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All Outputs (17)

Probing the Mechanism of Action of Bis(phenolato) Amine (ONO Donor Set) Titanium(IV) Anticancer Agents (2024)
Journal Article
Musa, M., Abid, M., Bradshaw, T. D., Boocock, D. J., Coveney, C., Argent, S. P., & Woodward, S. (2024). Probing the Mechanism of Action of Bis(phenolato) Amine (ONO Donor Set) Titanium(IV) Anticancer Agents. Journal of Medicinal Chemistry, 67(4), 2732-2744. https://doi.org/10.1021/acs.jmedchem.3c01874

The need for anticancer therapies that overcome metallodrug resistance while minimizing adverse toxicities is targeted, herein, using titanium coordination complexes. Octahedral titanium­(IV) trans, mer-[Ti­{R1N­(CH2–2-MeO-4-R1-C6H2)2}2] [R1 = Et, al... Read More about Probing the Mechanism of Action of Bis(phenolato) Amine (ONO Donor Set) Titanium(IV) Anticancer Agents.

Correction to “Apoferritin-Encapsulated Jerantinine A for Transferrin Receptor Targeting and Enhanced Selectivity in Breast Cancer Therapy” (2023)
Journal Article
Abuzaid, H., Abdelrazig, S., Ferreira, L., Collins, H. M., Kim, D., Lim, K., …Bradshaw, T. D. (2024). Correction to “Apoferritin-Encapsulated Jerantinine A for Transferrin Receptor Targeting and Enhanced Selectivity in Breast Cancer Therapy”. ACS Omega, 9(1), Article 2012. https://doi.org/10.1021/acsomega.3c09291

Neil R. Thomas was added as an author. The change in authorship is reflected in the authorship of this Correction.

Discovery of new imidazotetrazinones with potential to overcome tumor resistance (2023)
Journal Article
Summers, H. S., Lewis, W., Williams, H. E. L., Bradshaw, T. D., Moody, C. J., & Stevens, M. F. G. (2023). Discovery of new imidazotetrazinones with potential to overcome tumor resistance. European Journal of Medicinal Chemistry, 257, Article 115507. https://doi.org/10.1016/j.ejmech.2023.115507

We describe the design, organic synthesis, and characterization, including X-ray crystallography, of a series of novel analogues of the clinically used antitumor agent temozolomide, together with their in vitro biological evaluation. The work has res... Read More about Discovery of new imidazotetrazinones with potential to overcome tumor resistance.

Highly electron deficient diketopyrrolopyrroles (2023)
Journal Article
Humphreys, J., Malagreca, F., Hume, P. A., Davies, E. S., Argent, S. P., Bradshaw, T. D., & Amabilino, D. B. (2023). Highly electron deficient diketopyrrolopyrroles. Chemical Communications, 59(12), 1613-1616. https://doi.org/10.1039/d2cc06770f

The synthesis, spectroelectrochemical and structural characteristics of highly electron-accepting diketopyrrrolopyrrole (DPP) molecules with adjoining pyridinium rings is reported, along with an assessment of their toxicity, which is apparently low.... Read More about Highly electron deficient diketopyrrolopyrroles.

Design, and synthesis of selectively anticancer 4-cyanophenyl substituted thiazol-2-ylhydrazones (2022)
Journal Article
Mehmood, H., Musa, M., Woodward, S., Hossan, M. S., Bradshaw, T. D., Haroon, M., …Akhtar, T. (2022). Design, and synthesis of selectively anticancer 4-cyanophenyl substituted thiazol-2-ylhydrazones. RSC Advances, 12(52), 34126-34141. https://doi.org/10.1039/d2ra03226k

Cyclization of substituted thiosemicarbazones with α-bromo-4-cyanoacetophenone allows rapid single-step sustainable syntheses of 4-cyanophenyl-2-hydrazinylthiazoles libraries (30 examples, 66–79%). All show anticancer efficacy against HCT-116 and MCF... Read More about Design, and synthesis of selectively anticancer 4-cyanophenyl substituted thiazol-2-ylhydrazones.

Near-infrared PbS quantum dots functionalized with affibodies and ZnPP for targeted imaging and therapeutic applications (2021)
Journal Article
Al-Ani, A. W., Zamberlan, F., Ferreira, L., Bradshaw, T. D., Thomas, N. R., & Turyanska, L. (2021). Near-infrared PbS quantum dots functionalized with affibodies and ZnPP for targeted imaging and therapeutic applications. Nano Express, 2(4), Article 040005. https://doi.org/10.1088/2632-959x/ac33b8

We report a new theranostic device based on lead sulfide quantum dots (PbS QDs) with optical emission in the near infrared wavelength range decorated with affibodies (small 6.5 kDa protein-based antibody replacements) specific to the cancer biomarker... Read More about Near-infrared PbS quantum dots functionalized with affibodies and ZnPP for targeted imaging and therapeutic applications.

Protein Encapsulation of Experimental Anticancer Agents 5F 203 and Phortress: Towards Precision Drug Delivery (2019)
Journal Article
Breen, A. F., Scurr, D., Cassioli, M. L., Wells, G., Thomas, N. R., Zhang, J., …Bradshaw, T. D. (2019). Protein Encapsulation of Experimental Anticancer Agents 5F 203 and Phortress: Towards Precision Drug Delivery. International Journal of Nanomedicine, 14, 9525-9534. https://doi.org/10.2147/IJN.S226293

Introduction: Advancment of novel anticancer drugs into clinic is frequently halted by their lack of solubility, reduced stability under physiological conditions, and non-specific uptake by normal tissues, causing systemic toxicity. Their progress to... Read More about Protein Encapsulation of Experimental Anticancer Agents 5F 203 and Phortress: Towards Precision Drug Delivery.

In search of effective therapies to overcome resistance to Temozolomide in brain tumours (2019)
Journal Article
Grundy, R., Bouzinab, K., Summers, H., Zhang, J., Stevens, M. F. G., Moody, C. J., …Bradshaw, T. D. (2019). In search of effective therapies to overcome resistance to Temozolomide in brain tumours. Cancer Drug Resistance, 2(4), 1018-1031. https://doi.org/10.20517/cdr.2019.64

Glioblastoma multiforme is the most common and lethal brain tumour-type. The current standard of care includes Temozolomide (TMZ) chemotherapy. However, inherent and acquired resistance to TMZ thwart successful treatment. The direct repair protein me... Read More about In search of effective therapies to overcome resistance to Temozolomide in brain tumours.

Synthesis of folic acid functionalized gold nanoclusters for targeting folate receptor-positive cells (2019)
Journal Article
Liu, Z., Turyanska, L., Zamberlan, F., Pacifico, S., Bradshaw, T. D., Moro, F., …Thomas, N. R. (2019). Synthesis of folic acid functionalized gold nanoclusters for targeting folate receptor-positive cells. Nanotechnology, 30(50), Article 505102. https://doi.org/10.1088/1361-6528/ab437c

We report on the synthesis of water-soluble gold nanoclusters capped with polyethylene glycol (PEG)-based ligands and further functionalized with folic acid for specific cellular uptake. The dihydrolipoic acid-PEG-based ligands terminated with -OMe,... Read More about Synthesis of folic acid functionalized gold nanoclusters for targeting folate receptor-positive cells.

Synthesis of highly substituted 1,2-diazetidin-3-ones, small ring scaffolds for drug discovery (2018)
Journal Article
Santos, M. S., Nortcliffe, A., Lewis, W., Bradshaw, T. D., & Moody, C. J. (in press). Synthesis of highly substituted 1,2-diazetidin-3-ones, small ring scaffolds for drug discovery. Chemistry - A European Journal, https://doi.org/10.1002/chem.201801309

1,2-Diazetidin-3-ones are readily accessible, small ring scaffolds that upon functionalization have the potential to produce diverse 3-dimensional structures for drug discovery. Thus treatment of diazo hydrazides, obtained from simple hydrazides and... Read More about Synthesis of highly substituted 1,2-diazetidin-3-ones, small ring scaffolds for drug discovery.

Synthesis and growth-inhibitory activities of imidazo[5,1-d]-1,2,3,5-tetrazine-8-carboxamides related to the anti-tumour drug temozolomide, with appended silicon, benzyl and heteromethyl groups at the 3-position (2018)
Journal Article
Cousin, D., Hummersone, M., Bradshaw, T. D., Zhang, J., Moody, C. J., Foreiter, M., …Stevens, M. F. (in press). Synthesis and growth-inhibitory activities of imidazo[5,1-d]-1,2,3,5-tetrazine-8-carboxamides related to the anti-tumour drug temozolomide, with appended silicon, benzyl and heteromethyl groups at the 3-position. MedChemComm, https://doi.org/10.1039/C7MD00554G

A series of 3-(benzyl-substituted)-imidazo[5,1-d]-1,2,3,5-tetrazines (13) and related derivatives with 3-heteromethyl groups has been synthesised and screened for growth-inhibitory activity in vitro against two pairs of glioma cell lines with temozol... Read More about Synthesis and growth-inhibitory activities of imidazo[5,1-d]-1,2,3,5-tetrazine-8-carboxamides related to the anti-tumour drug temozolomide, with appended silicon, benzyl and heteromethyl groups at the 3-position.

Stable DHLA–PEG capped PbS quantum dots: from synthesis to near-infrared biomedical imaging (2018)
Journal Article
Zamberlan, F., Turyanska, L., Patanè, A., Liu, Z., Williams, H., Fay, M., …Grabowska, A. (in press). Stable DHLA–PEG capped PbS quantum dots: from synthesis to near-infrared biomedical imaging. Journal of Materials Chemistry B, 6, https://doi.org/10.1039/c7tb02912h

The short shelf-life of water-soluble quantum dots (QDs) due to colloidal instability represents a major drawback to their exploitation. This work examines the colloidal stability of PbS nanoparticles capped with dihydrolipoic acid–polyethylene glyco... Read More about Stable DHLA–PEG capped PbS quantum dots: from synthesis to near-infrared biomedical imaging.

Development of a series of bis-triazoles as G-quadruplex ligands (2017)
Journal Article
Saleh, M., Laughton, C. A., Bradshaw, T. D., & Moody, C. J. (in press). Development of a series of bis-triazoles as G-quadruplex ligands. RSC Advances, 7, https://doi.org/10.1039/c7ra07257k

Maintenance of telomeres – specialized complexes that protect the ends of chromosomes – is provided by the enzyme complex telomerase, which is a key factor that is activated in more than 80% of cancer cells, but absent in most normal cells. Targeting... Read More about Development of a series of bis-triazoles as G-quadruplex ligands.

Using titanium complexes to defeat cancer: the view from the shoulders of titans (2017)
Journal Article
Cini, M., Bradshaw, T. D., & Woodward, S. (in press). Using titanium complexes to defeat cancer: the view from the shoulders of titans. Chemical Society Reviews, https://doi.org/10.1039/C6CS00860G

When the first titanium complex with anticancer activity was identified in the 1970s, it was attractive, based on the presence of the dichloride unit in TiCl2Cp2 (Cp = ?-C5H5)2, to assume its mode of biological action was closely aligned with cisplat... Read More about Using titanium complexes to defeat cancer: the view from the shoulders of titans.

Asymmetric pentafulvene carbometalation-access to enantiopure titanocene dichlorides of biological relevance (2015)
Journal Article
Cini, M., Bradshaw, T. D., Woodward, S., & Lewis, W. (2015). Asymmetric pentafulvene carbometalation-access to enantiopure titanocene dichlorides of biological relevance. Angewandte Chemie International Edition, 54(47), https://doi.org/10.1002/anie.201508034

Unprecedented asymmetric copper-catalyzed addition of ZnEt2 (ZnBu2) to the exocyclic C[DOUBLE BOND]C bond of pentafulvenes C5H4([DOUBLE BOND]CHAr) (Ar=2-MeOPh and related species) results in enantiomerically enriched (up to 93:7 e.r.) cyclopentadieny... Read More about Asymmetric pentafulvene carbometalation-access to enantiopure titanocene dichlorides of biological relevance.

Cuprate addition to a 6-substituted pentafulvene: preparation of sec-alkyl substituted titanocene dichlorides and their biological activity (2013)
Journal Article
Cini, M., Bradshaw, T. D., Lewis, W., & Woodward, S. (2013). Cuprate addition to a 6-substituted pentafulvene: preparation of sec-alkyl substituted titanocene dichlorides and their biological activity. European Journal of Organic Chemistry, 2013(19),

The copper-catalysed (10 mol-% CuBr·SMe2, CuCN·LiCl or CuI/PPh3) addition of RMgBr to the pentafulvene 1-(cyclopenta-2,4-dien-1-ylidenemethyl)-2-methoxybenzene allows the formation of cyclopentadienyl derivatives with α-CHR(2-MeOPh) sidechains (R = M... Read More about Cuprate addition to a 6-substituted pentafulvene: preparation of sec-alkyl substituted titanocene dichlorides and their biological activity.