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Items: 10

1.

MLN8054 and Alisertib (MLN8237): Discovery of Selective Oral Aurora A Inhibitors.

Sells TB, Chau R, Ecsedy JA, Gershman RE, Hoar K, Huck J, Janowick DA, Kadambi VJ, LeRoy PJ, Stirling M, Stroud SG, Vos TJ, Weatherhead GS, Wysong DR, Zhang M, Balani SK, Bolen JB, Manfredi MG, Claiborne CF.

ACS Med Chem Lett. 2015 Apr 22;6(6):630-4. doi: 10.1021/ml500409n. eCollection 2015 Jun 11.

2.

MLN0905, a small-molecule plk1 inhibitor, induces antitumor responses in human models of diffuse large B-cell lymphoma.

Shi JQ, Lasky K, Shinde V, Stringer B, Qian MG, Liao D, Liu R, Driscoll D, Nestor MT, Amidon BS, Rao Y, Duffey MO, Manfredi MG, Vos TJ, D' Amore N, Hyer ML.

Mol Cancer Ther. 2012 Sep;11(9):2045-53. doi: 10.1158/1535-7163.MCT-11-1036. Epub 2012 May 18.

3.

Discovery of a potent and orally bioavailable benzolactam-derived inhibitor of Polo-like kinase 1 (MLN0905).

Duffey MO, Vos TJ, Adams R, Alley J, Anthony J, Barrett C, Bharathan I, Bowman D, Bump NJ, Chau R, Cullis C, Driscoll DL, Elder A, Forsyth N, Frazer J, Guo J, Guo L, Hyer ML, Janowick D, Kulkarni B, Lai SJ, Lasky K, Li G, Li J, Liao D, Little J, Peng B, Qian MG, Reynolds DJ, Rezaei M, Scott MP, Sells TB, Shinde V, Shi QJ, Sintchak MD, Soucy F, Sprott KT, Stroud SG, Nestor M, Visiers I, Weatherhead G, Ye Y, D'Amore N.

J Med Chem. 2012 Jan 12;55(1):197-208. doi: 10.1021/jm2011172. Epub 2011 Dec 5.

PMID:
22070629
4.

Design and optimization of potent and orally bioavailable tetrahydronaphthalene Raf inhibitors.

Gould AE, Adams R, Adhikari S, Aertgeerts K, Afroze R, Blackburn C, Calderwood EF, Chau R, Chouitar J, Duffey MO, England DB, Farrer C, Forsyth N, Garcia K, Gaulin J, Greenspan PD, Guo R, Harrison SJ, Huang SC, Iartchouk N, Janowick D, Kim MS, Kulkarni B, Langston SP, Liu JX, Ma LT, Menon S, Mizutani H, Paske E, Renou CC, Rezaei M, Rowland RS, Sintchak MD, Smith MD, Stroud SG, Tregay M, Tian Y, Veiby OP, Vos TJ, Vyskocil S, Williams J, Xu T, Yang JJ, Yano J, Zeng H, Zhang DM, Zhang Q, Galvin KM.

J Med Chem. 2011 Mar 24;54(6):1836-46. doi: 10.1021/jm101479y. Epub 2011 Feb 22.

PMID:
21341678
5.

Discovery and optimization of pyrazoline compounds as B-Raf inhibitors.

Duffey MO, Adams R, Blackburn C, Chau RW, Chen S, Galvin KM, Garcia K, Gould AE, Greenspan PD, Harrison S, Huang SC, Kim MS, Kulkarni B, Langston S, Liu JX, Ma LT, Menon S, Nagayoshi M, Rowland RS, Vos TJ, Xu T, Yang JJ, Yu S, Zhang Q.

Bioorg Med Chem Lett. 2010 Aug 15;20(16):4800-4. doi: 10.1016/j.bmcl.2010.06.113. Epub 2010 Jun 25.

PMID:
20634068
6.

Discovery and optimization of N-acyl and N-aroylpyrazolines as B-Raf kinase inhibitors.

Blackburn C, Duffey MO, Gould AE, Kulkarni B, Liu JX, Menon S, Nagayoshi M, Vos TJ, Williams J.

Bioorg Med Chem Lett. 2010 Aug 15;20(16):4795-9. doi: 10.1016/j.bmcl.2010.06.110. Epub 2010 Jun 25.

PMID:
20630752
7.

Antitumor activity of MLN8054, an orally active small-molecule inhibitor of Aurora A kinase.

Manfredi MG, Ecsedy JA, Meetze KA, Balani SK, Burenkova O, Chen W, Galvin KM, Hoar KM, Huck JJ, LeRoy PJ, Ray ET, Sells TB, Stringer B, Stroud SG, Vos TJ, Weatherhead GS, Wysong DR, Zhang M, Bolen JB, Claiborne CF.

Proc Natl Acad Sci U S A. 2007 Mar 6;104(10):4106-11. Epub 2007 Feb 23.

8.

Identification and structure-activity relationships of a new series of Melanocortin-4 receptor antagonists.

Vos TJ, Balani S, Blackburn C, Chau RW, Danca MD, Drabic SV, Farrer CA, Patane MA, Stroud SG, Yowe DL, Claiborne CF.

Bioorg Med Chem Lett. 2006 Apr 15;16(8):2302-5. Epub 2006 Feb 3.

PMID:
16458508
9.

Identification of 2-[2-[2-(5-bromo-2- methoxyphenyl)-ethyl]-3-fluorophenyl]-4,5-dihydro-1H-imidazole (ML00253764), a small molecule melanocortin 4 receptor antagonist that effectively reduces tumor-induced weight loss in a mouse model.

Vos TJ, Caracoti A, Che JL, Dai M, Farrer CA, Forsyth NE, Drabic SV, Horlick RA, Lamppu D, Yowe DL, Balani S, Li P, Zeng H, Joseph IB, Rodriguez LE, Maguire MP, Patane MA, Claiborne CF.

J Med Chem. 2004 Mar 25;47(7):1602-4.

PMID:
15027849
10.

An enyne metathesis/(4 + 2)-dimerization route to (+/-)-differolide.

Hoye TR, Donaldson SM, Vos TJ.

Org Lett. 1999 Jul 29;1(2):277-9.

PMID:
10822563

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