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All Outputs (47)

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.

Oral lipid-based formulations alter delivery of cannabidiol to different anatomical regions in the brain (2023)
Journal Article
Brookes, A., Jewell, A., Feng, W., Bradshaw, T. D., Butler, J., & Gershkovich, P. (2023). Oral lipid-based formulations alter delivery of cannabidiol to different anatomical regions in the brain. International Journal of Pharmaceutics, 635, Article 122651. https://doi.org/10.1016/j.ijpharm.2023.122651

Delivery to the brain is a challenging task due to its protection by the blood–brain barrier (BBB). Lipids and fatty acids are reported to affect the permeability of the BBB, although this has not been reported following oral administration. Cannabid... Read More about Oral lipid-based formulations alter delivery of cannabidiol to different anatomical regions in the brain.

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.

In Vitro Anticancer Properties of Novel Bis-Triazoles (2022)
Journal Article
Saleh, M. M., Abuarqoub, D. A., Hammad, A. M., Hossan, M. S., Ahmed, N., Aslam, N., …Bradshaw, T. D. (2023). In Vitro Anticancer Properties of Novel Bis-Triazoles. Current Issues in Molecular Biology, 45(1), 175-196. https://doi.org/10.3390/cimb45010014

Here, we describe the anticancer activity of our novel bis-triazoles MS47 and MS49, developed previously as G-quadruplex stabilizers, focusing specifically upon the human melanoma MDA-MB-435 cell line. At the National Cancer Institute (NCI), USA, bis... Read More about In Vitro Anticancer Properties of Novel Bis-Triazoles.

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.

Apoferritin-Encapsulated Jerantinine A for Transferrin Receptor Targeting and Enhanced Selectivity in Breast Cancer Therapy (2022)
Journal Article
Abuzaid, H., Abdelrazig, S., Ferreira, L., Collins, H. M., Kim, D. H., Lim, K. H., …Bradshaw, T. D. (2022). Apoferritin-Encapsulated Jerantinine A for Transferrin Receptor Targeting and Enhanced Selectivity in Breast Cancer Therapy. ACS Omega, https://doi.org/10.1021/acsomega.2c00997

The O-acetyl (or acetate) derivative of the Aspidosperma alkaloid Jerantinine A (JAa) elicits anti-tumor activity against cancer cell lines including mammary carcinoma cell lines irrespective of receptor status (0.14 < GI 50 < 0.38 μM), targeting mic... Read More about Apoferritin-Encapsulated Jerantinine A for Transferrin Receptor Targeting and Enhanced Selectivity in Breast Cancer Therapy.

Apoferritin-Encapsulated Jerantinine A for Transferrin Receptor Targeting and Enhanced Selectivity in Breast Cancer Therapy (2022)
Journal Article
Abuzaid, H., Abdelrazig, S., Ferreira, L., Collins, H. M., Kim, D., Lim, K., …Bradshaw, T. (2022). Apoferritin-Encapsulated Jerantinine A for Transferrin Receptor Targeting and Enhanced Selectivity in Breast Cancer Therapy. ACS Omega, 7(25), 21473-21482. https://doi.org/10.1021/acsomega.2c00997

he O-acetyl (or acetate) derivative of the Aspidosperma alkaloid Jerantinine A (JAa) elicits anti-tumor activity against cancer cell lines including mammary carcinoma cell lines irrespective of receptor status (0.14 < GI50 < 0.38 μM), targeting micro... Read More about Apoferritin-Encapsulated Jerantinine A for Transferrin Receptor Targeting and Enhanced Selectivity in Breast Cancer Therapy.

Pro-inflammatory effects of silver nanoparticles in the intestine (2022)
Journal Article
Sousa, A., Bradshaw, T. D., Ribeiro, D., Fernandes, E., & Freitas, M. (2022). Pro-inflammatory effects of silver nanoparticles in the intestine. Archives of Toxicology, 96(6), 1551-1571. https://doi.org/10.1007/s00204-022-03270-w

Nanotechnology is a promising technology of the twenty-first century, being a rapidly evolving field of research and industrial innovation widely applied in our everyday life. Silver nanoparticles (AgNP) are considered the most commercialized nanosys... Read More about Pro-inflammatory effects of silver nanoparticles in the intestine.

Apoferritin and Dps as drug delivery vehicles: Some selected examples in oncology (2021)
Journal Article
Kuruppu, A. I., Turyanska, L., Bradshaw, T. D., Manickam, S., Galhena, B. P., Paranagama, P., & De Silva, R. (2022). Apoferritin and Dps as drug delivery vehicles: Some selected examples in oncology. BBA - General Subjects, 1866(2), Article 130067. https://doi.org/10.1016/j.bbagen.2021.130067

Background: The ideal nanoparticle should be able to encapsulate either pharmaceutical agents or imaging probes so that it could treat or image clinical tumours by targeting the cancer site efficiently. Further, it would be an added advantage if it d... Read More about Apoferritin and Dps as drug delivery vehicles: Some selected examples in oncology.

Concurrent reactive oxygen species generation and aneuploidy induction contribute to thymoquinone anticancer activity (2021)
Journal Article
Al-Hayali, M., Garces, A., Stocks, M., Collins, H., & Bradshaw, T. D. (2021). Concurrent reactive oxygen species generation and aneuploidy induction contribute to thymoquinone anticancer activity. Molecules, 26(17), Article 5136. https://doi.org/10.3390/molecules26175136

Thymoquinone (TQ) is the main biologically active constituent of Nigella sativa. Many studies have confirmed its anticancer actions. Herein, we investigated the different anticancer activities of, and considered resistance mechanisms to, TQ. MTT and... Read More about Concurrent reactive oxygen species generation and aneuploidy induction contribute to thymoquinone anticancer activity.

Chemosensitization of temozolomide-resistant pediatric diffuse midline glioma using potent nanoencapsulated forms of a N(3)-propargyl analogue (2021)
Journal Article
Heravi Shargh, V., Luckett, J., Bouzinab, K., Paisey, S., Turyanska, L., Singleton, W. G., …Coyle, B. (2021). Chemosensitization of temozolomide-resistant pediatric diffuse midline glioma using potent nanoencapsulated forms of a N(3)-propargyl analogue. ACS Applied Materials and Interfaces, 13(30), 35266-35280. https://doi.org/10.1021/acsami.1c04164

The lack of clinical response to the alkylating agent temozolomide (TMZ) in pediatric diffuse midline/intrinsic pontine glioma (DIPG) has been associated with O6-methylguanine-DNA-methyltransferase (MGMT) expression and mismatch repair deficiency. He... Read More about Chemosensitization of temozolomide-resistant pediatric diffuse midline glioma using potent nanoencapsulated forms of a N(3)-propargyl analogue.

Structure-based design of highly selective 2,4,5-trisubstituted pyrimidine CDK9 inhibitors as anti-cancer agents (2021)
Journal Article
Shao, H., Foley, D. W., Huang, S., Abbas, A. Y., Lam, F., Gershkovich, P., …Wang, S. (2021). Structure-based design of highly selective 2,4,5-trisubstituted pyrimidine CDK9 inhibitors as anti-cancer agents. European Journal of Medicinal Chemistry, 214, Article 113244. https://doi.org/10.1016/j.ejmech.2021.113244

Cyclin-dependent kinases (CDKs) are a family of Ser/Thr kinases involved in cell cycle and transcriptional regulation. CDK9 regulates transcriptional elongation and this unique property has made it a potential target for several diseases. Due to the... Read More about Structure-based design of highly selective 2,4,5-trisubstituted pyrimidine CDK9 inhibitors as anti-cancer agents.

The natural alkaloid Jerantinine B has activity in acute myeloid leukemia cells through a mechanism involving c-Jun (2020)
Journal Article
Alhuthali, H. M., Bradshaw, T. D., Lim, K. H., Kam, T. S., & Seedhouse, C. H. (2020). The natural alkaloid Jerantinine B has activity in acute myeloid leukemia cells through a mechanism involving c-Jun. BMC Cancer, 20, Article 629. https://doi.org/10.1186/s12885-020-07119-2

© 2020 The Author(s). Background: Acute myeloid leukemia (AML) is a heterogenous hematological malignancy with poor long-term survival. New drugs which improve the outcome of AML patients are urgently required. In this work, the activity and mechanis... Read More about The natural alkaloid Jerantinine B has activity in acute myeloid leukemia cells through a mechanism involving c-Jun.

New Treatments in Renal Cancer: The AhR Ligands (2020)
Journal Article
Turyanska, L., Itkin, B., Breen, A., Loaiza-Perez, A. I., Sandes, E. O., & Bradshaw, T. D. (2020). New Treatments in Renal Cancer: The AhR Ligands. International Journal of Molecular Sciences, 21(10), https://doi.org/10.3390/ijms21103551

Kidney cancer rapidly acquires resistance to antiangiogenic agents, such as sunitinib, developing an aggressive migratory phenotype (facilitated by c-Metsignal transduction). The Aryl hydrocarbon receptor (AhR) has recently been postulated as a molec... Read More about New Treatments in Renal Cancer: The AhR Ligands.

Modulation of the acidity of the 8-carboxamide group in the temozolomide family of antitumor imidazo[5,1-d][1,2,3,5]tetrazines (2020)
Journal Article
Summers, H. S., Foreiter, M. B., Lewis, W., Moody, C. J., Bradshaw, T. D., & Stevens, M. F. (2020). Modulation of the acidity of the 8-carboxamide group in the temozolomide family of antitumor imidazo[5,1-d][1,2,3,5]tetrazines. Arkivoc, 2020(7), 36-45. https://doi.org/10.24820/ARK.5550190.P011.182

Imidazo[5,1-d][1,2,3,5]tetrazines related in structure to the anticancer drugs temozolomide and mitozolomide with modification of the 8-carboxamide group, have been synthesized, N-nitrocarboxamides by direct nitration of the corresponding carboxamide... Read More about Modulation of the acidity of the 8-carboxamide group in the temozolomide family of antitumor imidazo[5,1-d][1,2,3,5]tetrazines.

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.

Apoferritin encapsulation of cysteine protease inhibitors for cathepsin L inhibition in cancer cells (2019)
Journal Article
Quilles Junior, J. C., Bradshaw, T. D., Turyanska, L., Carlos, F. D. R. R., Montanari, A., Leitão, A., …Bradshaw, T. D. (2019). Apoferritin encapsulation of cysteine protease inhibitors for cathepsin L inhibition in cancer cells. RSC Advances, 9(63), 36699-36706. https://doi.org/10.1039/c9ra07161j

Cysteine proteases play a key role in tumorigenesis causing protein degradation and promoting invasive tumour growth. Cathepsin L is overexpressed in cancer cells and could provide a specific target for delivery of anticancer agents. We encapsulated... Read More about Apoferritin encapsulation of cysteine protease inhibitors for cathepsin L inhibition in cancer cells.

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.