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Page 1
SAR and in vivo evaluation of 4-aryl-2-aminoalkylpyrimidines as potent and selective Janus kinase 2 (JAK2) inhibitors.
Forsyth T, Kearney PC, Kim BG, Johnson HW, Aay N, Arcalas A, Brown DS, Chan V, Chen J, Du H, Epshteyn S, Galan AA, Huynh TP, Ibrahim MA, Kane B, Koltun ES, Mann G, Meyr LE, Lee MS, Lewis GL, Noguchi RT, Pack M, Ridgway BH, Shi X, Takeuchi CS, Zu P, Leahy JW, Nuss JM, Aoyama R, Engst S, Gendreau SB, Kassees R, Li J, Lin SH, Martini JF, Stout T, Tong P, Woolfrey J, Zhang W, Yu P. Forsyth T, et al. Among authors: engst s. Bioorg Med Chem Lett. 2012 Dec 15;22(24):7653-8. doi: 10.1016/j.bmcl.2012.10.007. Epub 2012 Oct 16. Bioorg Med Chem Lett. 2012. PMID: 23127890
The design, synthesis, and biological evaluation of PIM kinase inhibitors.
Tsuhako AL, Brown DS, Koltun ES, Aay N, Arcalas A, Chan V, Du H, Engst S, Franzini M, Galan A, Huang P, Johnston S, Kane B, Kim MH, Laird AD, Lin R, Mock L, Ngan I, Pack M, Stott G, Stout TJ, Yu P, Zaharia C, Zhang W, Zhou P, Nuss JM, Kearney PC, Xu W. Tsuhako AL, et al. Among authors: engst s. Bioorg Med Chem Lett. 2012 Jun 1;22(11):3732-8. doi: 10.1016/j.bmcl.2012.04.025. Epub 2012 Apr 11. Bioorg Med Chem Lett. 2012. PMID: 22542012
Discovery of XL413, a potent and selective CDC7 inhibitor.
Koltun ES, Tsuhako AL, Brown DS, Aay N, Arcalas A, Chan V, Du H, Engst S, Ferguson K, Franzini M, Galan A, Holst CR, Huang P, Kane B, Kim MH, Li J, Markby D, Mohan M, Noson K, Plonowski A, Richards SJ, Robertson S, Shaw K, Stott G, Stout TJ, Young J, Yu P, Zaharia CA, Zhang W, Zhou P, Nuss JM, Xu W, Kearney PC. Koltun ES, et al. Among authors: engst s. Bioorg Med Chem Lett. 2012 Jun 1;22(11):3727-31. doi: 10.1016/j.bmcl.2012.04.024. Epub 2012 Apr 16. Bioorg Med Chem Lett. 2012. PMID: 22560567
The design, synthesis, and biological evaluation of potent receptor tyrosine kinase inhibitors.
Kim MH, Tsuhako AL, Co EW, Aftab DT, Bentzien F, Chen J, Cheng W, Engst S, Goon L, Klein RR, Le DT, Mac M, Parks JJ, Qian F, Rodriquez M, Stout TJ, Till JH, Won KA, Wu X, Yakes FM, Yu P, Zhang W, Zhao Y, Lamb P, Nuss JM, Xu W. Kim MH, et al. Among authors: engst s. Bioorg Med Chem Lett. 2012 Aug 1;22(15):4979-85. doi: 10.1016/j.bmcl.2012.06.029. Epub 2012 Jun 16. Bioorg Med Chem Lett. 2012. PMID: 22765894
Pyrazolopyrimidines as dual Akt/p70S6K inhibitors.
Rice KD, Kim MH, Bussenius J, Anand NK, Blazey CM, Bowles OJ, Canne-Bannen L, Chan DS, Chen B, Co EW, Costanzo S, DeFina SC, Dubenko L, Engst S, Franzini M, Huang P, Jammalamadaka V, Khoury RG, Klein RR, Laird AD, Le DT, Mac MB, Matthews DJ, Markby D, Miller N, Nuss JM, Parks JJ, Tsang TH, Tsuhako AL, Wang Y, Xu W. Rice KD, et al. Among authors: engst s. Bioorg Med Chem Lett. 2012 Apr 15;22(8):2693-7. doi: 10.1016/j.bmcl.2012.03.011. Epub 2012 Mar 10. Bioorg Med Chem Lett. 2012. PMID: 22450127
Novel Carboxamide-Based Allosteric MEK Inhibitors: Discovery and Optimization Efforts toward XL518 (GDC-0973).
Rice KD, Aay N, Anand NK, Blazey CM, Bowles OJ, Bussenius J, Costanzo S, Curtis JK, Defina SC, Dubenko L, Engst S, Joshi AA, Kennedy AR, Kim AI, Koltun ES, Lougheed JC, Manalo JC, Martini JF, Nuss JM, Peto CJ, Tsang TH, Yu P, Johnston S. Rice KD, et al. Among authors: engst s. ACS Med Chem Lett. 2012 Apr 9;3(5):416-21. doi: 10.1021/ml300049d. eCollection 2012 May 10. ACS Med Chem Lett. 2012. PMID: 24900486 Free PMC article.
Design and evaluation of a series of pyrazolopyrimidines as p70S6K inhibitors.
Bussenius J, Anand NK, Blazey CM, Bowles OJ, Bannen LC, Chan DS, Chen B, Co EW, Costanzo S, DeFina SC, Dubenko L, Engst S, Franzini M, Huang P, Jammalamadaka V, Khoury RG, Kim MH, Klein RR, Laird D, Le DT, Mac MB, Matthews DJ, Markby D, Miller N, Nuss JM, Parks JJ, Tsang TH, Tsuhako AL, Wang Y, Xu W, Rice KD. Bussenius J, et al. Among authors: engst s. Bioorg Med Chem Lett. 2012 Mar 15;22(6):2283-6. doi: 10.1016/j.bmcl.2012.01.105. Epub 2012 Feb 2. Bioorg Med Chem Lett. 2012. PMID: 22342124
In vitro and in vivo activity of cabozantinib (XL184), an inhibitor of RET, MET, and VEGFR2, in a model of medullary thyroid cancer.
Bentzien F, Zuzow M, Heald N, Gibson A, Shi Y, Goon L, Yu P, Engst S, Zhang W, Huang D, Zhao L, Vysotskaia V, Chu F, Bautista R, Cancilla B, Lamb P, Joly AH, Yakes FM. Bentzien F, et al. Among authors: engst s. Thyroid. 2013 Dec;23(12):1569-77. doi: 10.1089/thy.2013.0137. Epub 2013 Sep 17. Thyroid. 2013. PMID: 23705946 Free PMC article.
Cabozantinib (XL184), a novel MET and VEGFR2 inhibitor, simultaneously suppresses metastasis, angiogenesis, and tumor growth.
Yakes FM, Chen J, Tan J, Yamaguchi K, Shi Y, Yu P, Qian F, Chu F, Bentzien F, Cancilla B, Orf J, You A, Laird AD, Engst S, Lee L, Lesch J, Chou YC, Joly AH. Yakes FM, et al. Among authors: engst s. Mol Cancer Ther. 2011 Dec;10(12):2298-308. doi: 10.1158/1535-7163.MCT-11-0264. Epub 2011 Sep 16. Mol Cancer Ther. 2011. PMID: 21926191
Inhibition of tumor cell growth, invasion, and metastasis by EXEL-2880 (XL880, GSK1363089), a novel inhibitor of HGF and VEGF receptor tyrosine kinases.
Qian F, Engst S, Yamaguchi K, Yu P, Won KA, Mock L, Lou T, Tan J, Li C, Tam D, Lougheed J, Yakes FM, Bentzien F, Xu W, Zaks T, Wooster R, Greshock J, Joly AH. Qian F, et al. Among authors: engst s. Cancer Res. 2009 Oct 15;69(20):8009-16. doi: 10.1158/0008-5472.CAN-08-4889. Epub 2009 Oct 6. Cancer Res. 2009. PMID: 19808973
24 results