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 Temozolomide analogues. Prodrug design, synthesis, activation kinetics and evaluation.

Existing collaborations relevant to drug delivery

Professor Jarkko Rautio and colleagues, University of Eastern Finland, Kuopio.

Professor Anant Paradkar, University of Bradford.

Publications relevant to drug delivery

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. D. Cousin, M.G. Hummersone, T.D. Bradshaw, J. Zhang, C.J. Moody, M.B. Foreiter, H.S. Summers, W. Lewis, R.T. Wheelhouse and M.F.G. Stevens. Med Chem Comm (2018) 9, 545–553. doi: 10.1039/C7MD00554G.

Evaluation of Novel Imidazotetrazine Analogues Designed to Overcome Temozolomide Resistance and Glioblastoma Regrowth. Y.P. Ramirez, A.C. Mladek, R.M. Phillips, M. Gynther, J. Rautio, A.H. Ross, R.T. Wheelhouse, J.N. Sakaria, Mol. Cancer Ther. (2015) 14, 111–119. doi: 10.1158/1535-7163.MCT-14-0113. PubMed PMID: 25351918.

Synthesis and Quantitative Structure–Activity Relationship of Imidazotetrazine Prodrugs with Activity Independent of O6-Methylguanine-DNA-methyltransferase, DNA Mismatch Repair and p53. D. Pletsas, E.A.E. Garelnabi, L. Li, R.M. Phillips, R.T. Wheelhouse. J. Med. Chem. (2013) 56, 7120–7132. doi:10.1021/jm401121k. PubMed PMID: 23895620.

Strategy for Imidazotetrazines with Anticancer Activity Independent of MGMT and MMR. E.A.E. Garelnabi, D. Pletsas, L. Li, K. Kiakos, N. Karodia, J.A. Hartley, R.M. Phillips and R.T. Wheelhouse. ACS Med. Chem. Lett. (2012) 3, 965–968. doi:10.1021/ml300132t. PubMed PMID: 24900418; PubMed Central PMCID: PMC4025673.