Tubulin inhibitors. Synthesis and biological activity of HTI-286 analogs with B-segment heterosubstituents

Bioorganic and Medicinal Chemistry Letters

Volumn 14, Issue 16, 2004, Pages 4329-4332

  Niu, Chuan ^a   Smith, Daniel ^a,b   Zask, Arie ^a   Loganzo, Frank ^a   Discafani, Carolyn ^a   Beyer, Carl ^a   Greenberger, Lee ^a   Ayral Kaloustian, Semiramis ^a  

^a WYETH RESEARCH   (United States)

^b UNIVERSITY OF VIRGINIA   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

FLUORIDE; GLYCOPROTEIN P; METHYLSULFIDE; PACLITAXEL; PROTEIN INHIBITOR; SULFIDE; TALTOBULIN; TUBULIN; UNCLASSIFIED DRUG;

ARTICLE; CELL ASSAY; CELL LINE; CYTOTOXICITY; DRUG ACTIVITY; DRUG POTENCY; DRUG STRUCTURE; DRUG SYNTHESIS; INHIBITION KINETICS; POLYMERIZATION; PROTEIN EXPRESSION; STRUCTURE ACTIVITY RELATION; STRUCTURE ANALYSIS;

CELL LINE; HUMANS; MELANOMA; OLIGOPEPTIDES; STRUCTURE-ACTIVITY RELATIONSHIP; TRANSPLANTATION, HETEROLOGOUS; TUBULIN MODULATORS;

EID: 3142755555     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2004.05.077     Document Type: Article

References (14)

1. Gottesman M.M. Annu. Rev. Med. 53:2002;615
2. Talpir R., Benayahu Y., Kashman Y., Pannell L., Schleyer M. Tetrahedron Lett. 35:1994;4453
3. Coleman J.E., Dilip de Silva E., Kong F., Andersen R.J., Allen T.M. Tetrahedron. 51:1995;10653
4. Anderson H.J., Coleman J.E., Andersen R.J., Roberge M. Cancer Chemother. Pharmacol. 39:1997;223
5. Andersen R.J., Coleman J.E. Tetrahedron Lett. 38:1997;317
6. (a) Andersen, R. J. WO 99/32509
7. Nieman J.A., Coleman J.E., Wallace D.J., Piers E., Lim L.Y., Roberge M., Andersen R.J. J. Nat. Prod. 66:2003;183
8. Loganzo F., Discafani C.M., Annable T., Beyer C., Musto S., Hari M., Tan X., Hardy C., Hernandez R., Baxter M., Singanallore T., Khafizova G., Poruchynsky M.S., Fojo T., Nieman J.A., Ayral-Kaloustian S., Zask A., Andersen R.J., Greenberger L.M. Cancer Res. 63:2003;1838
9. Ratain M.J., Undevia S., Janisch L., Roman S., Mayer P., Buckwalter M., Foss D., Hamilton B.L., Fischer J., Bukowski R.M. Proc. Am. Soc. Clin. Oncol. 22:2003;129
10. Zask, A.; Birnberg, G.; Cheung, K.; Kaplan, J.; Niu, C.; Norton, E.; Suayan, R.; Yamashita, A.; Cole, D.; Tang, Z.; Krishnamurthy, G.; Williamson, R.; Khafizova, G.; Musto, S.; Hernandez, R.; Annable, T.; Yang, X.; Discafani, C.; Beyer, C.; Greenberger, L. M.; Loganzo, F.; Ayral-Kaloustian, S. J. Med. Chem., in press
11. Schmidt U., Schumacher A., Mittendorf J., Riedl B. J. Pept. Res. 52:1998;143
12. Frerot E., Coste J., Pantaloni A., Dufour M.-N., Jouin P. Tetrahedron. 47:1991;259
13. Kansy M., Senner F., Gubernator K. J. Med. Chem. 41:1998;1007-1010
14. 2)/2] for up to 21 days. Relative tumor growth (Mean tumor mass on day of measurement divided by the mean tumor mass on day zero.) was determined for each treatment group. Statistical analysis (Student- t -test) of log relative tumor growth was used to compare treated verses control group in each experiment. A p -value ( p≤0.05 ) indicates a statistically significant reduction in relative tumor growth of treated group compared to the vehicle control