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Discovery and Preclinical Profiling of GSK3839919, a Potent HIV-1 Allosteric Integrase Inhibitor.
Parcella K, Wang T, Eastman K, Zhang Z, Yin Z, Patel M, Tu Y, Zheng BZ, Walker MA, Saulnier MG, Frennesson D, Bowsher M, Gillis E, Peese K, Belema M, Cianci C, Dicker IB, McAuliffe B, Ding B, Falk P, Simmermacher J, Parker DD, Sivaprakasam P, Kish K, Lewis H, Hanumegowda U, Jenkins S, Kadow JF, Krystal M, Meanwell NA, Naidu BN. Parcella K, et al. Among authors: eastman k. ACS Med Chem Lett. 2022 May 9;13(6):972-980. doi: 10.1021/acsmedchemlett.2c00115. eCollection 2022 Jun 9. ACS Med Chem Lett. 2022. PMID: 35707159 Free PMC article.
Improving Metabolic Stability with Deuterium: The Discovery of BMT-052, a Pan-genotypic HCV NS5B Polymerase Inhibitor.
Parcella K, Eastman K, Yeung KS, Grant-Young KA, Zhu J, Wang T, Zhang Z, Yin Z, Parker D, Mosure K, Fang H, Wang YK, Lemm J, Zhuo X, Hanumegowda U, Liu M, Rigat K, Donoso M, Tuttle M, Zvyaga T, Haarhoff Z, Meanwell NA, Soars MG, Roberts SB, Kadow JF. Parcella K, et al. Among authors: eastman k. ACS Med Chem Lett. 2017 Jun 29;8(7):771-774. doi: 10.1021/acsmedchemlett.7b00211. eCollection 2017 Jul 13. ACS Med Chem Lett. 2017. PMID: 28740615 Free PMC article.
Scaffold modifications to the 4-(4,4-dimethylpiperidinyl) 2,6-dimethylpyridinyl class of HIV-1 allosteric integrase inhibitors.
Parcella K, Patel M, Tu Y, Eastman K, Peese K, Gillis E, Belema M, Dicker IB, McAuliffe B, Ding B, Falk P, Simmermacher J, Parker DD, Sivaprakasam P, Khan JA, Kish K, Lewis H, Hanumegowda U, Jenkins S, Kadow JF, Krystal M, Meanwell NA, Naidu BN. Parcella K, et al. Among authors: eastman k. Bioorg Med Chem. 2022 Aug 1;67:116833. doi: 10.1016/j.bmc.2022.116833. Epub 2022 May 19. Bioorg Med Chem. 2022. PMID: 35605346
Identification of a novel series of potent HCV NS5B Site I inhibitors.
Eastman KJ, Yang Z, Bender JA, Mosure K, Lemm JA, Meanwell NA, Roberts SB, Knipe J, Kadow JF. Eastman KJ, et al. Bioorg Med Chem Lett. 2014 Apr 15;24(8):1993-7. doi: 10.1016/j.bmcl.2014.02.047. Epub 2014 Feb 28. Bioorg Med Chem Lett. 2014. PMID: 24656612
Applications of Fluorine in Medicinal Chemistry.
Gillis EP, Eastman KJ, Hill MD, Donnelly DJ, Meanwell NA. Gillis EP, et al. J Med Chem. 2015 Nov 12;58(21):8315-59. doi: 10.1021/acs.jmedchem.5b00258. Epub 2015 Jul 22. J Med Chem. 2015. PMID: 26200936 Review.
The discovery of a pan-genotypic, primer grip inhibitor of HCV NS5B polymerase.
Eastman KJ, Parcella K, Yeung KS, Grant-Young KA, Zhu J, Wang T, Zhang Z, Yin Z, Beno BR, Sheriff S, Kish K, Tredup J, Jardel AG, Halan V, Ghosh K, Parker D, Mosure K, Fang H, Wang YK, Lemm J, Zhuo X, Hanumegowda U, Rigat K, Donoso M, Tuttle M, Zvyaga T, Haarhoff Z, Meanwell NA, Soars MG, Roberts SB, Kadow JF. Eastman KJ, et al. Medchemcomm. 2017 Feb 8;8(4):796-806. doi: 10.1039/c6md00636a. eCollection 2017 Apr 1. Medchemcomm. 2017. PMID: 30108798 Free PMC article.
Regulated induced proximity targeting chimeras-RIPTACs-A heterobifunctional small molecule strategy for cancer selective therapies.
Raina K, Forbes CD, Stronk R, Rappi JP Jr, Eastman KJ, Zaware N, Yu X, Li H, Bhardwaj A, Gerritz SW, Forgione M, Hundt A, King MP, Posner ZM, Correia AD, McGovern A, Puleo DE, Chenard R, Mousseau JJ, Vergara JI, Garvin E, Macaluso J, Martin M, Bassoli K, Jones K, Garcia M, Howard K, Yaggi M, Smith LM, Chen JM, Mayfield AB, De Leon CA, Hines J, Kayser-Bricker KJ, Crews CM. Raina K, et al. Among authors: eastman kj. Cell Chem Biol. 2024 Aug 15;31(8):1490-1502.e42. doi: 10.1016/j.chembiol.2024.07.005. Epub 2024 Aug 7. Cell Chem Biol. 2024. PMID: 39116881
62 results