Identification of 2-amino-5-(thioaryl)thiazoles as inhibitors of nerve growth factor receptor TrkA

Bioorganic and Medicinal Chemistry Letters

Volumn 18, Issue 2, 2008, Pages 634-639

  Kim, Soong Hoon ^a   Tokarski, John S ^a   Leavitt, Kenneth J ^a   Fink, Brian E ^a   Salvati, Mark E ^a   Moquin, Robert ^a   Obermeier, Mary T ^a   Trainor, George L ^a   Vite, Gregory G ^a   Stadnick, Linda K ^a   Lippy, Jonathan S ^a   You, Dan ^a   Lorenzi, Matthew V ^a   Chen, Ping ^a  

^a BRISTOL MYERS SQUIBB   (United States)

Author keywords

2 Amino 5 (thioaryl) thiazoles; Kinase inhibitor; Nerve growth factor; NGF; TrkA; Troponyosin receptor kinase A

Indexed keywords

NERVE GROWTH FACTOR RECEPTOR; PROTEIN TYROSINE KINASE A; THIAZOLE DERIVATIVE;

ARTICLE; CHEMICAL REACTION; DRUG ACTIVITY; DRUG STRUCTURE; DRUG SYNTHESIS; ENZYME INHIBITION; ENZYME INHIBITOR COMPLEX; STRUCTURE ACTIVITY RELATION;

PHOSPHORYLATION; RECEPTOR, TRKA; STRUCTURE-ACTIVITY RELATIONSHIP; THIAZOLES;

EID: 38149024842     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2007.11.076     Document Type: Article

References (18)

1. Nakagawara A. Cancer Lett. 169 (2001) 107
2. Huang E.J., and Reichardt L.F. Annu. Rev. Biochem. 72 (2003) 609
3. Schramm A., Shulte J.H., Astrahantseff K., Apostolov O., Limpt V., Sieverts H., Kuhfittig-Kulle S., Pfeiffer P., Versteeg R., and Eggert A. Cancer Lett. 228 (2005) 143
4. Florenes V.A., Malanddsmo G.M., Holm R., Reich R., Lazarovici P., and Davidson B. Am. J. Clin. Pathol. 122 (2004) 412
5. Davidson B., Reich R., Lazarovici P., Nesland J.M., Skered M., Risberg B., Trope C.G., and Florenes V.A. Clin. Cancer Res. 9 (2003) 2248
6. Zhang Y., Dang C., Ma Q., and Shimahara Y. Oncol. Reports 14 (2005) 161
7. Ruggeri B.A., Miknyoczki S.J., Singh J., and Hudkins R.L. Curr. Med. Chem. 6 (1999) 845
8. George D.J., Dionne C.A., Jani J., Angeles T., Murakata C., Lamb J., and Issacs J.T. Cancer Res. 59 (1999) 2395
9. Undevia S.D., Vogelzang N.J., Mauer A.M., Janisch L., Mani S., and Ratain M.J. Invest. New Drugs 22 (2004) 449
10. Wood E.R., Kuyper L., Petrov K.G., Hunter III R.N., Harris P.A., and Lackey K. Biorg. Med. Chem. Lett 14 (2004) 953
11. Lippa B., Morris J., Corbett M., Kwan T.A., Noe M.C., Snow S.L., Gant T.G., Mangiaracina M., Coffey H.A., Foster B., Knauth E.A., and Wessel M.D. Biorg. Med. Chem. Lett. 16 (2006) 3444
12. Das J., Liu C., Moquin R., Lin J., Furch J.A., Spergel S.H., McIntyre K.W., Shuster D.J., O'Day K.D., Penhallow B., Hung C.-H., Kanner S.B., Lin T.-A., Dodd J.H., Barrish J.C., and Wityak J. Biog. Med. Chem. Lett. 16 (2006) 2411
13. Das J., Furch J.A., Liu C., Moquin R., Lin J., Spergel S.H., McIntyre K.W., Shuster D.J., O'Day K.D., Penhallow B., Hung C.-H., Doweyko A.M., Kamath A., Zhang H., Marathe P., Kanner S.B., Lin T.-A., Dodd J.H., Barrish J.C., and Wityak J. Biog. Med. Chem. Lett. 16 (2006) 3706
14. Values are means of three experiments with standard deviation of less than 15%. Assay conditions: ATP concentration at 10 μM, reaction time = 35 min, enzyme concentration (μg/well) = 0.008, Substrate concentration (μg/well) = 0.625 at 30 °C.
15. Till J.H., Becerra M., Watty A., Lu Y., Ma Y., Neubert T.A., Burden S.J., and Hubbard S.R. Structure 10 (2002) 1187
16. Schrodinger, L. L. C. 32nd Floor, Tower 45, 120 West Forty-Fifth Street, New York, 10036, 2003.
17. Tokarski J.S., Newitt J.A., Chang C.Y.J., Cheng J.D., Wittekind M., Kiefer S.E., Kish K., Lee F.Y.F., Borzilleri R., Lombardo L.J., Xie D., Zhang Y., and Klei H.E. Cancer Res. 66 (2006) 5790
18. 3H}-thymidine at 4 μCi/ml for 3 h. Values are means of three experiments.