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Items: 1 to 50 of 200

1.

Structure Guided Design, Synthesis, and Biological Evaluation of Novel Benzosuberene Analogues as Inhibitors of Tubulin Polymerization.

Niu H, Strecker TE, Gerberich JL, Campbell JW 3rd, Saha D, Mondal D, Hamel E, Chaplin DJ, Mason RP, Trawick ML, Pinney KG.

J Med Chem. 2019 Jun 13;62(11):5594-5615. doi: 10.1021/acs.jmedchem.9b00551. Epub 2019 May 24.

PMID:
31059248
2.

Synthesis of dihydronaphthalene analogues inspired by combretastatin A-4 and their biological evaluation as anticancer agents.

Maguire CJ, Chen Z, Mocharla VP, Sriram M, Strecker TE, Hamel E, Zhou H, Lopez R, Wang Y, Mason RP, Chaplin DJ, Trawick ML, Pinney KG.

Medchemcomm. 2018 Aug 24;9(10):1649-1662. doi: 10.1039/c8md00322j. eCollection 2018 Oct 1.

3.

Clinical trial experience with CA4P anticancer therapy: focus on efficacy, cardiovascular adverse events, and hypertension management.

Grisham R, Ky B, Tewari KS, Chaplin DJ, Walker J.

Gynecol Oncol Res Pract. 2018 Jan 5;5:1. doi: 10.1186/s40661-017-0058-5. eCollection 2018. Review.

4.

Realizing the Potential of Vascular Targeted Therapy: The Rationale for Combining Vascular Disrupting Agents and Anti-Angiogenic Agents to Treat Cancer.

Siemann DW, Chaplin DJ, Horsman MR.

Cancer Invest. 2017 Sep 14;35(8):519-534. doi: 10.1080/07357907.2017.1364745. Epub 2017 Sep 5.

PMID:
28872367
5.

The development and use of vascular targeted therapy in ovarian cancer.

Chase DM, Chaplin DJ, Monk BJ.

Gynecol Oncol. 2017 May;145(2):393-406. doi: 10.1016/j.ygyno.2017.01.031. Epub 2017 Feb 24. Review.

6.

Synthesis and Biological Evaluation of Benzocyclooctene-based and Indene-based Anticancer Agents that Function as Inhibitors of Tubulin Polymerization.

Herdman CA, Strecker TE, Tanpure RP, Chen Z, Winters A, Gerberich J, Liu L, Hamel E, Mason RP, Chaplin DJ, Trawick ML, Pinney KG.

Medchemcomm. 2016 Dec 1;7(12):2418-2427. doi: 10.1039/C6MD00459H. Epub 2016 Sep 22.

7.

Synthesis and biological evaluation of a water-soluble phosphate prodrug salt and structural analogues of KGP94, a lead inhibitor of cathepsin L.

Parker EN, Odutola SO, Wang Y, Strecker TE, Mukherjee R, Shi Z, Chaplin DJ, Trawick ML, Pinney KG.

Bioorg Med Chem Lett. 2017 Mar 1;27(5):1304-1310. doi: 10.1016/j.bmcl.2016.12.039. Epub 2016 Dec 21.

PMID:
28117205
8.

Bioreductively activatable prodrug conjugates of phenstatin designed to target tumor hypoxia.

Winn BA, Shi Z, Carlson GJ, Wang Y, Nguyen BL, Kelly EM, Ross RD 4th, Hamel E, Chaplin DJ, Trawick ML, Pinney KG.

Bioorg Med Chem Lett. 2017 Feb 1;27(3):636-641. doi: 10.1016/j.bmcl.2016.11.093. Epub 2016 Dec 1.

9.

Chemosensitizing AML cells by targeting bone marrow endothelial cells.

Bosse RC, Wasserstrom B, Meacham A, Wise E, Drusbosky L, Walter GA, Chaplin DJ, Siemann DW, Purich DL, Cogle CR.

Exp Hematol. 2016 May;44(5):363-377.e5. doi: 10.1016/j.exphem.2016.02.003. Epub 2016 Feb 16.

PMID:
26898708
10.

Design, synthesis, and biological evaluation of water-soluble amino acid prodrug conjugates derived from combretastatin, dihydronaphthalene, and benzosuberene-based parent vascular disrupting agents.

Devkota L, Lin CM, Strecker TE, Wang Y, Tidmore JK, Chen Z, Guddneppanavar R, Jelinek CJ, Lopez R, Liu L, Hamel E, Mason RP, Chaplin DJ, Trawick ML, Pinney KG.

Bioorg Med Chem. 2016 Mar 1;24(5):938-956. doi: 10.1016/j.bmc.2016.01.007. Epub 2016 Jan 6.

11.

Structural interrogation of benzosuberene-based inhibitors of tubulin polymerization.

Herdman CA, Devkota L, Lin CM, Niu H, Strecker TE, Lopez R, Liu L, George CS, Tanpure RP, Hamel E, Chaplin DJ, Mason RP, Trawick ML, Pinney KG.

Bioorg Med Chem. 2015 Dec 15;23(24):7497-520.

12.

Synthesis and biochemical evaluation of benzoylbenzophenone thiosemicarbazone analogues as potent and selective inhibitors of cathepsin L.

Parker EN, Song J, Kishore Kumar GD, Odutola SO, Chavarria GE, Charlton-Sevcik AK, Strecker TE, Barnes AL, Sudhan DR, Wittenborn TR, Siemann DW, Horsman MR, Chaplin DJ, Trawick ML, Pinney KG.

Bioorg Med Chem. 2015 Nov 1;23(21):6974-92. doi: 10.1016/j.bmc.2015.09.036. Epub 2015 Sep 25.

13.

The vascular disrupting activity of OXi8006 in endothelial cells and its phosphate prodrug OXi8007 in breast tumor xenografts.

Strecker TE, Odutola SO, Lopez R, Cooper MS, Tidmore JK, Charlton-Sevcik AK, Li L, MacDonough MT, Hadimani MB, Ghatak A, Liu L, Chaplin DJ, Mason RP, Pinney KG, Trawick ML.

Cancer Lett. 2015 Dec 1;369(1):229-41. doi: 10.1016/j.canlet.2015.08.021. Epub 2015 Sep 1.

14.

Exaggerated hypertensive response to combretastatin A-4 phosphate in hypertensive rats: Effective pharmacological inhibition by diltiazem.

Ke Q, Samad MA, Bae S, Chaplin DJ, Kang PM.

Vascul Pharmacol. 2015 Nov;74:73-79. doi: 10.1016/j.vph.2015.05.004. Epub 2015 May 16.

PMID:
25989107
15.

Synthesis of structurally diverse benzosuberene analogues and their biological evaluation as anti-cancer agents.

Tanpure RP, George CS, Strecker TE, Devkota L, Tidmore JK, Lin CM, Herdman CA, Macdonough MT, Sriram M, Chaplin DJ, Trawick ML, Pinney KG.

Bioorg Med Chem. 2013 Dec 15;21(24):8019-32. doi: 10.1016/j.bmc.2013.08.035. Epub 2013 Sep 4.

16.

Synthesis of a 2-aryl-3-aroyl indole salt (OXi8007) resembling combretastatin A-4 with application as a vascular disrupting agent.

Hadimani MB, Macdonough MT, Ghatak A, Strecker TE, Lopez R, Sriram M, Nguyen BL, Hall JJ, Kessler RJ, Shirali AR, Liu L, Garner CM, Pettit GR, Hamel E, Chaplin DJ, Mason RP, Trawick ML, Pinney KG.

J Nat Prod. 2013 Sep 27;76(9):1668-78. doi: 10.1021/np400374w. Epub 2013 Sep 9.

17.

Synthesis and biological evaluation of indole-based, anti-cancer agents inspired by the vascular disrupting agent 2-(3'-hydroxy-4'-methoxyphenyl)-3-(3″,4″,5″-trimethoxybenzoyl)-6-methoxyindole (OXi8006).

Macdonough MT, Strecker TE, Hamel E, Hall JJ, Chaplin DJ, Trawick ML, Pinney KG.

Bioorg Med Chem. 2013 Nov 1;21(21):6831-43. doi: 10.1016/j.bmc.2013.07.028. Epub 2013 Jul 23.

18.

An Amino-Benzosuberene Analogue That Inhibits Tubulin Assembly and Demonstrates Remarkable Cytotoxicity.

Tanpure RP, George CS, Sriram M, Strecker TE, Tidmore JK, Hamel E, Charlton-Sevcik AK, Chaplin DJ, Trawick ML, Pinney KG.

Medchemcomm. 2012 Jun;3(6):720-724.

19.

Small-molecule inhibitors of cathepsin L incorporating functionalized ring-fused molecular frameworks.

Song J, Jones LM, Chavarria GE, Charlton-Sevcik AK, Jantz A, Johansen A, Bayeh L, Soeung V, Snyder LK, Lade SD Jr, Chaplin DJ, Trawick ML, Pinney KG.

Bioorg Med Chem Lett. 2013 May 1;23(9):2801-7. doi: 10.1016/j.bmcl.2012.12.025. Epub 2012 Dec 20.

PMID:
23540644
20.

Initial evaluation of the antitumour activity of KGP94, a functionalized benzophenone thiosemicarbazone inhibitor of cathepsin L.

Chavarria GE, Horsman MR, Arispe WM, Kumar GD, Chen SE, Strecker TE, Parker EN, Chaplin DJ, Pinney KG, Trawick ML.

Eur J Med Chem. 2012 Dec;58:568-72. doi: 10.1016/j.ejmech.2012.10.039. Epub 2012 Oct 29.

PMID:
23168380
21.

Synthesis and biochemical evaluation of thiochromanone thiosemicarbazone analogues as inhibitors of cathepsin L.

Song J, Jones LM, Kumar GD, Conner ES, Bayeh L, Chavarria GE, Charlton-Sevcik AK, Chen SE, Chaplin DJ, Trawick ML, Pinney KG.

ACS Med Chem Lett. 2012 Apr 18;3(6):450-3. doi: 10.1021/ml200299g. eCollection 2012 Jun 14.

22.

Phase I clinical and pharmacokinetic evaluation of the vascular-disrupting agent OXi4503 in patients with advanced solid tumors.

Patterson DM, Zweifel M, Middleton MR, Price PM, Folkes LK, Stratford MR, Ross P, Halford S, Peters J, Balkissoon J, Chaplin DJ, Padhani AR, Rustin GJ.

Clin Cancer Res. 2012 Mar 1;18(5):1415-25. doi: 10.1158/1078-0432.CCR-11-2414. Epub 2012 Jan 10.

23.

Regioselective synthesis of water-soluble monophosphate derivatives of combretastatin A-1.

Tanpure RP, Nguyen BL, Strecker TE, Aguirre S, Sharma S, Chaplin DJ, Siim BG, Hamel E, Lippert JW, Pettit GR, Trawick ML, Pinney KG.

J Nat Prod. 2011 Jul 22;74(7):1568-74. doi: 10.1021/np200104t. Epub 2011 Jun 30.

24.

Phase II trial of combretastatin A4 phosphate, carboplatin, and paclitaxel in patients with platinum-resistant ovarian cancer.

Zweifel M, Jayson GC, Reed NS, Osborne R, Hassan B, Ledermann J, Shreeves G, Poupard L, Lu SP, Balkissoon J, Chaplin DJ, Rustin GJ.

Ann Oncol. 2011 Sep;22(9):2036-41. doi: 10.1093/annonc/mdq708. Epub 2011 Jan 27.

PMID:
21273348
25.

Functionalized benzophenone, thiophene, pyridine, and fluorene thiosemicarbazone derivatives as inhibitors of cathepsin L.

Kumar GD, Chavarria GE, Charlton-Sevcik AK, Yoo GK, Song J, Strecker TE, Siim BG, Chaplin DJ, Trawick ML, Pinney KG.

Bioorg Med Chem Lett. 2010 Nov 15;20(22):6610-5. doi: 10.1016/j.bmcl.2010.09.026. Epub 2010 Sep 15.

PMID:
20933415
26.

Guidelines for the welfare and use of animals in cancer research.

Workman P, Aboagye EO, Balkwill F, Balmain A, Bruder G, Chaplin DJ, Double JA, Everitt J, Farningham DA, Glennie MJ, Kelland LR, Robinson V, Stratford IJ, Tozer GM, Watson S, Wedge SR, Eccles SA; Committee of the National Cancer Research Institute.

Br J Cancer. 2010 May 25;102(11):1555-77. doi: 10.1038/sj.bjc.6605642.

27.

Regio- and stereospecific synthesis of mono-beta-d-glucuronic acid derivatives of combretastatin A-1.

Tanpure RP, Strecker TE, Chaplin DJ, Siim BG, Trawick ML, Pinney KG.

J Nat Prod. 2010 Jun 25;73(6):1093-101. doi: 10.1021/np100108e.

PMID:
20496923
28.

A Phase Ib trial of CA4P (combretastatin A-4 phosphate), carboplatin, and paclitaxel in patients with advanced cancer.

Rustin GJ, Shreeves G, Nathan PD, Gaya A, Ganesan TS, Wang D, Boxall J, Poupard L, Chaplin DJ, Stratford MR, Balkissoon J, Zweifel M.

Br J Cancer. 2010 Apr 27;102(9):1355-60. doi: 10.1038/sj.bjc.6605650. Epub 2010 Apr 13.

29.

Design, synthesis, and biological evaluation of potent thiosemicarbazone based cathepsin L inhibitors.

Kishore Kumar GD, Chavarria GE, Charlton-Sevcik AK, Arispe WM, Macdonough MT, Strecker TE, Chen SE, Siim BG, Chaplin DJ, Trawick ML, Pinney KG.

Bioorg Med Chem Lett. 2010 Feb 15;20(4):1415-9. doi: 10.1016/j.bmcl.2009.12.090. Epub 2010 Jan 6.

PMID:
20089402
30.

Low-dose metronomic cyclophosphamide combined with vascular disrupting therapy induces potent antitumor activity in preclinical human tumor xenograft models.

Daenen LG, Shaked Y, Man S, Xu P, Voest EE, Hoffman RM, Chaplin DJ, Kerbel RS.

Mol Cancer Ther. 2009 Oct;8(10):2872-81. doi: 10.1158/1535-7163.MCT-09-0583.

31.

Contribution of granulocyte colony-stimulating factor to the acute mobilization of endothelial precursor cells by vascular disrupting agents.

Shaked Y, Tang T, Woloszynek J, Daenen LG, Man S, Xu P, Cai SR, Arbeit JM, Voest EE, Chaplin DJ, Smythe J, Harris A, Nathan P, Judson I, Rustin G, Bertolini F, Link DC, Kerbel RS.

Cancer Res. 2009 Oct 1;69(19):7524-8. doi: 10.1158/0008-5472.CAN-09-0381. Epub 2009 Sep 8.

32.

Pharmacological inhibition of the hypertensive response to combretastatin A-4 phosphate in rats.

Ke Q, Bodyak N, Rigor DL, Hurst NW, Chaplin DJ, Kang PM.

Vascul Pharmacol. 2009 Nov-Dec;51(5-6):337-43. doi: 10.1016/j.vph.2009.08.004. Epub 2009 Sep 6.

PMID:
19737629
33.

A review and update of the current status of the vasculature-disabling agent combretastatin-A4 phosphate (CA4P).

Siemann DW, Chaplin DJ, Walicke PA.

Expert Opin Investig Drugs. 2009 Feb;18(2):189-97. doi: 10.1517/13543780802691068 . Review.

34.

Development of synthetic methodology suitable for the radiosynthesis of combretastatin A-1 (CA1) and its corresponding prodrug CA1P.

Shirali A, Sriram M, Hall JJ, Nguyen BL, Guddneppanavar R, Hadimani MB, Ackley JF, Siles R, Jelinek CJ, Arthasery P, Brown RC, Murrell VL, McMordie A, Sharma S, Chaplin DJ, Pinney KG.

J Nat Prod. 2009 Mar 27;72(3):414-21. doi: 10.1021/np800661r.

PMID:
19161336
35.

Design, synthesis, biochemical, and biological evaluation of nitrogen-containing trifluoro structural modifications of combretastatin A-4.

Hall JJ, Sriram M, Strecker TE, Tidmore JK, Jelinek CJ, Kumar GD, Hadimani MB, Pettit GR, Chaplin DJ, Trawick ML, Pinney KG.

Bioorg Med Chem Lett. 2008 Sep 15;18(18):5146-9. doi: 10.1016/j.bmcl.2008.07.070. Epub 2008 Jul 24.

PMID:
18710804
36.

Combretastatin dinitrogen-substituted stilbene analogues as tubulin-binding and vascular-disrupting agents.

Siles R, Ackley JF, Hadimani MB, Hall JJ, Mugabe BE, Guddneppanavar R, Monk KA, Chapuis JC, Pettit GR, Chaplin DJ, Edvardsen K, Trawick ML, Garner CM, Pinney KG.

J Nat Prod. 2008 Mar;71(3):313-20. doi: 10.1021/np070377j. Epub 2008 Feb 28.

PMID:
18303849
37.

The microtubule-targeting agent CA4P regresses leukemic xenografts by disrupting interaction with vascular cells and mitochondrial-dependent cell death.

Petit I, Karajannis MA, Vincent L, Young L, Butler J, Hooper AT, Shido K, Steller H, Chaplin DJ, Feldman E, Rafii S.

Blood. 2008 Feb 15;111(4):1951-61. Epub 2007 Nov 16.

38.

An update on the clinical development of drugs to disable tumor vasculature.

Siemann DW, Chaplin DJ.

Expert Opin Drug Discov. 2007 Oct;2(10):1357-67. doi: 10.1517/17460441.2.10.1357.

PMID:
23484531
39.

Current development status of small-molecule vascular disrupting agents.

Chaplin DJ, Horsman MR, Siemann DW.

Curr Opin Investig Drugs. 2006 Jun;7(6):522-8. Review.

PMID:
16784022
40.

Combretastatin A4 phosphate induces rapid regression of tumor neovessels and growth through interference with vascular endothelial-cadherin signaling.

Vincent L, Kermani P, Young LM, Cheng J, Zhang F, Shido K, Lam G, Bompais-Vincent H, Zhu Z, Hicklin DJ, Bohlen P, Chaplin DJ, May C, Rafii S.

J Clin Invest. 2005 Nov;115(11):2992-3006. Epub 2005 Oct 13.

41.

Combretastatin A4 phosphate: background and current clinical status.

Young SL, Chaplin DJ.

Expert Opin Investig Drugs. 2004 Sep;13(9):1171-82. Review.

PMID:
15330748
42.

Combretastatin family member OXI4503 induces tumor vascular collapse through the induction of endothelial apoptosis.

Sheng Y, Hua J, Pinney KG, Garner CM, Kane RR, Prezioso JA, Chaplin DJ, Edvardsen K.

Int J Cancer. 2004 Sep 10;111(4):604-10.

43.

Vascular-targeting therapies for treatment of malignant disease.

Siemann DW, Chaplin DJ, Horsman MR.

Cancer. 2004 Jun 15;100(12):2491-9. Review.

44.

Drug based approaches for targeting tumor vasculature: development of combretastatin A4 phosphate.

Chaplin DJ.

Pathophysiol Haemost Thromb. 2003;33 Suppl 1:9-10. No abstract available.

45.

Oxi4503, a novel vascular targeting agent: effects on blood flow and antitumor activity in comparison to combretastatin A-4 phosphate.

Hua J, Sheng Y, Pinney KG, Garner CM, Kane RR, Prezioso JA, Pettit GR, Chaplin DJ, Edvardsen K.

Anticancer Res. 2003 Mar-Apr;23(2B):1433-40.

PMID:
12820406
46.

The first international conference on vascular targeting: meeting overview.

Thorpe PE, Chaplin DJ, Blakey DC.

Cancer Res. 2003 Mar 1;63(5):1144-7.

47.

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.

48.

Selective induction of tumor ischemia: development of vascular targeting agents for cancer therapy.

Chaplin DJ, Hill SA.

Curr Opin Investig Drugs. 2002 Sep;3(9):1381-4. Review. No abstract available.

PMID:
12498016
49.

The development of combretastatin A4 phosphate as a vascular targeting agent.

Chaplin DJ, Hill SA.

Int J Radiat Oncol Biol Phys. 2002 Dec 1;54(5):1491-6.

PMID:
12459376
50.

Schedule dependence of combretastatin A4 phosphate in transplanted and spontaneous tumour models.

Hill SA, Chaplin DJ, Lewis G, Tozer GM.

Int J Cancer. 2002 Nov 1;102(1):70-4.

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