Discovery of Mcl-1-specific inhibitor AZD5991 and preclinical activity in multiple myeloma and acute myeloid leukemia AE Tron, MA Belmonte, A Adam, BM Aquila, LH Boise, E Chiarparin, ... Nature communications 9 (1), 5341, 2018 | 451 | 2018 |
The identification of potent and selective imidazole-based inhibitors of B-Raf kinase AK Takle, MJB Brown, S Davies, DK Dean, G Francis, A Gaiba, AW Hird, ... Bioorganic & medicinal chemistry letters 16 (2), 378-381, 2006 | 256 | 2006 |
A practical method for enantioselective synthesis of all-carbon quaternary stereogenic centers through NHC-Cu-catalyzed conjugate additions of alkyl-and arylzinc reagents to β … K Lee, MK Brown, AW Hird, AH Hoveyda Journal of the American Chemical Society 128 (22), 7182-7184, 2006 | 254 | 2006 |
Inhibition of Mcl-1 through covalent modification of a noncatalytic lysine side chain G Akçay, MA Belmonte, B Aquila, C Chuaqui, AW Hird, ML Lamb, ... Nature chemical biology 12 (11), 931-936, 2016 | 192 | 2016 |
Catalytic enantioselective alkylations of tetrasubstituted olefins. Synthesis of all-carbon quaternary stereogenic centers through Cu-catalyzed asymmetric conjugate additions … AW Hird, AH Hoveyda Journal of the American Chemical Society 127 (43), 14988-14989, 2005 | 160 | 2005 |
Cu‐Catalyzed Enantioselective Conjugate Additions of Alkyl Zinc Reagents to Unsaturated N‐Acyloxazolidinones Promoted by a Chiral Triamide Phosphane AW Hird, AH Hoveyda Angewandte Chemie International Edition 42 (11), 1276-1279, 2003 | 147 | 2003 |
Recent advances in the development of Mcl-1 inhibitors for cancer therapy AW Hird, AE Tron Pharmacology & therapeutics 198, 59-67, 2019 | 138 | 2019 |
Discovery of novel benzylidene-1, 3-thiazolidine-2, 4-diones as potent and selective inhibitors of the PIM-1, PIM-2, and PIM-3 protein kinases LA Dakin, MH Block, H Chen, E Code, JE Dowling, X Feng, AD Ferguson, ... Bioorganic & medicinal chemistry letters 22 (14), 4599-4604, 2012 | 113 | 2012 |
Discovery of a novel class of dimeric Smac mimetics as potent IAP antagonists resulting in a clinical candidate for the treatment of cancer (AZD5582) EJ Hennessy, A Adam, BM Aquila, LM Castriotta, D Cook, M Hattersley, ... Journal of medicinal chemistry 56 (24), 9897-9919, 2013 | 101 | 2013 |
Structure based design of non-natural peptidic macrocyclic Mcl-1 inhibitors JW Johannes, S Bates, C Beigie, MA Belmonte, J Breen, S Cao, ... ACS medicinal chemistry letters 8 (2), 239-244, 2017 | 73 | 2017 |
Discovery of AZD4573, a potent and selective inhibitor of CDK9 that enables short duration of target engagement for the treatment of hematological malignancies B Barlaam, R Casella, J Cidado, C Cook, C De Savi, A Dishington, ... Journal of Medicinal Chemistry 63 (24), 15564-15590, 2020 | 71 | 2020 |
Structure and property based design of pyrazolo [1, 5-a] pyrimidine inhibitors of CK2 kinase with activity in vivo JE Dowling, M Alimzhanov, L Bao, MH Block, C Chuaqui, EL Cooke, ... ACS medicinal chemistry letters 4 (8), 800-805, 2013 | 48 | 2013 |
Small peptides as ligands for catalytic asymmetric alkylations of olefins. Rational design of catalysts or of searches that lead to them? AH Hoveyda, AW Hird, MA Kacprzynski Chemical communications, 1779-1785, 2004 | 41 | 2004 |
Free ligand 1D NMR conformational signatures to enhance structure based drug design of a Mcl-1 inhibitor (AZD5991) and other synthetic macrocycles AYS Balazs, RJ Carbajo, NL Davies, Y Dong, AW Hird, JW Johannes, ... Journal of Medicinal Chemistry 62 (21), 9418-9437, 2019 | 29 | 2019 |
Abstract DDT01-02: AZD5991: A potent and selective macrocyclic inhibitor of Mcl-1 for treatment of hematologic cancers AW Hird, JP Secrist, A Adam, MA Belmonte, E Gangl, F Gibbons, ... Cancer Research 77 (13_Supplement), DDT01-02-DDT01-02, 2017 | 29 | 2017 |
Structure-based design and synthesis of tricyclic IAP (Inhibitors of Apoptosis Proteins) inhibitors AW Hird, BM Aquila, MH Block, EJ Hennessy, VM Kamhi, CA Omer, ... Bioorganic & Medicinal Chemistry Letters 24 (7), 1820-1824, 2014 | 29 | 2014 |
Adventures in scaffold morphing: discovery of fused ring heterocyclic checkpoint kinase 1 (CHK1) inhibitors B Yang, MM Vasbinder, AW Hird, Q Su, H Wang, Y Yu, D Toader, ... Journal of Medicinal Chemistry 61 (3), 1061-1073, 2018 | 22 | 2018 |
Discovery of novel hedgehog antagonists from cell-based screening: Isosteric modification of p38 bisamides as potent inhibitors of SMO B Yang, AW Hird, DJ Russell, BP Fauber, LA Dakin, X Zheng, Q Su, ... Bioorganic & medicinal chemistry letters 22 (14), 4907-4911, 2012 | 22 | 2012 |
The structure of human GCN2 reveals a parallel, back-to-back kinase dimer with a plastic DFG activation loop motif T Maia de Oliveira, V Korboukh, S Caswell, JJ Winter Holt, M Lamb, ... Biochemical Journal 477 (1), 275-284, 2020 | 21 | 2020 |
Small molecule inhibitor of apoptosis proteins antagonists: a patent review AW Hird, BM Aquila, EJ Hennessy, MM Vasbinder, B Yang Expert Opinion on Therapeutic Patents 25 (7), 755-774, 2015 | 20 | 2015 |