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Codrug Approach for the Potential Treatment of EML4-ALK Positive Lung Cancer (2019)
Journal Article
Garces, A. E., Al-Hayali, M., Lee, J. B., Li, J., Gershkovich, P., Bradshaw, T. D., & Stocks, M. J. (2020). Codrug Approach for the Potential Treatment of EML4-ALK Positive Lung Cancer. ACS Medicinal Chemistry Letters, 11(3), 316-321. https://doi.org/10.1021/acsmedchemlett.9b00378

We report on the synergistic effect of PI3K inhibition with ALK inhibition for the possible treatment of EML4-ALK positive lung cancer. We have brought together ceritinib (ALK inhibitor) and pictilisib (PI3K inhibitor) into a single bivalent molecule... Read More about Codrug Approach for the Potential Treatment of EML4-ALK Positive Lung Cancer.

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.

C8-substituted imidazotetrazine analogs overcome temozolomide resistance by inducing DNA adducts and DNA damage (2019)
Journal Article
Yang, Z., Wei, D., Dai, X., Stevens, M. F., Bradshaw, T. D., Luo, Y., & Zhang, J. (2019). C8-substituted imidazotetrazine analogs overcome temozolomide resistance by inducing DNA adducts and DNA damage. Frontiers in Oncology, 9, https://doi.org/10.3389/fonc.2019.00485

Copyright © 2019 Yang, Wei, Dai, Stevens, Bradshaw, Luo and Zhang. This is an open-access article distributed under the terms of the Creative Commons Attribution License (CC BY). The use, distribution or reproduction in other forums is permitted, pro... Read More about C8-substituted imidazotetrazine analogs overcome temozolomide resistance by inducing DNA adducts and DNA damage.

A novel low molecular weight nanocomposite hydrogel formulation for intra-tumoural delivery of anti-cancer drugs (2019)
Journal Article
Štaka, I., Cadete, A., Surikutchi, B. T., Abuzaid, H., Bradshaw, T. D., Alonso, M. J., & Marlow, M. (2019). A novel low molecular weight nanocomposite hydrogel formulation for intra-tumoural delivery of anti-cancer drugs. International Journal of Pharmaceutics, 565, 151-161. https://doi.org/10.1016/j.ijpharm.2019.04.070

Herein, an injectable formulation composed of a low molecular weight gelator (LMWG) based hydrogel and drug-loaded polymeric nanocapsules (NCs) is described. The NCs, made of hyaluronic acid and polyglutamic acid and loaded with C14-Gemcitabine (GEM... Read More about A novel low molecular weight nanocomposite hydrogel formulation for intra-tumoural delivery of anti-cancer drugs.

Cardiac glycoside cerberin exerts anticancer activity through PI3K/AKT/mTOR signal transduction inhibition (2019)
Journal Article
Hossan, M. S., Chan, Z. Y., Collins, H. M., Shipton, F. N., Butler, M. S., Rahmatullah, M., …Bradshaw, T. D. (2019). Cardiac glycoside cerberin exerts anticancer activity through PI3K/AKT/mTOR signal transduction inhibition. Cancer Letters, 453, 57-73. https://doi.org/10.1016/j.canlet.2019.03.034

Natural products possess a significant role in anticancer therapy and many currently-used anticancer drugs are of natural origin. Cerberin (CR), a cardenolide isolated from the fruit kernel of Cerbera odollam, was found to potently inhibit cancer cel... Read More about Cardiac glycoside cerberin exerts anticancer activity through PI3K/AKT/mTOR signal transduction inhibition.

Development of novel apoferritin formulations for antitumour benzothiazoles (2019)
Journal Article
Breen, A. F., Wells, G., Turyanska, L., & Bradshaw, T. D. (2019). Development of novel apoferritin formulations for antitumour benzothiazoles. Cancer Reports, 2(4), 1-7. https://doi.org/10.1002/cnr2.1155

Background The benzothiazole structure is important in medicinal chemistry, and 5‐fluoro‐2‐(3,4‐dimethoxyphenyl) benzothiazole (GW 610) is of particular interest as it shows outstanding anticancer activity in sensitive breast and colorectal carcinom... Read More about Development of novel apoferritin formulations for antitumour benzothiazoles.

Cytotoxic potential of ethanol extract of Parquetina nigrescens on MCF-7, C4-2WT, HT 29 and HTC 116 cell lines (2018)
Journal Article
M. Onyegeme-Okerenta, B., Agyare, C., D. Bradshaw, T., & A. Spriggs, K. (2018). Cytotoxic potential of ethanol extract of Parquetina nigrescens on MCF-7, C4-2WT, HT 29 and HTC 116 cell lines. African journal of pharmacy and pharmacology, 12(23), 310-318. https://doi.org/10.5897/ajpp2018.4947

The cytotoxic activity of ethanol extract of Parquetina nigrescen was investigated using a (3-(4, 5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay, methylene blue and Trypan Blue exclusion assay on four human cancer cell lines, MCF... Read More about Cytotoxic potential of ethanol extract of Parquetina nigrescens on MCF-7, C4-2WT, HT 29 and HTC 116 cell lines.

Lipophilic activated ester prodrug approach for drug delivery to the intestinal lymphatic system (2018)
Journal Article
Lee, J. B., Zgair, A., Malec, J., Kim, T. H., Kim, M. G., Ali, J., …Gershkovich, P. (2018). Lipophilic activated ester prodrug approach for drug delivery to the intestinal lymphatic system. Journal of Controlled Release, 286, 10-19. https://doi.org/10.1016/j.jconrel.2018.07.022

The intestinal lymphatic system plays an important role in the pathophysiology of multiple diseases including lymphomas, cancer metastasis, autoimmune diseases, and human immunodeficiency virus (HIV) infection. It is thus an important compartment for... Read More about Lipophilic activated ester prodrug approach for drug delivery to the intestinal lymphatic system.

Sustainable Syntheses of (-)-Jerantinines A & e and Structural Characterisation of the Jerantinine-Tubulin Complex at the Colchicine Binding Site (2018)
Journal Article
Smedley, C. J., Stanley, P. A., Qazzaz, M. E., Prota, A. E., Olieric, N., Collins, H., …Moses, J. E. (2018). Sustainable Syntheses of (-)-Jerantinines A & e and Structural Characterisation of the Jerantinine-Tubulin Complex at the Colchicine Binding Site. Scientific Reports, 8(1), Article 10617. https://doi.org/10.1038/s41598-018-28880-2

The jerantinine family of Aspidosperma indole alkaloids from Tabernaemontana corymbosa are potent microtubule-targeting agents with broad spectrum anticancer activity. The natural supply of these precious metabolites has been significantly disrupted... Read More about Sustainable Syntheses of (-)-Jerantinines A & e and Structural Characterisation of the Jerantinine-Tubulin Complex at the Colchicine Binding Site.

Nucleoside based self-assembling drugs for localized drug delivery (2018)
Journal Article
Skilling, K. J., Stocks, M. J., Kellam, B., Ashford, M., Bradshaw, T., Burroughs, L., & Marlow, M. (in press). Nucleoside based self-assembling drugs for localized drug delivery. ChemMedChem, https://doi.org/10.1002/cmdc.201800063

We have synthesized a range of gelators based on nucleoside analogues gemcitabine and lamivudine, characterizing representative gels from the series using rheology and TEM. Growth inhibition studies of gemcitabine derivatives confirmed the feasibilit... Read More about Nucleoside based self-assembling drugs for localized drug delivery.

Self-assembling benzothiazole-based gelators: a mechanistic understanding of in vitro bioactivation and gelation (2018)
Journal Article
Citossi, F., Smith, T., Lee, J. B., Segal, J., Gershkovich, P., Stocks, M. J., …Marlow, M. (in press). Self-assembling benzothiazole-based gelators: a mechanistic understanding of in vitro bioactivation and gelation. Molecular Pharmaceutics, 15(4), https://doi.org/10.1021/acs.molpharmaceut.7b01106

Low molecular weight gelators (LMWGs) of chemotherapeutic drugs represent a valid alternative to the existing poly-mer-based formulations used for targeted delivery of anticancer drugs. Herein we report the design and development of novel self-assemb... Read More about Self-assembling benzothiazole-based gelators: a mechanistic understanding of in vitro bioactivation and gelation.

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.

Discovery of a highly active anticancer analogue of cardamonin that acts as an inducer of caspase-dependent apoptosis and modulator of the mTOR pathway (2018)
Journal Article
Khaled bin Break, M., Hossan, M. S., Khooa, Y., Emad Qazzaz, M., Al-Hayali, M., Chow, S. C., …Khoo, T. (2018). Discovery of a highly active anticancer analogue of cardamonin that acts as an inducer of caspase-dependent apoptosis and modulator of the mTOR pathway. Fitoterapia, 125, https://doi.org/10.1016/j.fitote.2018.01.006

Nineteen analogues of cardamonin were semi-synthesized and tested against A549 and HK1 cell lines. The analogues were fully characterized via IR and NMR analyses, while compound 19 (a Cu (II) complex of cardamonin) was further characterized via HRMS,... Read More about Discovery of a highly active anticancer analogue of cardamonin that acts as an inducer of caspase-dependent apoptosis and modulator of the mTOR pathway.

Temozolomide analog PMX 465 downregulates MGMT expression in HCT116 colorectal carcinoma cells (2018)
Journal Article
Yang, Z., Wei, D., Liu, F., Liu, J., Wu, X., Stevens, M. F. G., …Zhang, J. (in press). Temozolomide analog PMX 465 downregulates MGMT expression in HCT116 colorectal carcinoma cells. Journal of Cellular Biochemistry, https://doi.org/10.1002/jcb.26674

The efficacy of temozolomide (TMZ) treatment for cancers is currently limited by inherent or the development of resistance, particularly, but not exclusively, due to the expression of the DNA repair enzyme O6-methylguanine-DNA methyltransferase (MGMT... Read More about Temozolomide analog PMX 465 downregulates MGMT expression in HCT116 colorectal carcinoma cells.

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.

Cellular pharmacology studies of anticancer agents: recommendations from the EORTC-PAMM group (2017)
Journal Article
Perego, P., Hempel, G., Linder, S., Bradshaw, T. D., Larsen, A. K., Peters, G. J., & Phillips, R. M. (in press). Cellular pharmacology studies of anticancer agents: recommendations from the EORTC-PAMM group. Cancer Chemotherapy and Pharmacology, https://doi.org/10.1007/s00280-017-3502-7

An increasing number of manuscripts focus on the in vitro evaluation of established and novel anti-tumour agents in experimental models. Whilst the design of such in vitro assays is inherently flexible, some of these studies lack the minimum informat... Read More about Cellular pharmacology studies of anticancer agents: recommendations from the EORTC-PAMM group.

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.

In vitro antitumor effects of AHR ligands aminoflavone (AFP 464) and benzothiazole (5F 203) in human renal carcinoma cells (2017)
Journal Article
Luzzani, G. A., Callero, M. A., Kuruppu, A. I., Trapani, V., Flumian, C., Todaro, L., …Loaiza Perez, A. I. (in press). In vitro antitumor effects of AHR ligands aminoflavone (AFP 464) and benzothiazole (5F 203) in human renal carcinoma cells. Journal of Cellular Biochemistry, https://doi.org/10.1002/jcb.26114

We investigated activity and mechanism of action of two AhR ligand antitumor agents, AFP 464 and 5F 203 on human renal cancer cells, specifically examining their effects on cell cycle progression, apoptosis, and migration. TK-10, SN12C, Caki-1, and A... Read More about In vitro antitumor effects of AHR ligands aminoflavone (AFP 464) and benzothiazole (5F 203) in human renal carcinoma cells.

Jerantinine A induces tumor-specific cell death through modulation of splicing factor 3b subunit 1 (SF3B1) (2017)
Journal Article
Chung, F. F., Tan, P. F. T. M., Raja, V. J., Tan, B., Lim, K., Kam, T., …Leong, C. (2017). Jerantinine A induces tumor-specific cell death through modulation of splicing factor 3b subunit 1 (SF3B1). Scientific Reports, 7(42504), https://doi.org/10.1038/srep42504

Precursor mRNA (pre-mRNA) splicing is catalyzed by a large ribonucleoprotein complex known as the spliceosome. Numerous studies have indicated that aberrant splicing patterns or mutations in spliceosome components, including the splicing factor 3b su... Read More about Jerantinine A induces tumor-specific cell death through modulation of splicing factor 3b subunit 1 (SF3B1).

Design and elaboration of a tractable tricyclic scaffold to synthesize druglike inhibitors of dipeptidyl peptidase-4 (DPP-4), antagonists of the C–C Chemokine Receptor Type 5 (CCR5), and highly potent and selective phosphoinositol-3 Kinase δ (PI3Kδ) inhibitors (2017)
Journal Article
Schwehm, C., Kellam, B., Garces, A., Hill, S. J., Kindon, N., Bradshaw, T. D., …Stocks, M. (2017). Design and elaboration of a tractable tricyclic scaffold to synthesize druglike inhibitors of dipeptidyl peptidase-4 (DPP-4), antagonists of the C–C Chemokine Receptor Type 5 (CCR5), and highly potent and selective phosphoinositol-3 Kinase δ (PI3Kδ) inhibitors. Journal of Medicinal Chemistry, 60(4), https://doi.org/10.1021/acs.jmedchem.6b01801

A novel molecular scaffold has been synthesized, and its incorporation into new analogues of biologically active molecules across multiple target classes will be discussed. In these studies, we have shown use of the tricyclic scaffold to synthesize p... Read More about Design and elaboration of a tractable tricyclic scaffold to synthesize druglike inhibitors of dipeptidyl peptidase-4 (DPP-4), antagonists of the C–C Chemokine Receptor Type 5 (CCR5), and highly potent and selective phosphoinositol-3 Kinase δ (PI3Kδ) inhibitors.