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4-methylpteridinones as orally active and selective PI3K/mTOR dual inhibitors.
Liu KK, Bagrodia S, Bailey S, Cheng H, Chen H, Gao L, Greasley S, Hoffman JE, Hu Q, Johnson TO, Knighton D, Liu Z, Marx MA, Nambu MD, Ninkovic S, Pascual B, Rafidi K, Rodgers CM, Smith GL, Sun S, Wang H, Yang A, Yuan J, Zou A. Liu KK, et al. Among authors: yuan j. Bioorg Med Chem Lett. 2010 Oct 15;20(20):6096-9. doi: 10.1016/j.bmcl.2010.08.045. Epub 2010 Aug 14. Bioorg Med Chem Lett. 2010. PMID: 20817449
Antitumor Efficacy of the Dual PI3K/mTOR Inhibitor PF-04691502 in a Human Xenograft Tumor Model Derived from Colorectal Cancer Stem Cells Harboring a PIK3CA Mutation.
Fang DD, Zhang CC, Gu Y, Jani JP, Cao J, Tsaparikos K, Yuan J, Thiel M, Jackson-Fisher A, Zong Q, Lappin PB, Hayashi T, Schwab RB, Wong A, John-Baptiste A, Bagrodia S, Los G, Bender S, Christensen J, Vanarsdale T. Fang DD, et al. Among authors: yuan j. PLoS One. 2013 Jun 27;8(6):e67258. doi: 10.1371/journal.pone.0067258. Print 2013. PLoS One. 2013. PMID: 23826249 Free PMC article.
Design and Discovery of N-(3-(2-(2-Hydroxyethoxy)-6-morpholinopyridin-4-yl)-4-methylphenyl)-2-(trifluoromethyl)isonicotinamide, a Selective, Efficacious, and Well-Tolerated RAF Inhibitor Targeting RAS Mutant Cancers: The Path to the Clinic.
Ramurthy S, Taft BR, Aversa RJ, Barsanti PA, Burger MT, Lou Y, Nishiguchi GA, Rico A, Setti L, Smith A, Subramanian S, Tamez V, Tanner H, Wan L, Hu C, Appleton BA, Mamo M, Tandeske L, Tellew JE, Huang S, Yue Q, Chaudhary A, Tian H, Iyer R, Hassan AQ, Mathews Griner LA, La Bonte LR, Cooke VG, Van Abbema A, Merritt H, Gampa K, Feng F, Yuan J, Mishina Y, Wang Y, Haling JR, Vaziri S, Hekmat-Nejad M, Polyakov V, Zang R, Sethuraman V, Amiri P, Singh M, Sellers WR, Lees E, Shao W, Dillon MP, Stuart DD. Ramurthy S, et al. Among authors: yuan j. J Med Chem. 2020 Mar 12;63(5):2013-2027. doi: 10.1021/acs.jmedchem.9b00161. Epub 2019 May 16. J Med Chem. 2020. PMID: 31059256
1-amino-4-benzylphthalazines as orally bioavailable smoothened antagonists with antitumor activity.
Miller-Moslin K, Peukert S, Jain RK, McEwan MA, Karki R, Llamas L, Yusuff N, He F, Li Y, Sun Y, Dai M, Perez L, Michael W, Sheng T, Lei H, Zhang R, Williams J, Bourret A, Ramamurthy A, Yuan J, Guo R, Matsumoto M, Vattay A, Maniara W, Amaral A, Dorsch M, Kelleher JF 3rd. Miller-Moslin K, et al. Among authors: yuan j. J Med Chem. 2009 Jul 9;52(13):3954-68. doi: 10.1021/jm900309j. J Med Chem. 2009. PMID: 19469545
Design and Discovery of N-(2-Methyl-5'-morpholino-6'-((tetrahydro-2H-pyran-4-yl)oxy)-[3,3'-bipyridin]-5-yl)-3-(trifluoromethyl)benzamide (RAF709): A Potent, Selective, and Efficacious RAF Inhibitor Targeting RAS Mutant Cancers.
Nishiguchi GA, Rico A, Tanner H, Aversa RJ, Taft BR, Subramanian S, Setti L, Burger MT, Wan L, Tamez V, Smith A, Lou Y, Barsanti PA, Appleton BA, Mamo M, Tandeske L, Dix I, Tellew JE, Huang S, Mathews Griner LA, Cooke VG, Van Abbema A, Merritt H, Ma S, Gampa K, Feng F, Yuan J, Wang Y, Haling JR, Vaziri S, Hekmat-Nejad M, Jansen JM, Polyakov V, Zang R, Sethuraman V, Amiri P, Singh M, Lees E, Shao W, Stuart DD, Dillon MP, Ramurthy S. Nishiguchi GA, et al. Among authors: yuan j. J Med Chem. 2017 Jun 22;60(12):4869-4881. doi: 10.1021/acs.jmedchem.6b01862. Epub 2017 Jun 8. J Med Chem. 2017. PMID: 28557458
Design and optimization of renin inhibitors: Orally bioavailable alkyl amines.
Tice CM, Xu Z, Yuan J, Simpson RD, Cacatian ST, Flaherty PT, Zhao W, Guo J, Ishchenko A, Singh SB, Wu Z, Scott BB, Bukhtiyarov Y, Berbaum J, Mason J, Panemangalore R, Cappiello MG, Müller D, Harrison RK, McGeehan GM, Dillard LW, Baldwin JJ, Claremon DA. Tice CM, et al. Among authors: yuan j. Bioorg Med Chem Lett. 2009 Jul 1;19(13):3541-5. doi: 10.1016/j.bmcl.2009.04.140. Epub 2009 May 5. Bioorg Med Chem Lett. 2009. PMID: 19457666
Optimization of orally bioavailable alkyl amine renin inhibitors.
Xu Z, Cacatian S, Yuan J, Simpson RD, Jia L, Zhao W, Tice CM, Flaherty PT, Guo J, Ishchenko A, Singh SB, Wu Z, McKeever BM, Scott BB, Bukhtiyarov Y, Berbaum J, Mason J, Panemangalore R, Cappiello MG, Bentley R, Doe CP, Harrison RK, McGeehan GM, Dillard LW, Baldwin JJ, Claremon DA. Xu Z, et al. Among authors: yuan j. Bioorg Med Chem Lett. 2010 Jan 15;20(2):694-9. doi: 10.1016/j.bmcl.2009.11.066. Epub 2009 Dec 1. Bioorg Med Chem Lett. 2010. PMID: 19959358
Biphenyl/diphenyl ether renin inhibitors: filling the S1 pocket of renin via the S3 pocket.
Yuan J, Simpson RD, Zhao W, Tice CM, Xu Z, Cacatian S, Jia L, Flaherty PT, Guo J, Ishchenko A, Wu Z, McKeever BM, Scott BB, Bukhtiyarov Y, Berbaum J, Panemangalore R, Bentley R, Doe CP, Harrison RK, McGeehan GM, Singh SB, Dillard LW, Baldwin JJ, Claremon DA. Yuan J, et al. Bioorg Med Chem Lett. 2011 Aug 15;21(16):4836-43. doi: 10.1016/j.bmcl.2011.06.043. Epub 2011 Jun 17. Bioorg Med Chem Lett. 2011. PMID: 21741239
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