. 758 - 770
Purpose: Tumor hypoxia underlies treatment failure and yields a more aggressive, invasive, and metastatic cancer phenotype. TH-302 is a 2-nitroimidazole... 
OXYGENATION PREDICTS | RADIATION RESPONSE | LUNG-CANCER | APOPTOSIS | ONCOLOGY | MUSTARDS | PHASE-1 | VASCULAR DYSFUNCTION | SQUAMOUS-CELL CARCINOMA | TIRAPAZAMINE | FAILURE | Immunohistochemistry | Cell Hypoxia - drug effects | Nitroimidazoles - pharmacology | Phosphoramide Mustards - pharmacology | Humans | Neovascularization, Pathologic | Mice, SCID | Xenograft Model Antitumor Assays | Animals | Cell Line, Tumor | Female | Antineoplastic Agents - pharmacology | Mice | Neoplasms, Experimental - drug therapy | Prodrugs - pharmacology | Neoplasms, Experimental - blood supply
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19. Full Text Hypoxia-activated prodrugs: Paths forward in the era of personalised medicine
by Hunter, Francis W and Wouters, Bradly G and Wilson, William R
British Journal of Cancer, ISSN 0007-0920, 05/2016, Volume 114, Issue 10, pp. 1071 - 1077
Tumour hypoxia has been pursued as a cancer drug target for over 30 years, most notably using bioreductive (hypoxia-activated) prodrugs that target... 
evofosfamide | prodrug | hypoxia | tarloxotinib | P450 oxidoreductase | PR-104 | tirapazamine | biomarker | TUMOR HYPOXIA | GENE-EXPRESSION CLASSIFIER | DINITROBENZAMIDE MUSTARD PR-104A | NECK-CANCER | POSITRON-EMISSION-TOMOGRAPHY | ONCOLOGY | ACUTE LYMPHOBLASTIC-LEUKEMIA | PROSTATE-CANCER | KETO REDUCTASE 1C3 | HOMOLOGOUS RECOMBINATION | SQUAMOUS-CELL CARCINOMAS | Cell Hypoxia | Neoplasms - metabolism | Oxidoreductases - metabolism | Humans | Antineoplastic Agents - pharmacology | Antineoplastic Agents - therapeutic use | Prodrugs - therapeutic use | Prodrugs - pharmacology | Neoplasms - drug therapy | Precision Medicine | Minireview
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20. Full Text Distribution of Hematopoietic Stem Cells in the Bone Marrow According to Regional Hypoxia
by Kalindi Parmar and Peter Mauch and Jo-Anne Vergilio and Robert Sackstein and Julian D. Down
Proceedings of the National Academy of Sciences of the United States of America, ISSN 0027-8424, 3/2007, Volume 104, Issue 13, pp. 5431 - 5436
The interaction of stem cells with their bone marrow microenvironment is a critical process in maintaining normal hematopoiesis. We applied an approach to... 
T lymphocytes | Oxygen | Dyes | B lymphocytes | Perfusion | Stem cells | Bone marrow | Antibodies | Hypoxia | Bone marrow cells | Hoechst perfusion | Tirapazamine | Gradient pimonidazole | Niche oxygen | Stem cell | oxygen gradient | PROGENITOR CELLS | stem cell niche | SIDE POPULATION CELLS | TELOMERASE | MULTIDISCIPLINARY SCIENCES | tirapazamine | REGULATORY FACTOR | NICHE | OSTEOPONTIN | ENGRAFTMENT | IN-VIVO | ARCHITECTURE | MEASURING TUMOR HYPOXIA | pimonidazole | Triazines - pharmacology | Nitroimidazoles - pharmacology | Bone Marrow Cells - cytology | Mice, Inbred C57BL | Stem Cells - cytology | Oxygen - metabolism | Hematopoietic System | Animals | Hematopoietic Stem Cells - cytology | Benzimidazoles - pharmacology | Cell Differentiation | Mice | Research | Hematopoietic stem cells | Distribution | Drugs | Cellular biology | Toxicity | Biological Sciences
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