Alpha 2.0
Login Register
» Authors » Raymond P Baumann

Raymond P Baumann

Explore the profile of Raymond P Baumann including associated specialties, affiliations and a list of published articles. Areas
Snapshot
Articles 25
Citations 230
Followers 0
Related Specialties
Biochemistry
Pharmacology
Toxicology
Top 10 Co-Authors
Philip G Penketh
Krishnamurthy Shyam
Alan C Sartorelli
Kimiko Ishiguro
Rui Zhu
Helen A Seow
Elena S Ratner
Yong-Lian Zhu
Thomas J Rutherford
Z Ping Lin
Published In
Biochem Pharmacol
Chem Biol Drug Des
J Med Chem
Chem Res Toxicol
Bioorg Med Chem Lett
Affiliations
Soon will be listed here.
Recent Articles
1.
Design Strategy for the EPR Tumor-Targeting of 1,2-Bis(sulfonyl)-1-alkylhydrazines
Penketh P, Williamson H, Baumann R, Shyam K
Molecules . 2021 Jan; 26(2). PMID: 33419160
A design strategy for macromolecular prodrugs is described, that are expected to exhibit robust activity against most solid tumor types while resulting in minimal toxicities to normal tissues. This approach...
2.
pH-dependent general base catalyzed activation rather than isocyanate liberation may explain the superior anticancer efficacy of laromustine compared to related 1,2-bis(methylsulfonyl)-1-(2-chloroethyl)hydrazine prodrugs
Penketh P, Finch R, Sauro R, Baumann R, Ratner E, Shyam K
Chem Biol Drug Des . 2017 Jun; 91(1):62-74. PMID: 28636806
Laromustine (also known as cloretazine, onrigin, VNP40101M, 101M) is a prodrug of 90CE, a short-lived chloroethylating agent with anticancer activity. The short half-life of 90CE necessitates the use of latentiated...
3.
When alcohol is the answer: Trapping, identifying and quantifying simple alkylating species in aqueous environments
Penketh P, Shyam K, Baumann R, Zhu R, Ishiguro K, Sartorelli A, et al.
Anal Biochem . 2016 May; 508:34-7. PMID: 27188264
Alkylating agents are a significant class of environmental carcinogens as well as commonly used anticancer therapeutics. Traditional alkylating activity assays have utilized the colorimetric reagent 4-(4-nitrobenzyl)pyridine (4NBP). However, 4NBP based...
4.
Cataloging antineoplastic agents according to their effectiveness against platinum-resistant and platinum-sensitive ovarian carcinoma cell lines
Ishiguro K, Zhu Y, Lin Z, Penketh P, Shyam K, Zhu R, et al.
J Transl Sci . 2016 Apr; 2(2):117-124. PMID: 27076919
Although epithelial ovarian cancers (EOCs) are initially treated with platinum-based chemotherapy, EOCs vary in platinum responsiveness. Cataloging antineoplastic agents according to their effectiveness against platinum-resistant and platinum-sensitive EOC cell lines...
5.
Antitumor sulfonylhydrazines: design, structure-activity relationships, resistance mechanisms, and strategies for improving therapeutic utility
Shyam K, Penketh P, Baumann R, Finch R, Zhu R, Zhu Y, et al.
J Med Chem . 2015 Jan; 58(9):3639-71. PMID: 25612194
1,2-Bis(sulfonyl)-1-alkylhydrazines (BSHs) were conceived as more specific DNA guanine O-6 methylating and chloroethylating agents lacking many of the undesirable toxicophores contained in antitumor nitrosoureas. O(6)-Alkylguanine-DNA alkyltransferase (MGMT) is the sole...
6.
Distinct mechanisms of cell-kill by triapine and its terminally dimethylated derivative Dp44mT due to a loss or gain of activity of their copper(II) complexes
Ishiguro K, Lin Z, Penketh P, Shyam K, Zhu R, Baumann R, et al.
Biochem Pharmacol . 2014 Aug; 91(3):312-22. PMID: 25130544
Triapine, currently being evaluated as an antitumor agent in phase II clinical trials, and its terminally dimethylated derivative Dp44mT share the α-pyridyl thiosemicarbazone backbone that functions as ligands for transition...
7.
Influence of glutathione and glutathione S-transferases on DNA interstrand cross-link formation by 1,2-bis(methylsulfonyl)-1-(2-chloroethyl)hydrazine, the active anticancer moiety generated by laromustine
Penketh P, Patridge E, Shyam K, Baumann R, Zhu R, Ishiguro K, et al.
Chem Res Toxicol . 2014 Jul; 27(8):1440-9. PMID: 25012050
Prodrugs of 1,2-bis(methylsulfonyl)-1-(2-chloroethyl)hydrazine (90CE) are promising anticancer agents. The 90CE moiety is a readily latentiated, short-lived (t1/2 ∼ 30 s) chloroethylating agent that can generate high yields of oxophilic electrophiles...
8.
Influence of phosphate and phosphoesters on the decomposition pathway of 1,2-bis(methylsulfonyl)-1-(2-chloroethyhydrazine (90CE), the active anticancer moiety generated by Laromustine, KS119, and KS119W
Penketh P, Shyam K, Zhu R, Baumann R, Ishiguro K, Sartorelli A
Chem Res Toxicol . 2014 Mar; 27(5):818-33. PMID: 24618018
Prodrugs of the short-lived chloroethylating agent 1,2-bis(methylsulfonyl)-1-(2-chloroethyl)hydrazine (90CE) and its methylating analogue 1,2-bis(methylsulfonyl)-1-(methyl)hydrazine (KS90) are potentially useful anticancer agents. This class of agents frequently yields higher ratios of therapeutically active...
9.
Expression of -Methylguanine-DNA Methyltransferase Examined by Alkyl-Transfer Assays, Methylation-Specific PCR and Western Blots in Tumors and Matched Normal Tissue
Ishiguro K, Shyam K, Penketh P, Baumann R, Sartorelli A, Rutherford T, et al.
J Cancer Ther . 2013 Aug; 4(4):919-931. PMID: 23946891
The tumor selectivity of alkylating agents that produce guanine -chloroethyl (laromustine and carmustine) and -methyl (temozolomide) lesions, depends upon -methylguanine-DNA methyltransferase (MGMT) activity being lower in tumor than in host...
10.
Chloroethylating and methylating dual function antineoplastic agents display superior cytotoxicity against repair proficient tumor cells
Zhu R, Baumann R, Patridge E, Penketh P, Shyam K, Ishiguro K, et al.
Bioorg Med Chem Lett . 2013 Feb; 23(6):1853-9. PMID: 23395657
Two new agents based upon the structure of the clinically active prodrug laromustine were synthesized. These agents, 2-(2-chloroethyl)-N-methyl-1,2-bis(methylsulfonyl)-N-nitrosohydrazinecarboxamide (1) and N-(2-chloroethyl)-2-methyl-1,2-bis(methylsulfonyl)-N-nitrosohydrazinecarboxamide (2), were designed to retain the potent chloroethylating and...