Outputs (47)

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.