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Raymond P Baumann

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Articles 25
Citations 230
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Recent Articles
11.
Zhu R, Baumann R, Penketh P, Shyam K, Sartorelli A
J Med Chem . 2013 Jan; 56(3):1355-9. PMID: 23311288
O(6)-Alkylguanine-DNA alkyltransferase (AGT) is a DNA repair protein which removes alkyl groups from the O-6 position of guanine, thereby providing strong resistance to anticancer agents which alkylate this position. The...
12.
Zhu R, Seow H, Baumann R, Ishiguro K, Penketh P, Shyam K, et al.
Bioorg Med Chem Lett . 2012 Aug; 22(19):6242-7. PMID: 22932317
The efficacy of agents that alkylate the O-6 position of guanine is inhibited by O(6)-alkylguanine-DNA alkyltransferase (AGT) which removes these lesions from the tumor DNA. To increase differential toxicity, inhibitors...
13.
Patridge E, Eriksson E, Penketh P, Baumann R, Zhu R, Shyam K, et al.
Arch Toxicol . 2012 Jun; 86(10):1613-25. PMID: 22669514
Here, we report on 7-nitro-4-(phenylthio)benzofurazan (NBF-SPh), the most potent derivative among a set of patented anticancer 7-nitrobenzofurazans (NBFs), which have been suggested to function by perturbing protein-protein interactions. We demonstrate...
14.
Penketh P, Shyam K, Baumann R, Ishiguro K, Patridge E, Zhu R, et al.
Chem Biol Drug Des . 2012 May; 80(2):279-90. PMID: 22553921
Cellular resistance to chemotherapeutics that alkylate the O-6 position of guanine residues in DNA correlates with their O(6)-alkylguanine-DNA alkyltransferase activity. In normal cells high [O(6)-alkylguanine-DNA alkyltransferase] is beneficial, sparing the...
15.
Rockwell S, Liu Y, Seow H, Ishiguro K, Baumann R, Penketh P, et al.
Int J Radiat Biol . 2011 Nov; 88(3):277-85. PMID: 22111842
Purpose: These studies explored questions related to the potential use of Laromustine in the treatment of solid tumors and in combination with radiotherapy. Materials And Methods: The studies used mouse...
16.
Zhu R, Liu M, Luo M, Penketh P, Baumann R, Shyam K, et al.
J Med Chem . 2011 Sep; 54(21):7720-8. PMID: 21955333
A series of 4-nitrobenzyloxycarbonyl prodrug derivatives of O(6)-benzylguanine (O(6)-BG), conceived as prodrugs of O(6)-BG, an inhibitor of the resistance protein O(6)-alkylguanine-DNA alkyltransferase (AGT), were synthesized and evaluated for their ability...
17.
Penketh P, Baumann R, Shyam K, Williamson H, Ishiguro K, Zhu R, et al.
Chem Biol Drug Des . 2011 Jul; 78(4):513-26. PMID: 21777394
The anticancer prodrug 1,2-bis(methylsulfonyl)-1-(2-chloroethyl)-2-[[1-(4-nitrophenyl)ethoxy]carbonyl]hydrazine (KS119) selectively releases a short-lived cytotoxin following enzymatic reduction in hypoxic environments found in solid tumors. KS119, in addition to two enantiomers, has two stable atropisomers...
18.
Baumann R, Ishiguro K, Penketh P, Shyam K, Zhu R, Sartorelli A
Biochem Pharmacol . 2011 Mar; 81(10):1201-10. PMID: 21396917
To most effectively treat cancer it may be necessary to preferentially destroy tumor tissue while sparing normal tissues. One strategy to accomplish this is to selectively cripple the involved tumor...
19.
Ishiguro K, Zhu Y, Shyam K, Penketh P, Baumann R, Sartorelli A
Biochem Pharmacol . 2010 Jul; 80(9):1317-25. PMID: 20654586
O(6)-Alkylguanine-DNA alkyltransferase (AGT) mediates tumor resistance to alkylating agents that generate guanine O(6)-chloroethyl (Onrigin™ and carmustine) and O(6)-methyl (temozolomide) lesions; however, the relative efficiency of AGT protection against these lesions...
20.
Baumann R, Penketh P, Ishiguro K, Shyam K, Zhu Y, Sartorelli A
Biochem Pharmacol . 2009 Dec; 79(11):1553-61. PMID: 20005211
1,2-Bis(methylsulfonyl)-1-(2-chloroethyl)-2-[[1-(4-nitrophenyl)ethoxy]carbonyl]hydrazine (KS119) is a prodrug of the 1,2-bis(sulfonyl)hydrazine class of antineoplastic agents designed to exploit the oxygen-deficient regions of cancerous tissue. Thus, under reductive conditions in hypoxic cells this agent...