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Items: 1 to 20 of 101

1.

Optimized S-trityl-L-cysteine-based inhibitors of kinesin spindle protein with potent in vivo antitumor activity in lung cancer xenograft models.

Good JA, Wang F, Rath O, Kaan HY, Talapatra SK, Podg├│rski D, MacKay SP, Kozielski F.

J Med Chem. 2013 Mar 14;56(5):1878-93. doi: 10.1021/jm3014597. Epub 2013 Feb 27.

2.

Triphenylbutanamines: kinesin spindle protein inhibitors with in vivo antitumor activity.

Wang F, Good JA, Rath O, Kaan HY, Sutcliffe OB, Mackay SP, Kozielski F.

J Med Chem. 2012 Feb 23;55(4):1511-25. doi: 10.1021/jm201195m. Epub 2012 Feb 13.

3.

Structure-activity relationship of S-trityl-L-cysteine analogues as inhibitors of the human mitotic kinesin Eg5.

Debonis S, Skoufias DA, Indorato RL, Liger F, Marquet B, Laggner C, Joseph B, Kozielski F.

J Med Chem. 2008 Mar 13;51(5):1115-25. doi: 10.1021/jm070606z. Epub 2008 Feb 12.

PMID:
18266314
4.

Activity of the kinesin spindle protein inhibitor ispinesib (SB-715992) in models of breast cancer.

Purcell JW, Davis J, Reddy M, Martin S, Samayoa K, Vo H, Thomsen K, Bean P, Kuo WL, Ziyad S, Billig J, Feiler HS, Gray JW, Wood KW, Cases S.

Clin Cancer Res. 2010 Jan 15;16(2):566-76. doi: 10.1158/1078-0432.CCR-09-1498. Epub 2010 Jan 12.

5.

A potent chemotherapeutic strategy in prostate cancer: S-(methoxytrityl)-L-cysteine, a novel Eg5 inhibitor.

Xing ND, Ding ST, Saito R, Nishizawa K, Kobayashi T, Inoue T, Oishi S, Fujii N, Lv JJ, Ogawa O, Nishiyama H.

Asian J Androl. 2011 Mar;13(2):236-41. doi: 10.1038/aja.2010.171. Epub 2011 Feb 7.

6.

Initial testing (stage 1) of the kinesin spindle protein inhibitor ispinesib by the pediatric preclinical testing program.

Carol H, Lock R, Houghton PJ, Morton CL, Kolb EA, Gorlick R, Reynolds CP, Maris JM, Keir ST, Billups CA, Smith MA.

Pediatr Blood Cancer. 2009 Dec 15;53(7):1255-63. doi: 10.1002/pbc.22056.

7.

In vitro screening for inhibitors of the human mitotic kinesin Eg5 with antimitotic and antitumor activities.

DeBonis S, Skoufias DA, Lebeau L, Lopez R, Robin G, Margolis RL, Wade RH, Kozielski F.

Mol Cancer Ther. 2004 Sep;3(9):1079-90.

8.

S-trityl-L-cysteine is a reversible, tight binding inhibitor of the human kinesin Eg5 that specifically blocks mitotic progression.

Skoufias DA, DeBonis S, Saoudi Y, Lebeau L, Crevel I, Cross R, Wade RH, Hackney D, Kozielski F.

J Biol Chem. 2006 Jun 30;281(26):17559-69. Epub 2006 Feb 28.

9.

Doing the methylene shuffle--further insights into the inhibition of mitotic kinesin Eg5 with S-trityl L-cysteine.

Abualhasan MN, Good JA, Wittayanarakul K, Anthony NG, Berretta G, Rath O, Kozielski F, Sutcliffe OB, Mackay SP.

Eur J Med Chem. 2012 Aug;54:483-98. doi: 10.1016/j.ejmech.2012.05.034. Epub 2012 Jun 7.

PMID:
22749640
10.

Identification of the protein binding region of S-trityl-L-cysteine, a new potent inhibitor of the mitotic kinesin Eg5.

Brier S, Lemaire D, Debonis S, Forest E, Kozielski F.

Biochemistry. 2004 Oct 19;43(41):13072-82.

PMID:
15476401
11.

Eg5 inhibitor, a novel potent targeted therapy, induces cell apoptosis in renal cell carcinoma.

Ding S, Zhao Z, Sun D, Wu F, Bi D, Lu J, Xing N, Sun L, Wu H, Ding K.

Tumour Biol. 2014 Aug;35(8):7659-68. doi: 10.1007/s13277-014-2022-x. Epub 2014 May 7.

PMID:
24801905
12.

A potent chemotherapeutic strategy for bladder cancer: (S)-methoxy-trityl-L-cystein, a novel Eg5 inhibitor.

Ding S, Nishizawa K, Kobayashi T, Oishi S, Lv J, Fujii N, Ogawa O, Nishiyama H.

J Urol. 2010 Sep;184(3):1175-81. doi: 10.1016/j.juro.2010.04.073. Epub 2010 Jul 21.

PMID:
20663523
13.

Structure-activity relationship and multidrug resistance study of new S-trityl-L-cysteine derivatives as inhibitors of Eg5.

Kaan HY, Weiss J, Menger D, Ulaganathan V, Tkocz K, Laggner C, Popowycz F, Joseph B, Kozielski F.

J Med Chem. 2011 Mar 24;54(6):1576-86. doi: 10.1021/jm100991m. Epub 2011 Feb 23.

PMID:
21344920
14.

Photocontrol of the mitotic kinesin Eg5 using a novel S-trityl-L-cysteine analogue as a photochromic inhibitor.

Ishikawa K, Tohyama K, Mitsuhashi S, Maruta S.

J Biochem. 2014 Apr;155(4):257-63. doi: 10.1093/jb/mvu004. Epub 2014 Jan 21.

PMID:
24451491
15.

Validating the mitotic kinesin Eg5 as a therapeutic target in pancreatic cancer cells and tumor xenografts using a specific inhibitor.

Liu M, Yu H, Huo L, Liu J, Li M, Zhou J.

Biochem Pharmacol. 2008 Jul 15;76(2):169-78. doi: 10.1016/j.bcp.2008.04.018. Epub 2008 May 4.

PMID:
18539263
16.

STLC-resistant cell lines as tools to classify chemically divergent Eg5 targeting agents according to their mode of action and target specificity.

Indorato RL, DeBonis S, Kozielski F, Garcia-Saez I, Skoufias DA.

Biochem Pharmacol. 2013 Nov 15;86(10):1441-51. doi: 10.1016/j.bcp.2013.09.003. Epub 2013 Sep 13.

PMID:
24041742
17.

Docetaxel-resistant prostate cancer cells remain sensitive to S-trityl-L-cysteine-mediated Eg5 inhibition.

Wiltshire C, Singh BL, Stockley J, Fleming J, Doyle B, Barnetson R, Robson CN, Kozielski F, Leung HY.

Mol Cancer Ther. 2010 Jun;9(6):1730-9. doi: 10.1158/1535-7163.MCT-09-1103. Epub 2010 Jun 1.

18.

Receptor-ligand interaction-based virtual screening for novel Eg5/kinesin spindle protein inhibitors.

Nagarajan S, Skoufias DA, Kozielski F, Pae AN.

J Med Chem. 2012 Mar 22;55(6):2561-73. doi: 10.1021/jm201290v. Epub 2012 Mar 1.

PMID:
22309208
19.

The novel kinesin spindle protein (KSP) inhibitor SB-743921 exhibits marked activity in in vivo and in vitro models of aggressive large B-cell lymphoma.

Bongero D, Paoluzzi L, Marchi E, Zullo KM, Neisa R, Mao Y, Escandon R, Wood K, O'Connor OA.

Leuk Lymphoma. 2015;56(10):2945-52. doi: 10.3109/10428194.2015.1020058. Epub 2015 May 14.

PMID:
25860245
20.

Synthesis and biological evaluation of L-cysteine derivatives as mitotic kinesin Eg5 inhibitors.

Ogo N, Oishi S, Matsuno K, Sawada J, Fujii N, Asai A.

Bioorg Med Chem Lett. 2007 Jul 15;17(14):3921-4. Epub 2007 May 3.

PMID:
17524640

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