Search Results - "TERCEL, Moana"

Conjugation of Palbociclib with MHI-148 Has an Increased Cytotoxic Effect for Breast Cancer Cells and an Altered Mechanism of Action by Choi, Peter Jaein, Tomek, Petr, Tercel, Moana, Reynisson, Jóhannes, Park, Thomas In Hyeup, Cooper, Elizabeth Alexandra, Denny, William Alexander, Jose, Jiney, Leung, Euphemia

“…The CDK4/6 inhibitor palbociclib, combined with endocrine therapy, has been shown to be effective in postmenopausal women with estrogen receptor-positive,…”
Get full text

Clinical relevance and therapeutic predictive ability of hypoxia biomarkers in head and neck cancer tumour models by Lee, Tet Woo, Singleton, Dean C., Harms, Julia K., Lu, Man, McManaway, Sarah P., Lai, Amy, Tercel, Moana, Pruijn, Frederik B., Macann, Andrew M. J., Hunter, Francis W., Wilson, William R., Jamieson, Stephen M. F.

“…Tumour hypoxia promotes poor patient outcomes, with particularly strong evidence for head and neck squamous cell carcinoma (HNSCC). To effectively target…”
Get full text

Spatially-resolved pharmacokinetic/pharmacodynamic modelling of bystander effects of a nitrochloromethylbenzindoline hypoxia-activated prodrug by Hong, Cho Rong, Mehta, Sunali Y., Liyanage, H. D. Sarath, McManaway, Sarah P., Lee, Ho H., Jaiswal, Jagdish K., Bogle, Gib, Tercel, Moana, Pruijn, Frederik B., Wilson, William R., Hicks, Kevin O.

“…Purpose Hypoxia-activated prodrugs (HAPs) have the potential for eliminating chemo- and radiation-resistant hypoxic tumour cells, but their activity is often…”
Get full text

Engineering the Escherichia coli Nitroreductase NfsA to Create a Flexible Enzyme-Prodrug Activation System by Sharrock, Abigail V, McManaway, Sarah P, Rich, Michelle H, Mumm, Jeff S, Hermans, Ian F, Tercel, Moana, Pruijn, Frederik B, Ackerley, David F

“…Bacterial nitroreductase enzymes that can efficiently convert nitroaromatic prodrugs to a cytotoxic form have numerous applications in targeted cellular…”
Get full text

Nitro-chloromethylbenzindolines: hypoxia-activated prodrugs of potent adenine N3 DNA minor groove alkylators by Wilson, William R, Stribbling, Stephen M, Pruijn, Frederik B, Syddall, Sophie P, Patterson, Adam V, Liyanage, H D Sarath, Smith, Eileen, Botting, K Jane, Tercel, Moana

“…Hypoxia represents an important therapeutic target in tumors because of the resistance of hypoxic cells to radiotherapy and chemotherapy and because it is more…”
Get full text

Hypoxic selectivity and solubility—investigating the properties of A-ring substituted nitro seco-1,2,9,9a-tetrahydrocyclopropa[c]benz[e]indol-4-ones (nitroCBIs) as hypoxia-activated prodrugs for antitumor therapy by Tercel, Moana, Yang, Shangjin, Atwell, Graham J., Smith, Eileen, Gu, Yongchuan, Anderson, Robert F., Denny, William A., Wilson, William R., Pruijn, Frederik B.

“…Nitro seco-1,2,9,9a-tetrahydrocyclopropa[c]benz[e]indol-4-ones (nitroCBIs) are a new class of prodrugs for antitumor therapy that undergo hypoxia-selective…”
Get full text

Optimised synthesis of a nitroCBI hypoxia-activated prodrug with substantial anticancer activity by Lee, Ho H., Dickson, Benjamin D., Stevenson, Ralph J., Yang, Shangjin, Tercel, Moana

“…An optimised synthesis of a hypoxia-activated anticancer prodrug related to the duocarmycin family of natural products is described. The improved 10-step…”
Get full text

Influence of a Basic Side Chain on the Properties of Hypoxia-Selective Nitro Analogues of the Duocarmycins: Demonstration of Substantial Anticancer Activity in Combination with Irradiation or Chemotherapy by Tercel, Moana, Lee, Ho H, Mehta, Sunali Y, Youte Tendoung, Jean-Jacques, Bai, Sally Y, Liyanage, H. D. Sarath, Pruijn, Frederik B

“…A new series of nitro analogues of the duocarmycins was prepared and evaluated for hypoxia-selective anticancer activity. The compounds incorporate 13…”
Get full text

Hypoxia-Selective Antitumor Agents. 12. Nitrobenzyl Quaternary Salts as Bioreductive Prodrugs of the Alkylating Agent Mechlorethamine by Tercel, Moana, Wilson, William R, Anderson, Robert F, Denny, William A

“…A series of benzene-substituted analogues of the novel hypoxia-selective cytotoxin N,N-bis(2-chloroethyl)-N-methyl-N-(2-nitrobenzyl)ammonium chloride (3a),…”
Get full text

Antibody–Drug Conjugates Derived from Cytotoxic seco-CBI-Dimer Payloads Are Highly Efficacious in Xenograft Models and Form Protein Adducts In Vivo by Su, Dian, Chen, Jinhua, Cosino, Ely, dela Cruz-Chuh, Josefa, Davis, Helen, Del Rosario, Geoffrey, Figueroa, Isabel, Goon, Leanne, He, Jintang, Kamath, Amrita V, Kaur, Surinder, Kozak, Katherine R, Lau, Jeffrey, Lee, Donna, Lee, M. Violet, Leipold, Douglas, Liu, Luna, Liu, Peter, Lu, Guo-Liang, Nelson, Chris, Ng, Carl, Pillow, Thomas H, Polakis, Paul, Polson, Andrew G, Rowntree, Rebecca K, Saad, Ola, Safina, Brian, Stagg, Nicola J, Tercel, Moana, Vandlen, Richard, Vollmar, Breanna S, Wai, John, Wang, Tao, Wei, BinQing, Xu, Keyang, Xue, Juanjuan, Xu, Zijin, Yan, Gang, Yao, Hui, Yu, Shang-Fan, Zhang, Donglu, Zhong, Fiona, Dragovich, Peter S

“…This work discloses the first examples of antibody–drug conjugates (ADCs) that are constructed from linker-drugs bearing dimeric seco-CBI payloads (duocarmycin…”
Get full text

Cross-Bridged Cyclen or Cyclam Co(III) Complexes Containing Cytotoxic Ligands as Hypoxia-Activated Prodrugs by Chang, John Yu-Chih, Lu, Guo-Liang, Stevenson, Ralph J, Brothers, Penelope J, Clark, George R, Botting, K. Jane, Ferry, Dianne M, Tercel, Moana, Wilson, William R, Denny, William A, Ware, David C

“…A series of cobalt(III) complexes of the potent DNA minor groove alkylator…”
Get full text

Analogues of DNA minor groove cross-linking agents incorporating aminoCBI, an amino derivative of the duocarmycins: Synthesis, cytotoxicity, and potential as payloads for antibody-drug conjugates by Giddens, Anna C, Lee, Ho H, Lu, Guo-Liang, Miller, Christian K, Guo, Jun, Lewis Phillips, Gail D, Pillow, Thomas H, Tercel, Moana

“…A Pd-catalysed amination method is used to convert seco-CBI, a synthetic analogue of the alkylating subunit of the duocarmycin natural products, from the…”
Get full text

Nitro seco Analogues of the Duocarmycins Containing Sulfonate Leaving Groups as Hypoxia-Activated Prodrugs for Cancer Therapy by Stevenson, Ralph J, Denny, William A, Tercel, Moana, Pruijn, Frederik B, Ashoorzadeh, Amir

“…The synthesis of 19 (5-nitro-2,3-dihydro-1H-benzo[e]indol-1-yl)methyl sulfonate prodrugs containing sulfonate leaving groups and 7-substituted…”
Get full text

The flavoprotein FOXRED2 reductively activates nitro-chloromethylbenzindolines and other hypoxia-targeting prodrugs by Hunter, Francis W., Jaiswal, Jagdish K., Hurley, Daniel G., Liyanage, H.D. Sarath, McManaway, Sarah P., Gu, Yongchuan, Richter, Susan, Wang, Jingli, Tercel, Moana, Print, Cristin G., Wilson, William R., Pruijn, Frederik B.

“…The nitro-chloromethylbenzindoline prodrug SN29428 has been rationally designed to target tumour hypoxia. SN29428 is metabolised to a DNA minor groove…”
Get full text

The Cytotoxicity of Duocarmycin Analogues is Mediated through Alkylation of DNA, not Aldehyde Dehydrogenase 1: A Comment by Tercel, Moana, McManaway, Sarah P., Leung, Euphemia, Liyanage, H. D. Sarath, Lu, Guo-Liang, Pruijn, Frederik B.

“…The answer lies in the DNA: Recent claims that the alkylation of a particular protein contributes to the cytotoxicity of the duocarmycins could not be…”
Get full text

Nitrobenzyl mustard quaternary salts: a new class of hypoxia-selective cytotoxins showing very high in vitro selectivity by Tercel, Moana, Wilson, William R, Denny, William A

Get full text

Selective Treatment of Hypoxic Tumor Cells In Vivo: Phosphate Pre-Prodrugs of Nitro Analogues of the Duocarmycins by Tercel, Moana, Atwell, Graham J, Yang, Shangjin, Ashoorzadeh, Amir, Stevenson, Ralph J, Botting, K. Jane, Gu, Yongchuan, Mehta, Sunali Y, Denny, William A, Wilson, William R, Pruijn, Frederik B

“…Hitting the hypoxic target: Combining a nitro prodrug with a water‐soluble phosphate converts duocarmycin analogues from highly toxic DNA‐alkylating agents to…”
Get full text

Tyrosine kinase inhibitors. 1. Structure-activity relationships for inhibition of epidermal growth factor receptor tyrosine kinase activity by 2,3-dihydro-2-thioxo-1H-indole-3-alkanoic acids and 2,2'-dithiobis(1H-indole-3-alkanoic acids) by Thompson, Andrew M, Rewcastle, Gordon W, Tercel, Moana, Dobrusin, Ellen M, Fry, David W, Kraker, Alan J, Denny, William A

“…A series of 2,3-dihydro-2-thioxo-1H-indole-3-alkanoic acids, and their methyl esters were prepared, the majority by oxidation of 1H-indole-3-alkanoic acids…”
Get full text

Hypoxia-Activated Prodrugs: Substituent Effects on the Properties of Nitro seco-1,2,9,9a-Tetrahydrocyclopropa[c]benz[e]indol-4-one (nitroCBI) Prodrugs of DNA Minor Groove Alkylating Agents by Tercel, Moana, Atwell, Graham J, Yang, Shangjin, Stevenson, Ralph J, Botting, K. Jane, Boyd, Maruta, Smith, Eileen, Anderson, Robert F, Denny, William A, Wilson, William R, Pruijn, Frederik B

“…Nitrochloromethylbenzindolines (nitroCBIs) are a new class of hypoxia-activated prodrugs for antitumor therapy. The recently reported prototypes undergo…”
Get full text

A new enantioselective approach to the core structure of hypoxia selective prodrugs related to the duocarmycins by Heinrich, Daniel M., Youte, Jean-Jacques, Denny, William A., Tercel, Moana

“…The indoline scaffold of hypoxia selective prodrugs of DNA-alkylating agents related to the duocarmycin natural products was synthesized via an…”
Get full text