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MK-5204: An orally active β-1,3-glucan synthesis inhibitor.
Apgar JM, Wilkening RR, Parker DL Jr, Meng D, Wildonger KJ, Sperbeck D, Greenlee ML, Balkovec JM, Flattery AM, Abruzzo GK, Galgoci AM, Giacobbe RA, Gill CJ, Hsu MJ, Liberator P, Misura AS, Motyl M, Kahn JN, Powles M, Racine F, Dragovic J, Fan W, Kirwan R, Lee S, Liu H, Mamai A, Nelson K, Peel M. Apgar JM, et al. Among authors: balkovec jm. Bioorg Med Chem Lett. 2020 Sep 1;30(17):127357. doi: 10.1016/j.bmcl.2020.127357. Epub 2020 Jun 19. Bioorg Med Chem Lett. 2020. PMID: 32738971
Synthesis and biological evaluation of antifungal derivatives of enfumafungin as orally bioavailable inhibitors of β-1,3-glucan synthase.
Heasley BH, Pacofsky GJ, Mamai A, Liu H, Nelson K, Coti G, Peel MR, Balkovec JM, Greenlee ML, Liberator P, Meng D, Parker DL, Wilkening RR, Apgar JM, Racine F, Hsu MJ, Giacobbe RA, Kahn JN. Heasley BH, et al. Among authors: balkovec jm. Bioorg Med Chem Lett. 2012 Nov 15;22(22):6811-6. doi: 10.1016/j.bmcl.2012.05.031. Epub 2012 May 17. Bioorg Med Chem Lett. 2012. PMID: 22672801
Novel orally active inhibitors of β-1,3-glucan synthesis derived from enfumafungin.
Apgar JM, Wilkening RR, Greenlee ML, Balkovec JM, Flattery AM, Abruzzo GK, Galgoci AM, Giacobbe RA, Gill CJ, Hsu MJ, Liberator P, Misura AS, Motyl M, Nielsen Kahn J, Powles M, Racine F, Dragovic J, Habulihaz B, Fan W, Kirwan R, Lee S, Liu H, Mamai A, Nelson K, Peel M. Apgar JM, et al. Among authors: balkovec jm. Bioorg Med Chem Lett. 2015 Dec 15;25(24):5813-8. doi: 10.1016/j.bmcl.2015.10.011. Epub 2015 Oct 9. Bioorg Med Chem Lett. 2015. PMID: 26542966
Ibrexafungerp: An orally active β-1,3-glucan synthesis inhibitor.
Apgar JM, Wilkening RR, Parker DL Jr, Meng D, Wildonger KJ, Sperbeck D, Greenlee ML, Balkovec JM, Flattery AM, Abruzzo GK, Galgoci AM, Giacobbe RA, Gill CJ, Hsu MJ, Liberator P, Misura AS, Motyl M, Nielsen Kahn J, Powles M, Racine F, Dragovic J, Fan W, Kirwan R, Lee S, Liu H, Mamai A, Nelson K, Peel M. Apgar JM, et al. Among authors: balkovec jm. Bioorg Med Chem Lett. 2021 Jan 15;32:127661. doi: 10.1016/j.bmcl.2020.127661. Epub 2020 Nov 4. Bioorg Med Chem Lett. 2021. PMID: 33160023
Discovery of 4-heteroarylbicyclo[2.2.2]octyltriazoles as potent and selective inhibitors of 11beta-HSD1: novel therapeutic agents for the treatment of metabolic syndrome.
Gu X, Dragovic J, Koo GC, Koprak SL, LeGrand C, Mundt SS, Shah K, Springer MS, Tan EY, Thieringer R, Hermanowski-Vosatka A, Zokian HJ, Balkovec JM, Waddell ST. Gu X, et al. Among authors: balkovec jm. Bioorg Med Chem Lett. 2005 Dec 1;15(23):5266-9. doi: 10.1016/j.bmcl.2005.08.052. Epub 2005 Sep 26. Bioorg Med Chem Lett. 2005. PMID: 16185866
Benzimidazole-based DGAT1 inhibitors with a [3.1.0] bicyclohexane carboxylic acid moiety.
He S, Lai Z, Hong Q, Shang J, Reibarkh M, Kuethe JT, Liu J, Guiadeen D, Krikorian AD, Cernak TA, Dykstra KD, Sperbeck DM, Wu Z, Yu Y, Yang GX, Jian T, Verras A, Sonatore LM, Wiltsie J, Chung CC, Murphy BA, Gorski JN, Liu J, Xiao J, Wolff M, Tong SX, Madeira M, Karanam BV, Shen DM, Balkovec JM, Pinto S, Nargund RP, DeVita RJ. He S, et al. Among authors: balkovec jm. Bioorg Med Chem Lett. 2019 May 15;29(10):1182-1186. doi: 10.1016/j.bmcl.2019.03.025. Epub 2019 Mar 21. Bioorg Med Chem Lett. 2019. PMID: 30926247
Accelerating the discovery of DGAT1 inhibitors through the application of parallel medicinal chemistry (PMC).
Yu Y, Wu Z, Shi ZC, He S, Lai Z, Cernak TA, Vachal P, Liu M, Liu J, Hong Q, Jian T, Guiadeen D, Krikorian A, Sperbeck DM, Verras A, Sonatore LM, Murphy BA, Wiltsie J, Chung CC, Gorski JN, Liu J, Xiao J, Wolff M, Tong SX, Madeira M, Karanam BV, Shen DM, Balkovec JM, De Vita RJ, Pinto S, Nargund RP. Yu Y, et al. Among authors: balkovec jm. Bioorg Med Chem Lett. 2019 Jun 1;29(11):1380-1385. doi: 10.1016/j.bmcl.2019.03.039. Epub 2019 Mar 27. Bioorg Med Chem Lett. 2019. PMID: 30952592
49 results