Welsh School of Pharmacy

2007:

Gomaa, M. S. et al. 2007. Homology model of 1α,25-dihydroxyvitamin D3 24-hydroxylase cytochrome P450 24A1 (CYP24A1): active site architecture and ligand binding. Journal of Steroid Biochemistry and Molecular Biology 104(1-2), pp. 53-60.

2006:

Gomaa, M. S., Yee, S. W., Milbourne, C. E., Barbera, M. C., Simons, C. & Brancale, A. 2006. Homology model of human retinoic acid metabolising enzyme cytochrome P450 26A1 (CYP26A1): Active site architecture and ligand binding. Journal of Enzyme Inhibition and Medicinal Chemistry 21(4), pp. 361-369.

Pautus, S., Yee, S. W., Jayne, M., Coogan, M. P. & Simons, C. 2006. Synthesis and CYP26A1 inhibitory activity of 1-[benzofuran-2-yl-(4-alkyl/aryl-phenyl)-methyl]-1H-triazoles. Bioorganic & Medicinal Chemistry 14(11), pp. 3643-3653.

Saberi, M. R., Vinh, T. K., Yee, S. W., Griffiths, B. J. N., Evans, P. J. & Simons, C. 2006. Potent CYP19 (aromatase) 1-[(benzofuran-2-yl)(phenylmethyl)pyridine, -imidazole, and -triazole inhibitors: Synthesis and biological evaluation. Journal of Medicinal Chemistry 49(3), pp. 1016-1022.

Yee, S. W., Campbell, M. J. & Simons, C. 2006. Inhibition of Vitamin D-3 metabolism enhances VDR signalling in androgen-independent prostate cancer cells. Journal of Steroid Biochemistry and Molecular Biology 98(4-5), pp. 228-235.

2005:

Angotti, M., Hartmann, R. W., Kirby, A. J., Simons, C., Nicholls, P. J., Sewell, R. D. E. & Smith, H. J. 2005. Effect of 2-(4-aminophenylmethyl)-6-hydroxy-3, 4-dihydronaphthalen-1 (2H)-one on all-trans and 13-cis-retinoic acid levels in plasma quantified by high perfomance liquid chromatography coupled to tandem mass spectrometry. Journal of Enzyme Inhibition and Medicinal Chemistry 20(3), pp. 219-226.

Jasamai, M. & Simons, C. 2005. Synthesis of novel 6-azapyrimidine thionucleoside analogues. BPC Science Proceedings A047, pp. S-33.

Saberi, M. R., Shah, K. & Simons, C. 2005. Benzofuran- and furan-2-yl-(phenyl)-3-pyridylmethanols: Synthesis and inhibition of P450 aromatase. Journal of Enzyme Inhibition and Medicinal Chemistry 20(2), pp. 135-141.

Simons, C. 2005. Nucleoside and nucleotide therapeutics: Recent targets in medicinal chemistry. Current Topics in Medicinal Chemistry 5(13), pp. 1189-1190.

Simons, C. & Russell, A. D. 2005. Design of antibacterial, antifungal and antiviral agents. In: Smith, H.J. ed. Introduction to the Principles of Drug Design and Action. 4th ed. Florida, USA: CRC Press, Taylor & Francis Books, pp. 557-615.

Simons, C., Wu, Q. P. & Htar, T. T. 2005. Recent advances in antiviral nucleoside and nucleotide therapeutics. Current Topics in Medicinal Chemistry 5(13), pp. 1191-1203.

Yee, S. W., Jarno, L., Gomaa, M. S., Elford, C., Ooi, L. L., Coogan, M. P., McClelland, R., Nicholson, R. I., Evans, B. A. J., Brancale, A. & Simons, C. 2005. Novel tetralone-derived retinoic acid metabolism blocking agents: Synthesis and in vitro evaluation with liver microsomal and MCF-7 CYP26A1 cell assays. Journal of Medicinal Chemistry 48(23), pp. 7123-7131.

Yee, S. W., Jarno, L., Simons, C., Brancale, A. & Nicholson, R. L. 2005. Synthesis and evaluation of retinoic acid metabolism blocking agents (RAMBAS) as indirect differentiating agents for cancer therapeutics. Abstracts of Papers of the American Chemical Society 229, pp. U161-U161.

Yee, S. W., Shah, B. & Simons, C. 2005. Synthesis and antimycobacterial activity of 7-O-substituted-4-methyl-2H-2-chromenone derivatives vs Mycobacterium tuberculosis. Journal of Enzyme Inhibition and Medicinal Chemistry 20(2), pp. 109-113.

2004:

Abulrob, A. N., Suller, M. T. E., Gumbleton, M., Simons, C. & Russell, A. D. 2004. Identification and biological evaluation of grapefruit oil components as potential novel efflux pump modulators in methicillin-resistant Staphylococcus aureus bacterial strains. Phytochemistry 65(22), pp. 3021-3027.

Kifli, N., De Clercq, E., Balzarini, J. & Simons, C. 2004. Novel imidazo[1,2-c]pyrimidine base-modified nucleosides: synthesis and antiviral evaluation. Bioorganic & Medicinal Chemistry 12(15), pp. 4245-4252.

Kifli, N., Htar, T. T., De Clercq, E., Balzarini, J. & Simons, C. 2004. Novel bicyclic sugar modified nucleosides: synthesis, conformational analysis and antiviral evaluation. Bioorganic & Medicinal Chemistry 12(12), pp. 3247-3257.

Maslen, H. L., Hughes, D., Hursthouse, M., De Clercq, E., Balzarini, J. & Simons, C. 2004. 6-Azapyrimidine-2 '-deoxy-4 '-thionucleosides: Antiviral agents against TK+ and TK- HSV and VZV strains. Journal of Medicinal Chemistry 47(22), pp. 5482-5491.

Smith, H. J. & Simons, C. eds. 2004. Enzymes and Their Inhibitors: Drug Development. Boca Raton, Florida: CRC Press, Taylor & Francis Books.

Smith, H. J. & Simons, C. 2004. Development of enzyme inhibitors as drugs. In: Smith, H.J. & Simons, C. eds. Enzymes and Their Inhibitors: Drug Development.  Florida, USA: CRC Press, Taylor & Francis Books, pp. 171-300.

Wu, Q. P. & Simons, C. 2004. Synthetic methodologies for C-nucleosides. Synthesis-Stuttgart (10), pp. 1533-1553.

Yee, S. W. & Simons, C. 2004. Synthesis and evaluation of tetralone derivatives: P450 enzyme inhibitors as differentiating agents for the treatment of hormone-refractory prostate cancer. Journal of Pharmacy and Pharmacology 56(Suppl), p. 159.

Yee, S. W. & Simons, C. 2004. Synthesis and CYP24 inhibitory activity of 2-substituted-3,4-dihydro-2H-naphthalen-1-one (tetralone) derivatives. Bioorganic & Medicinal Chemistry Letters 14(22), pp. 5651-5654.

2003:

Bueno, G. J., Klimkait, T., Gilbert, I. H. & Simons, C. 2003. Solid-phase synthesis of diamine and polyamine amino acid derivatives as HIV-1 Tat-TAR binding inhibitors. Bioorganic & Medicinal Chemistry 11(1), pp. 87-94.

Greer, V. P., Mason, P., Kirby, A. J., Smith, H. J., Nicholls, P. J. & Simons, C. 2003. Some 1,2-diphenylethane derivatives as inhibitors of retinoic acid-metabolising enzymes. Journal of Enzyme Inhibition and Medicinal Chemistry 18(5), pp. 431-443.

Kirby, A. J., Le Lain, R., Maharlouie, F., Mason, P., Nicholls, P. J., Smith, H. J. & Simons, C. 2003. Inhibition of retinoic acid metabolising enzymes by 2-(4-aminophenylmethyl)-6-hydroxy-3,4-dihydronaphthalen-1(2H)-one and related compounds. Journal of Enzyme Inhibition and Medicinal Chemistry 18(1), pp. 27-33.

Mason, P., Greer, V. P., Kirby, A. J., Simons, C., Nicholls, P. J. & Smith, H. J. 2003. Some aryl substituted 2-(4-nitrophenyl)-4-oxo-4-phenylbutanoates and 3-(4-nitrophenyl)-1-phenyl-1,4-butanediols and related compounds as inhibitors of rat liver microsomal retinoic acid metabolising enzymes. Journal of Enzyme Inhibition and Medicinal Chemistry 18(6), pp. 511-528.

2002:

Kirby, A. J., Lelain, R., Mason, P., Maharlouie, F., Nicholls, P. J., Smith, H. J. & Simons, C. 2002. Some 3-(4-aminophenyl)pyrrolidine-2,5-diones as all-trans-retinoic acid metabolising enzyme inhibitors (RAMBAs). Journal of Enzyme Inhibition and Medicinal Chemistry 17(5), pp. 321-327.

Le Lain, R., Barrell, K. J., Saeed, G. S., Nicholls, P. J., Simons, C., Kirby, A. & Smith, H. J. 2002. Some coumarins and triphenylethene derivatives as inhibitors of human testes microsomal 17 beta-hydroxysteroid dehydrogenase (17 beta-HSD type 3): Further studies with tamoxifen on the rat testes microsomal enzyme. Journal of Enzyme Inhibition and Medicinal Chemistry 17(2), pp. 93-100.

Smith, H. J. & Simons, C. eds. 2002. Proteinase and Peptidase Inhibition: Recent Potential Targets for Drug Development. London and New York: Taylor & Francis.

2001:

Huntley, C. M., Cotterill, A. S., Maillard, J. Y., Balzarini, J. & Simons, C. 2001. Synthesis and biological evaluation of pyridin-2-one nucleosides. Nucleosides Nucleotides & Nucleic Acids 20(4-7), pp. 731-733.

Kifli, N. & Simons, C. 2001. Synthesis of novel conformationally restrained nucleosides. Antiviral Research (49), p. A22.

Le Lain, R. et al. 2001. Some coumarin and triphenylethene derivatives as inhibitors of human testes microsomal 17 beta-hydroxysteroid dehydrogenase (17 beta-HSD): lead anti-prostatic cancer agents. BPC Science Proceedings, p. A222.

Molina, J., Maslen, H. L. & Simons, C. 2001. Methyl 5-O-benzoyl-2,3-oxazole-D-ribofuranoside: A useful intermediate for the synthesis of conformationally restrained nucleosides. Nucleosides Nucleotides & Nucleic Acids 20(4-7), pp. 981-983.

Saberi, M. R. et al. 2001. 1-[(Benzofuran-2-yl)phenylmethyl] pyridines as inhibitors of P450 aromatase. BPC Science Proceedings, p. A224.

Simons, C. 2001. Nucleoside Mimetics: Their Chemistry and Biological Properties. Gordon and Breach Science Publishers, p. 191.

Smith, H. J., Nicholls, P. J., Simons, C. & Le Lain, R. 2001. Inhibitors of steroidogenesis as agents for the treatment of hormone-dependent cancers. Expert Opinion on Therapeutic Patents 11(5), pp. 789-824.

Vinh, T. K., Nicholls, P. J., Kirby, A. J. & Simons, C. 2001. Evaluation of 7-hydroxy-flavones as inhibitors of oestrone and oestradiol biosynthesis. Journal of Enzyme Inhibition 16(5), pp. 417-424.

Vinh, T. K., Yee, S. W., Kirby, A. J., Nicholls, P. J. & Simons, C. 2001. 1-[(Benzofuran-2-yl) phenylmethyl] triazoles as steroidogenic inhibitors: synthesis and in vitro inhibition of human placental CYP19 aromatase. Anti-Cancer Drug Design 16(4-5), pp. 217-225.

Yee, S. W. et al. 2001. Substituted coumarins as inhibitors of type 3 17 beta-hydroxysteroid dehydrogenase. BPC Science Proceedings, p. A223.