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272 results

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Page 1
The discovery of PLK4 inhibitors: (E)-3-((1H-Indazol-6-yl)methylene)indolin-2-ones as novel antiproliferative agents.
Laufer R, Forrest B, Li SW, Liu Y, Sampson P, Edwards L, Lang Y, Awrey DE, Mao G, Plotnikova O, Leung G, Hodgson R, Beletskaya I, Mason JM, Luo X, Wei X, Yao Y, Feher M, Ban F, Kiarash R, Green E, Mak TW, Pan G, Pauls HW. Laufer R, et al. Among authors: feher m. J Med Chem. 2013 Aug 8;56(15):6069-87. doi: 10.1021/jm400380m. Epub 2013 Jul 26. J Med Chem. 2013. PMID: 23829549
The discovery of Polo-like kinase 4 inhibitors: design and optimization of spiro[cyclopropane-1,3'[3H]indol]-2'(1'H).ones as orally bioavailable antitumor agents.
Sampson PB, Liu Y, Patel NK, Feher M, Forrest B, Li SW, Edwards L, Laufer R, Lang Y, Ban F, Awrey DE, Mao G, Plotnikova O, Leung G, Hodgson R, Mason JM, Wei X, Kiarash R, Green E, Qiu W, Chirgadze NY, Mak TW, Pan G, Pauls HW. Sampson PB, et al. Among authors: feher m. J Med Chem. 2015 Jan 8;58(1):130-46. doi: 10.1021/jm5005336. Epub 2014 Jun 24. J Med Chem. 2015. PMID: 24867403
Discovery of inhibitors of the mitotic kinase TTK based on N-(3-(3-sulfamoylphenyl)-1H-indazol-5-yl)-acetamides and carboxamides.
Laufer R, Ng G, Liu Y, Patel NK, Edwards LG, Lang Y, Li SW, Feher M, Awrey DE, Leung G, Beletskaya I, Plotnikova O, Mason JM, Hodgson R, Wei X, Mao G, Luo X, Huang P, Green E, Kiarash R, Lin DC, Harris-Brandts M, Ban F, Nadeem V, Mak TW, Pan GJ, Qiu W, Chirgadze NY, Pauls HW. Laufer R, et al. Among authors: feher m. Bioorg Med Chem. 2014 Sep 1;22(17):4968-97. doi: 10.1016/j.bmc.2014.06.027. Epub 2014 Jun 23. Bioorg Med Chem. 2014. PMID: 25043312
The discovery of Polo-like kinase 4 inhibitors: identification of (1R,2S).2-(3-((E).4-(((cis).2,6-dimethylmorpholino)methyl)styryl). 1H.indazol-6-yl)-5'-methoxyspiro[cyclopropane-1,3'-indolin]-2'-one (CFI-400945) as a potent, orally active antitumor agent.
Sampson PB, Liu Y, Forrest B, Cumming G, Li SW, Patel NK, Edwards L, Laufer R, Feher M, Ban F, Awrey DE, Mao G, Plotnikova O, Hodgson R, Beletskaya I, Mason JM, Luo X, Nadeem V, Wei X, Kiarash R, Madeira B, Huang P, Mak TW, Pan G, Pauls HW. Sampson PB, et al. Among authors: feher m. J Med Chem. 2015 Jan 8;58(1):147-69. J Med Chem. 2015. PMID: 25723005
The Discovery of Orally Bioavailable Tyrosine Threonine Kinase (TTK) Inhibitors: 3-(4-(heterocyclyl)phenyl)-1H-indazole-5-carboxamides as Anticancer Agents.
Liu Y, Lang Y, Patel NK, Ng G, Laufer R, Li SW, Edwards L, Forrest B, Sampson PB, Feher M, Ban F, Awrey DE, Beletskaya I, Mao G, Hodgson R, Plotnikova O, Qiu W, Chirgadze NY, Mason JM, Wei X, Lin DC, Che Y, Kiarash R, Madeira B, Fletcher GC, Mak TW, Bray MR, Pauls HW. Liu Y, et al. Among authors: feher m. J Med Chem. 2015 Apr 23;58(8):3366-92. doi: 10.1021/jm501740a. Epub 2015 Apr 3. J Med Chem. 2015. PMID: 25763473
Discovery of 4-(4-aminopyrazolo[1,5-a][1,3,5]triazin-8-yl)benzamides as novel, highly potent and selective, orally bioavailable inhibitors of Tyrosine Threonine Kinase, TTK.
Laufer R, Li SW, Liu Y, Ng G, Lang Y, Feher M, Brokx R, Beletskaya I, Hodgson R, Mao G, Plotnikova O, Awrey DE, Mason JM, Wei X, Lin DC, Che Y, Kiarash R, Madeira B, Fletcher GC, Mak TW, Bray MR, Pauls HW. Laufer R, et al. Among authors: feher m. Bioorg Med Chem Lett. 2016 Aug 1;26(15):3562-6. doi: 10.1016/j.bmcl.2016.06.021. Epub 2016 Jun 9. Bioorg Med Chem Lett. 2016. PMID: 27335255
Discovery of Pyrazolo[1,5-a]pyrimidine TTK Inhibitors: CFI-402257 is a Potent, Selective, Bioavailable Anticancer Agent.
Liu Y, Laufer R, Patel NK, Ng G, Sampson PB, Li SW, Lang Y, Feher M, Brokx R, Beletskaya I, Hodgson R, Plotnikova O, Awrey DE, Qiu W, Chirgadze NY, Mason JM, Wei X, Lin DC, Che Y, Kiarash R, Fletcher GC, Mak TW, Bray MR, Pauls HW. Liu Y, et al. Among authors: feher m. ACS Med Chem Lett. 2016 May 6;7(7):671-5. doi: 10.1021/acsmedchemlett.5b00485. eCollection 2016 Jul 14. ACS Med Chem Lett. 2016. PMID: 27437075 Free PMC article.
Design and optimization of (3-aryl-1H-indazol-6-yl)spiro[cyclopropane-1,3'-indolin]-2'-ones as potent PLK4 inhibitors with oral antitumor efficacy.
Li SW, Liu Y, Sampson PB, Patel NK, Forrest BT, Edwards L, Laufer R, Feher M, Ban F, Awrey DE, Hodgson R, Beletskaya I, Mao G, Mason JM, Wei X, Luo X, Kiarash R, Green E, Mak TW, Pan G, Pauls HW. Li SW, et al. Among authors: feher m. Bioorg Med Chem Lett. 2016 Oct 1;26(19):4625-4630. doi: 10.1016/j.bmcl.2016.08.063. Epub 2016 Aug 23. Bioorg Med Chem Lett. 2016. PMID: 27592744
272 results