研究领域

Medicinal and Biomolecular Chemistry

In the field of medicinal chemistry, the design of new molecules as potential pharmaceutical agents is of particular interest. The interactions of such small molecules with their protein targets is also a focus. Collaborative work with synthetic chemists at UNSW, School of Chemistry, is concerned with antibacterial agents with a novel mechanism of action and with kinase inhibitors. The antibacterial project also involves collaboration with the University of Newcastle. Collaborative work with colleagues at UNSW, School of Medical Sciences, is concerned with molecules selectively modulating cell signalling through adrenergic receptors, and also with the development of novel anticancer agents.

近期论文

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Thach O; Mielczarek M; Ma C; Kutty SK; Yang X; Black DSC; Griffith R; Lewis PJ; Kumar N, 2016, 'From indole to pyrrole, furan, thiophene and pyridine: Search for novel small molecule inhibitors of bacterial transcription initiation complex formation', Bioorganic and Medicinal Chemistry, vol. 24, no. 6, pp. 1171 - 1182, http://dx.doi.org/10.1016/j.bmc.2016.01.040 Mashkani B; Tanipour MH; Saadatmandzadeh M; Ashman LK; Griffith R, 2016, 'FMS-like tyrosine kinase 3 (FLT3) inhibitors: Molecular docking and experimental studies.', European Journal of Pharmacology, vol. 776, pp. 156 - 166, http://dx.doi.org/10.1016/j.ejphar.2016.02.048 Nizalapur S; Kimyon O; Biswas NN; Gardner CR; Griffith R; Rice SA; Manefield M; Willcox M; Black DS; Kumar N, 2016, 'Design, synthesis and evaluation of N-aryl-glyoxamide derivatives as structurally novel bacterial quorum sensing inhibitors', Organic and Biomolecular Chemistry, vol. 14, no. 2, pp. 680 - 693, http://dx.doi.org/10.1039/c5ob01973g Sele AM; Bremner JB; Willis AC; Haritakun R; Griffith R; Keller PA, 2015, 'A cascade synthetic route to new bioactive spiroindolinepyrido[1,2-a]indolediones from indirubin', Tetrahedron, vol. 71, no. 43, pp. 8357 - 8367, http://dx.doi.org/10.1016/j.tet.2015.08.012 Kutty SK; Barraud N; Ho KKK; Iskander GM; Griffith R; Rice SA; Bhadbhade M; Willcox MDP; Black DS; Kumar N, 2015, 'Hybrids of acylated homoserine lactone and nitric oxide donors as inhibitors of quorum sensing and virulence factors in Pseudomonas aeruginosa', Organic and Biomolecular Chemistry, vol. 13, no. 38, pp. 9850 - 9861, http://dx.doi.org/10.1039/c5ob01373a Mielczarek M; Thomas RV; Ma C; Kandemir H; Yang X; Bhadbhade M; Black DS; Griffith R; Lewis PJ; Kumar N, 2015, 'Synthesis and biological activity of novel mono-indole and mono-benzofuran inhibitors of bacterial transcription initiation complex formation', Bioorganic and Medicinal Chemistry, vol. 23, no. 8, pp. 1763 - 1775, http://dx.doi.org/10.1016/j.bmc.2015.02.037 Biswas NN; Kutty SK; Barraud N; Iskander GM; Griffith R; Rice SA; Willcox M; Black DS; Kumar N, 2015, 'Indole-based novel small molecules for the modulation of bacterial signalling pathways', Organic and Biomolecular Chemistry, vol. 13, no. 3, pp. 925 - 937, http://dx.doi.org/10.1039/c4ob02096k Zhou L; Griffith R; Gaeta B, 2014, 'Combining spatial and chemical information for clustering pharmacophores', BMC Bioinformatics, vol. 15, no. 16, http://dx.doi.org/10.1186/1471-2105-15-S16-S5 Mashkani B; Griffith R; Ashman L, 2014, 'Differences in growth promotion, drug response and intracellular protein trafficking of flt3 mutants', Iranian Journal of Basic Medical Sciences, vol. 17, no. 11, pp. 867 - 873 Drwal MN; Marinello J; Manzo SG; Wakelin LPG; Capranico G; Griffith R, 2014, 'Novel DNA topoisomerase iia inhibitors from combined ligand- and structure- based virtual screening', PLoS One, vol. 9, no. 12, http://dx.doi.org/10.1371/journal.pone.0114904 Chen J; Campbell AP; Urmi KF; Wakelin LPG; Denny WA; Griffith R; Finch AM, 2014, 'Human α1-adrenoceptor subtype selectivity of substituted homobivalent 4-aminoquinolines', Bioorganic and Medicinal Chemistry, vol. 22, no. 21, pp. 5910 - 5916, http://dx.doi.org/10.1016/j.bmc.2014.09.017 Hu X-G; Hunter L; Thomas DS; Griffith R, 2014, 'Stereoselective fluorination alters the geometry of a cyclic peptide: Exploration of backbone-fluorinated analogues of unguisin A', Angewandte Chemie International Edition, http://dx.doi.org/10.1002/anie.201403071 Campbell AP; MacDougall IJA; Griffith R; Finch AM, 2014, 'An aspartate in the second extracellular loop of the α1B adrenoceptor regulates agonist binding', European Journal of Pharmacology, vol. 733, no. 1, pp. 90 - 96, http://dx.doi.org/10.1016/j.ejphar.2014.03.034 Mielczarek M; Devakaram RV; Ma C; Yang X; Kandemir H; Purwono B; Black DS; Griffith R; Lewis PJ; Kumar N, 2014, 'Synthesis and biological activity of novel bis-indole inhibitors of bacterial transcription initiation complex formation', Organic and Biomolecular Chemistry, vol. 12, no. 18, pp. 2882 - 2894, http://dx.doi.org/10.1039/c4ob00460d Kandemir H; Kutty SK; Black DS; Kumar N; Ma C; Lewis PJ; Griffith R, 2014, 'Synthesis and biological evaluation of 2,5-di(7-indolyl)-1,3,4-oxadiazoles, and 2- and 7-indolyl 2-(1,3,4-thiadiazolyl)ketones as antimicrobials', Bioorganic and Medicinal Chemistry, http://dx.doi.org/10.1016/j.bmc.2014.01.025 Griffith R; Ngo T; Finch AM, 2013, 'Structure-based drug design and drug discovery for G protein-coupled receptors', Australian Biochemist, vol. 44, no. 2, pp. 4 - 6 Mashkani B; Odell AF; Byrnes EM; Griffith R; Ashman LK, 2013, 'Expression of biologically active human colony stimulating factor-1 in Pichia pastoris', Protein Expression and Purification, vol. 88, no. 1, pp. 93 - 97, http://dx.doi.org/10.1016/j.pep.2012.11.017 Drwal MN; Griffith R; Agama K; Pommier Y, 2013, 'Development of purely structure-based pharmacophores for the topoisomerase I-DNA-ligand binding pocket', Journal of Computer-Aided Molecular Design, pp. 1 - 13, http://dx.doi.org/10.1007/s10822-013-9695-x Ngo T; Nicholas TJ; Chen J; Finch AM; Griffith R, 2013, '5-HT1A receptor pharmacophores to screen for off-target activity of α1-adrenoceptor antagonists', Journal of Computer-Aided Molecular Design, vol. 27, no. 4, pp. 305 - 319, http://dx.doi.org/10.1007/s10822-013-9647-5 Chen J; Murad AK; Wakelin LPG; Denny WA; Griffith R; Finch AM, 2013, 'α1-Adrenoceptor and serotonin 5-HT1A receptor affinity of homobivalent 4-aminoquinoline compounds: An investigation of the effect of linker length', Biochemical Pharmacology, vol. 85, no. 10, pp. 1534 - 1541, http://dx.doi.org/10.1016/j.bcp.2013.03.010