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Significant antitumor activity in vivo following treatment with the microtubule agent ENMD-1198.

LaVallee TM, Burke PA, Swartz GM, Hamel E, Agoston GE, Shah J, Suwandi L, Hanson AD, Fogler WE, Sidor CF, Treston AM.

Mol Cancer Ther. 2008 Jun;7(6):1472-82. doi: 10.1158/1535-7163.MCT-08-0107.


Structure activity analysis of 2-methoxyestradiol analogues reveals targeting of microtubules as the major mechanism of antiproliferative and proapoptotic activity.

Chua YS, Chua YL, Hagen T.

Mol Cancer Ther. 2010 Jan;9(1):224-35. doi: 10.1158/1535-7163.MCT-09-1003. Epub 2010 Jan 6.


2-Methoxyestradiol suppresses microtubule dynamics and arrests mitosis without depolymerizing microtubules.

Kamath K, Okouneva T, Larson G, Panda D, Wilson L, Jordan MA.

Mol Cancer Ther. 2006 Sep;5(9):2225-33.


Novel 2-methoxyestradiol analogues with antitumor activity.

Tinley TL, Leal RM, Randall-Hlubek DA, Cessac JW, Wilkens LR, Rao PN, Mooberry SL.

Cancer Res. 2003 Apr 1;63(7):1538-49.


BPR0L075, a novel synthetic indole compound with antimitotic activity in human cancer cells, exerts effective antitumoral activity in vivo.

Kuo CC, Hsieh HP, Pan WY, Chen CP, Liou JP, Lee SJ, Chang YL, Chen LT, Chen CT, Chang JY.

Cancer Res. 2004 Jul 1;64(13):4621-8.


Pseudolaric acid B, a novel microtubule-destabilizing agent that circumvents multidrug resistance phenotype and exhibits antitumor activity in vivo.

Wong VK, Chiu P, Chung SS, Chow LM, Zhao YZ, Yang BB, Ko BC.

Clin Cancer Res. 2005 Aug 15;11(16):6002-11.


ENMD-1198, a new analogue of 2-methoxyestradiol, displays both antiangiogenic and vascular-disrupting properties.

Pasquier E, Sinnappan S, Munoz MA, Kavallaris M.

Mol Cancer Ther. 2010 May;9(5):1408-18. doi: 10.1158/1535-7163.MCT-09-0894. Epub 2010 May 4.


ENMD-1198, a novel tubulin-binding agent reduces HIF-1alpha and STAT3 activity in human hepatocellular carcinoma(HCC) cells, and inhibits growth and vascularization in vivo.

Moser C, Lang SA, Mori A, Hellerbrand C, Schlitt HJ, Geissler EK, Fogler WE, Stoeltzing O.

BMC Cancer. 2008 Jul 23;8:206. doi: 10.1186/1471-2407-8-206.


Structure-based virtual screening of novel tubulin inhibitors and their characterization as anti-mitotic agents.

Kim ND, Park ES, Kim YH, Moon SK, Lee SS, Ahn SK, Yu DY, No KT, Kim KH.

Bioorg Med Chem. 2010 Oct 1;18(19):7092-100. doi: 10.1016/j.bmc.2010.07.072. Epub 2010 Aug 6.


Design, synthesis, and biological evaluation of thiophene analogues of chalcones.

Romagnoli R, Baraldi PG, Carrion MD, Cara CL, Cruz-Lopez O, Preti D, Tolomeo M, Grimaudo S, Di Cristina A, Zonta N, Balzarini J, Brancale A, Sarkar T, Hamel E.

Bioorg Med Chem. 2008 May 15;16(10):5367-76. doi: 10.1016/j.bmc.2008.04.026. Epub 2008 Apr 15.


Synthesis, antiproliferative, and pharmacokinetic properties of 3- and 17-double-modified analogs of 2-methoxyestradiol.

Agoston GE, Shah JH, Suwandi L, Hanson AD, Zhan X, LaVallee TM, Pribluda V, Treston AM.

Bioorg Med Chem Lett. 2009 Nov 1;19(21):6241-4. doi: 10.1016/j.bmcl.2009.08.020. Epub 2009 Aug 8.


Quinolone analogue inhibits tubulin polymerization and induces apoptosis via Cdk1-involved signaling pathways.

Chen YC, Lu PH, Pan SL, Teng CM, Kuo SC, Lin TP, Ho YF, Huang YC, Guh JH.

Biochem Pharmacol. 2007 Jun 30;74(1):10-9. Epub 2007 Mar 24.


2-aroylindoles, a novel class of potent, orally active small molecule tubulin inhibitors.

Beckers T, Reissmann T, Schmidt M, Burger AM, Fiebig HH, Vanhoefer U, Pongratz H, Hufsky H, Hockemeyer J, Frieser M, Mahboobi S.

Cancer Res. 2002 Jun 1;62(11):3113-9.


9-Benzylidene-naphtho[2,3-b]thiophen-4-ones as novel antimicrotubule agents-synthesis, antiproliferative activity, and inhibition of tubulin polymerization.

Zuse A, Schmidt P, Baasner S, Böhm KJ, Müller K, Gerlach M, Günther EG, Unger E, Prinz H.

J Med Chem. 2006 Dec 28;49(26):7816-25.


Class I beta-tubulin mutations in 2-methoxyestradiol-resistant acute lymphoblastic leukemia cells: implications for drug-target interactions.

Liaw TY, Salam NK, McKay MJ, Cunningham AM, Hibbs DE, Kavallaris M.

Mol Cancer Ther. 2008 Oct;7(10):3150-9. doi: 10.1158/1535-7163.MCT-08-0442.


Voreloxin, formerly SNS-595, has potent activity against a broad panel of cancer cell lines and in vivo tumor models.

Hoch U, Lynch J, Sato Y, Kashimoto S, Kajikawa F, Furutani Y, Silverman JA.

Cancer Chemother Pharmacol. 2009 Jun;64(1):53-65. doi: 10.1007/s00280-008-0850-3. Epub 2008 Oct 19.


A-204197, a new tubulin-binding agent with antimitotic activity in tumor cell lines resistant to known microtubule inhibitors.

Tahir SK, Han EK, Credo B, Jae HS, Pietenpol JA, Scatena CD, Wu-Wong JR, Frost D, Sham H, Rosenberg SH, Ng SC.

Cancer Res. 2001 Jul 15;61(14):5480-5.

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