Bronwyn G Siim
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Explore the profile of Bronwyn G Siim including associated specialties, affiliations and a list of published articles.
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13
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394
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Recent Articles
1.
Tanpure R, Nguyen B, Strecker T, Aguirre S, Sharma S, Chaplin D, et al.
J Nat Prod
. 2011 Jul;
74(7):1568-74.
PMID: 21718055
The natural products combretastatin A-4 (CA4) and combretastatin A-1 (CA1) are potent cancer vascular disrupting agents and inhibitors of tubulin assembly (IC₅₀ = 1-2 μM). The phosphorylated prodrugs CA4P and...
2.
Kishore Kumar G, Chavarria G, Charlton-Sevcik A, Yoo G, Song J, Strecker T, et al.
Bioorg Med Chem Lett
. 2010 Oct;
20(22):6610-5.
PMID: 20933415
A series of thiosemicarbazone analogs based on the benzophenone, thiophene, pyridine, and fluorene molecular frameworks has been prepared by chemical synthesis and evaluated as small-molecule inhibitors of the cysteine proteases...
3.
Hicks K, Siim B, Jaiswal J, Pruijn F, Fraser A, Patel R, et al.
Clin Cancer Res
. 2010 Aug;
16(20):4946-57.
PMID: 20732963
Purpose: Tirapazamine (TPZ) has attractive features for targeting hypoxic cells in tumors but has limited clinical activity, in part because of poor extravascular penetration. Here, we identify improved TPZ analogues...
4.
Regio- and stereospecific synthesis of mono-beta-d-glucuronic acid derivatives of combretastatin A-1
Tanpure R, Strecker T, Chaplin D, Siim B, Trawick M, Pinney K
J Nat Prod
. 2010 May;
73(6):1093-101.
PMID: 20496923
Synthetic routes have been established for the preparation of regio- and stereoisomerically pure samples of the mono-beta-d-glucuronic acid derivatives of combretastatin A-1, referred to as CA1G1 (5a) and CA1G2 (6a)....
5.
Kishore Kumar G, Chavarria G, Charlton-Sevcik A, Arispe W, MacDonough M, Strecker T, et al.
Bioorg Med Chem Lett
. 2010 Jan;
20(4):1415-9.
PMID: 20089402
A small library of 36 functionalized benzophenone thiosemicarbazone analogs has been prepared by chemical synthesis and evaluated for their ability to inhibit the cysteine proteases cathepsin L and cathepsin B....
6.
Hay M, Pchalek K, Pruijn F, Hicks K, Siim B, Anderson R, et al.
J Med Chem
. 2007 Dec;
50(26):6654-64.
PMID: 18052317
Tirapazamine (TPZ) and related 1,2,4-benzotriazine 1,4 dioxides (BTOs) are selectively toxic under hypoxia, but their ability to kill hypoxic cells in tumors is generally limited by their poor extravascular transport....
7.
Hay M, Hicks K, Pruijn F, Pchalek K, Siim B, Wilson W, et al.
J Med Chem
. 2007 Nov;
50(25):6392-404.
PMID: 18001018
Pharmacokinetic/pharmacodynamic (PK/PD) modeling has shown the antitumor activity of tirapazamine (TPZ), a bioreductive hypoxia-selective cytotoxin, to be limited by poor penetration through hypoxic tumor tissue. We have prepared a series...
8.
Hicks K, Myint H, Patterson A, Pruijn F, Siim B, Patel K, et al.
Int J Radiat Oncol Biol Phys
. 2007 Sep;
69(2):560-71.
PMID: 17869669
Purpose: To compare oxygen dependence and tissue transport properties of a new hypoxia-activated prodrug, PR-104A, with tirapazamine, and to evaluate the implications for antitumor activity when combined with radiotherapy. Methods...
9.
Hicks K, Siim B, Pruijn F, Wilson W
Radiat Res
. 2004 May;
161(6):656-66.
PMID: 15161354
The hypoxic cytotoxin tirapazamine (TPZ) is currently in phase III clinical trial and appears to have clinical activity. One hypothesis as to why TPZ has been used more successfully in...
10.
Siim B, Pruijn F, Sturman J, Hogg A, Hay M, Brown J, et al.
Cancer Res
. 2004 Jan;
64(2):736-42.
PMID: 14744792
Tirapazamine (TPZ), a bioreductive drug with selective toxicity for hypoxic cells in tumors, is currently in Phase III clinical trials. It has been suggested to have a dual mechanism of...