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Discovery of 1H-Pyrazole Biaryl Sulfonamides as Novel G2019S-LRRK2 Kinase Inhibitors.
Leśniak RK, Nichols RJ, Schonemann M, Zhao J, Gajera CR, Lam G, Nguyen KC, Langston JW, Smith M, Montine TJ. Leśniak RK, et al. Among authors: nguyen kc. ACS Med Chem Lett. 2022 May 23;13(6):981-988. doi: 10.1021/acsmedchemlett.2c00116. eCollection 2022 Jun 9. ACS Med Chem Lett. 2022. PMID: 35707141 Free PMC article.
PI4KIIIβ is a therapeutic target in chromosome 1q-amplified lung adenocarcinoma.
Tan X, Banerjee P, Pham EA, Rutaganira FUN, Basu K, Bota-Rabassedas N, Guo HF, Grzeskowiak CL, Liu X, Yu J, Shi L, Peng DH, Rodriguez BL, Zhang J, Zheng V, Duose DY, Solis LM, Mino B, Raso MG, Behrens C, Wistuba II, Scott KL, Smith M, Nguyen K, Lam G, Choong I, Mazumdar A, Hill JL, Gibbons DL, Brown PH, Russell WK, Shokat K, Creighton CJ, Glenn JS, Kurie JM. Tan X, et al. Sci Transl Med. 2020 Jan 22;12(527):eaax3772. doi: 10.1126/scitranslmed.aax3772. Sci Transl Med. 2020. PMID: 31969487 Free PMC article.
Programmable antivirals targeting critical conserved viral RNA secondary structures from influenza A virus and SARS-CoV-2.
Hagey RJ, Elazar M, Pham EA, Tian S, Ben-Avi L, Bernardin-Souibgui C, Yee MF, Moreira FR, Rabinovitch MV, Meganck RM, Fram B, Beck A, Gibson SA, Lam G, Devera J, Kladwang W, Nguyen K, Xiong A, Schaffert S, Avisar T, Liu P, Rustagi A, Fichtenbaum CJ, Pang PS, Khatri P, Tseng CT, Taubenberger JK, Blish CA, Hurst BL, Sheahan TP, Das R, Glenn JS. Hagey RJ, et al. Nat Med. 2022 Sep;28(9):1944-1955. doi: 10.1038/s41591-022-01908-x. Epub 2022 Aug 18. Nat Med. 2022. PMID: 35982307 Free PMC article.
Design, synthesis, and biological evaluation of pyrazolopyrimidine-sulfonamides as potent multiple-mitotic kinase (MMK) inhibitors (part I).
Zhang L, Fan J, Chong JH, Cesena A, Tam BY, Gilson C, Boykin C, Wang D, Aivazian D, Marcotte D, Xiao G, Le Brazidec JY, Piao J, Lundgren K, Hong K, Vu K, Nguyen K, Gan LS, Silvian L, Ling L, Teng M, Reff M, Takeda N, Timple N, Wang Q, Morena R, Khan S, Zhao S, Li T, Lee WC, Taveras AG, Chao J. Zhang L, et al. Bioorg Med Chem Lett. 2011 Sep 15;21(18):5633-7. doi: 10.1016/j.bmcl.2011.06.129. Epub 2011 Jul 13. Bioorg Med Chem Lett. 2011. PMID: 21798738
Discovery and optimization of a series of 3-(3-phenyl-3H-imidazo[4,5-b]pyridin-2-yl)pyridin-2-amines: orally bioavailable, selective, and potent ATP-independent Akt inhibitors.
Ashwell MA, Lapierre JM, Brassard C, Bresciano K, Bull C, Cornell-Kennon S, Eathiraj S, France DS, Hall T, Hill J, Kelleher E, Khanapurkar S, Kizer D, Koerner S, Link J, Liu Y, Makhija S, Moussa M, Namdev N, Nguyen K, Nicewonger R, Palma R, Szwaya J, Tandon M, Uppalapati U, Vensel D, Volak LP, Volckova E, Westlund N, Wu H, Yang RY, Chan TC. Ashwell MA, et al. J Med Chem. 2012 Jun 14;55(11):5291-310. doi: 10.1021/jm300276x. Epub 2012 May 31. J Med Chem. 2012. PMID: 22533986
Synthesis, SAR and biological evaluation of 1,6-disubstituted-1H-pyrazolo[3,4-d]pyrimidines as dual inhibitors of Aurora kinases and CDK1.
Le Brazidec JY, Pasis A, Tam B, Boykin C, Black C, Wang D, Claassen G, Chong JH, Chao J, Fan J, Nguyen K, Silvian L, Ling L, Zhang L, Choi M, Teng M, Pathan N, Zhao S, Li T, Taveras A. Le Brazidec JY, et al. Bioorg Med Chem Lett. 2012 Mar 1;22(5):2070-4. doi: 10.1016/j.bmcl.2012.01.019. Epub 2012 Jan 18. Bioorg Med Chem Lett. 2012. PMID: 22326168
194 results