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Antivascular and antitumor evaluation of 2-amino-4-(3-bromo-4,5-dimethoxy-phenyl)-3-cyano-4H-chromenes, a novel series of anticancer agents.

Gourdeau H, Leblond L, Hamelin B, Desputeau C, Dong K, Kianicka I, Custeau D, Boudreau C, Geerts L, Cai SX, Drewe J, Labrecque D, Kasibhatla S, Tseng B.

Mol Cancer Ther. 2004 Nov;3(11):1375-84.


Discovery and mechanism of action of a novel series of apoptosis inducers with potential vascular targeting activity.

Kasibhatla S, Gourdeau H, Meerovitch K, Drewe J, Reddy S, Qiu L, Zhang H, Bergeron F, Bouffard D, Yang Q, Herich J, Lamothe S, Cai SX, Tseng B.

Mol Cancer Ther. 2004 Nov;3(11):1365-74.


Discovery of 4-aryl-4H-chromenes as a new series of apoptosis inducers using a cell- and caspase-based high-throughput screening assay. 1. Structure-activity relationships of the 4-aryl group.

Kemnitzer W, Drewe J, Jiang S, Zhang H, Wang Y, Zhao J, Jia S, Herich J, Labreque D, Storer R, Meerovitch K, Bouffard D, Rej R, Denis R, Blais C, Lamothe S, Attardo G, Gourdeau H, Tseng B, Kasibhatla S, Cai SX.

J Med Chem. 2004 Dec 2;47(25):6299-310.


Discovery of 4-aryl-4H-chromenes as a new series of apoptosis inducers using a cell- and caspase-based high throughput screening assay. 4. Structure-activity relationships of N-alkyl substituted pyrrole fused at the 7,8-positions.

Kemnitzer W, Drewe J, Jiang S, Zhang H, Crogan-Grundy C, Labreque D, Bubenick M, Attardo G, Denis R, Lamothe S, Gourdeau H, Tseng B, Kasibhatla S, Cai SX.

J Med Chem. 2008 Feb 14;51(3):417-23. doi: 10.1021/jm7010657. Epub 2008 Jan 16.


ZD6126: a novel vascular-targeting agent that causes selective destruction of tumor vasculature.

Davis PD, Dougherty GJ, Blakey DC, Galbraith SM, Tozer GM, Holder AL, Naylor MA, Nolan J, Stratford MR, Chaplin DJ, Hill SA.

Cancer Res. 2002 Dec 15;62(24):7247-53.


A vascular targeted pan phosphoinositide 3-kinase inhibitor prodrug, SF1126, with antitumor and antiangiogenic activity.

Garlich JR, De P, Dey N, Su JD, Peng X, Miller A, Murali R, Lu Y, Mills GB, Kundra V, Shu HK, Peng Q, Durden DL.

Cancer Res. 2008 Jan 1;68(1):206-15. doi: 10.1158/0008-5472.CAN-07-0669. Erratum in: Cancer Res. 2008 Jul 15;68(1):6030.


BNC105: a novel tubulin polymerization inhibitor that selectively disrupts tumor vasculature and displays single-agent antitumor efficacy.

Kremmidiotis G, Leske AF, Lavranos TC, Beaumont D, Gasic J, Hall A, O'Callaghan M, Matthews CA, Flynn B.

Mol Cancer Ther. 2010 Jun;9(6):1562-73. doi: 10.1158/1535-7163.MCT-09-0815. Epub 2010 Jun 1.


Discovery of 4-aryl-4H-chromenes as a new series of apoptosis inducers using a cell- and caspase-based high-throughput screening assay. 3. Structure-activity relationships of fused rings at the 7,8-positions.

Kemnitzer W, Drewe J, Jiang S, Zhang H, Zhao J, Crogan-Grundy C, Xu L, Lamothe S, Gourdeau H, Denis R, Tseng B, Kasibhatla S, Cai SX.

J Med Chem. 2007 Jun 14;50(12):2858-64. Epub 2007 May 11.


Antitumor efficacy of conventional anticancer drugs is enhanced by the vascular targeting agent ZD6126.

Siemann DW, Rojiani AM.

Int J Radiat Oncol Biol Phys. 2002 Dec 1;54(5):1512-7.


Antitumor activity of orally bioavailable farnesyltransferase inhibitor, ABT-100, is mediated by antiproliferative, proapoptotic, and antiangiogenic effects in xenograft models.

Ferguson D, Rodriguez LE, Palma JP, Refici M, Jarvis K, O'Connor J, Sullivan GM, Frost D, Marsh K, Bauch J, Zhang H, Lin NH, Rosenberg S, Sham HL, Joseph IB.

Clin Cancer Res. 2005 Apr 15;11(8):3045-54.


CRA-026440: a potent, broad-spectrum, hydroxamic histone deacetylase inhibitor with antiproliferative and antiangiogenic activity in vitro and in vivo.

Cao ZA, Bass KE, Balasubramanian S, Liu L, Schultz B, Verner E, Dai Y, Molina RA, Davis JR, Misialek S, Sendzik M, Orr CJ, Leung L, Callan O, Young P, Dalrymple SA, Buggy JJ.

Mol Cancer Ther. 2006 Jul;5(7):1693-701.


Activity screening and structure-activity relationship of the hit compounds targeting APN/CD13.

Wang X, Jing F, Zhu H, Fang H, Zhang J, Xu W.

Fundam Clin Pharmacol. 2011 Apr;25(2):217-28. doi: 10.1111/j.1472-8206.2010.00844.x.


MPC-6827: a small-molecule inhibitor of microtubule formation that is not a substrate for multidrug resistance pumps.

Kasibhatla S, Baichwal V, Cai SX, Roth B, Skvortsova I, Skvortsov S, Lukas P, English NM, Sirisoma N, Drewe J, Pervin A, Tseng B, Carlson RO, Pleiman CM.

Cancer Res. 2007 Jun 15;67(12):5865-71.


Endorepellin in vivo: targeting the tumor vasculature and retarding cancer growth and metabolism.

Bix G, Castello R, Burrows M, Zoeller JJ, Weech M, Iozzo RA, Cardi C, Thakur ML, Barker CA, Camphausen K, Iozzo RV.

J Natl Cancer Inst. 2006 Nov 15;98(22):1634-46.


The microtubule depolymerizing agent CYT997 causes extensive ablation of tumor vasculature in vivo.

Burns CJ, Fantino E, Powell AK, Shnyder SD, Cooper PA, Nelson S, Christophi C, Malcontenti-Wilson C, Dubljevic V, Harte MF, Joffe M, Phillips ID, Segal D, Wilks AF, Smith GD.

J Pharmacol Exp Ther. 2011 Dec;339(3):799-806. doi: 10.1124/jpet.111.186965. Epub 2011 Sep 14.


KRN951, a highly potent inhibitor of vascular endothelial growth factor receptor tyrosine kinases, has antitumor activities and affects functional vascular properties.

Nakamura K, Taguchi E, Miura T, Yamamoto A, Takahashi K, Bichat F, Guilbaud N, Hasegawa K, Kubo K, Fujiwara Y, Suzuki R, Kubo K, Shibuya M, Isae T.

Cancer Res. 2006 Sep 15;66(18):9134-42.


Discovery of N-(4-methoxyphenyl)-N,2-dimethylquinazolin-4-amine, a potent apoptosis inducer and efficacious anticancer agent with high blood brain barrier penetration.

Sirisoma N, Pervin A, Zhang H, Jiang S, Willardsen JA, Anderson MB, Mather G, Pleiman CM, Kasibhatla S, Tseng B, Drewe J, Cai SX.

J Med Chem. 2009 Apr 23;52(8):2341-51. doi: 10.1021/jm801315b.


A novel class of tubulin inhibitors that exhibit potent antiproliferation and in vitro vessel-disrupting activity.

Meng F, Cai X, Duan J, Matteucci MG, Hart CP.

Cancer Chemother Pharmacol. 2008 May;61(6):953-63. Epub 2007 Jul 18.

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