Skip to main content

Research Repository

Advanced Search

All Outputs (7)

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.

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.

Cudraflavone C induces tumor-specific apoptosis in colorectal cancer cells through inhibition of the phosphoinositide 3-kinase (PI3K)-AKT pathway (2017)
Journal Article
Castresana, J. S., Soo, H., Chung, F. F., Lim, K., Yap, V. A., Bradshaw, T. D., …Mai, C. (2017). Cudraflavone C induces tumor-specific apoptosis in colorectal cancer cells through inhibition of the phosphoinositide 3-kinase (PI3K)-AKT pathway. PLoS ONE, 12(1), Article e0170551. https://doi.org/10.1371/journal.pone.0170551

Cudraflavone C (Cud C) is a naturally-occurring flavonol with reported anti-proliferative activities. However, the mechanisms by which Cud C induced cytotoxicity have yet to be fully elucidated. Here, we investigated the effects of Cud C on cell prol... Read More about Cudraflavone C induces tumor-specific apoptosis in colorectal cancer cells through inhibition of the phosphoinositide 3-kinase (PI3K)-AKT pathway.