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Page 1
Identification of Novel 2,4,5-Trisubstituted Pyrimidines as Potent Dual Inhibitors of Plasmodial PfGSK3/PfPK6 with Activity against Blood Stage Parasites In Vitro.
Galal KA, Truong A, Kwarcinski F, de Silva C, Avalani K, Havener TM, Chirgwin ME, Merten E, Ong HW, Willis C, Abdelwaly A, Helal MA, Derbyshire ER, Zutshi R, Drewry DH. Galal KA, et al. Among authors: havener tm. J Med Chem. 2022 Oct 13;65(19):13172-13197. doi: 10.1021/acs.jmedchem.2c00996. Epub 2022 Sep 27. J Med Chem. 2022. PMID: 36166733 Free PMC article.
Discovery of potent Plasmodium falciparum protein kinase 6 (PfPK6) inhibitors with a type II inhibitor pharmacophore.
Ong HW, Truong A, Kwarcinski F, de Silva C, Avalani K, Havener TM, Chirgwin M, Galal KA, Willis C, Krämer A, Liu S, Knapp S, Derbyshire ER, Zutshi R, Drewry DH. Ong HW, et al. Among authors: havener tm. Eur J Med Chem. 2023 Mar 5;249:115043. doi: 10.1016/j.ejmech.2022.115043. Epub 2022 Dec 30. Eur J Med Chem. 2023. PMID: 36736152 Free PMC article.
Discovery of a Potent and Selective Naphthyridine-Based Chemical Probe for Casein Kinase 2.
Davis-Gilbert ZW, Krämer A, Dunford JE, Howell S, Senbabaoglu F, Wells CI, Bashore FM, Havener TM, Smith JL, Hossain MA, Oppermann U, Drewry DH, Axtman AD. Davis-Gilbert ZW, et al. Among authors: havener tm. ACS Med Chem Lett. 2023 Mar 14;14(4):432-441. doi: 10.1021/acsmedchemlett.2c00530. eCollection 2023 Apr 13. ACS Med Chem Lett. 2023. PMID: 37077385 Free PMC article.
More than an Amide Bioisostere: Discovery of 1,2,4-Triazole-containing Pyrazolo[1,5-a]pyrimidine Host CSNK2 Inhibitors for Combatting β-Coronavirus Replication.
Ong HW, Yang X, Smith JL, Dickmander RJ, Brown JW, Havener TM, Taft-Benz S, Howell S, Sanders MK, Capener JL, Couñago RM, Chang E, Krämer A, Moorman NJ, Heise M, Axtman AD, Drewry DH, Willson TM. Ong HW, et al. Among authors: havener tm. J Med Chem. 2024 Jul 25;67(14):12261-12313. doi: 10.1021/acs.jmedchem.4c00962. Epub 2024 Jul 3. J Med Chem. 2024. PMID: 38959455 Free PMC article.
Strategic Fluorination to Achieve a Potent, Selective, Metabolically Stable, and Orally Bioavailable Inhibitor of CSNK2.
Ong HW, Yang X, Smith JL, Taft-Benz S, Howell S, Dickmander RJ, Havener TM, Sanders MK, Brown JW, Couñago RM, Chang E, Krämer A, Moorman NJ, Heise M, Axtman AD, Drewry DH, Willson TM. Ong HW, et al. Among authors: havener tm. Molecules. 2024 Sep 2;29(17):4158. doi: 10.3390/molecules29174158. Molecules. 2024. PMID: 39275006 Free PMC article.
Multiple approaches to repurposing drugs for neuroblastoma.
Rank L, Puhl AC, Havener TM, Anderson E, Foil DH, Zorn KM, Monakhova N, Riabova O, Hickey AJ, Makarov V, Ekins S. Rank L, et al. Among authors: havener tm. Bioorg Med Chem. 2022 Nov 1;73:117043. doi: 10.1016/j.bmc.2022.117043. Epub 2022 Oct 4. Bioorg Med Chem. 2022. PMID: 36208544 Free PMC article.
32 results