189341-51-3Relevant academic research and scientific papers
SYNTHESIS AND GROWTH REGULATORY ACTIVITY OF A PROTOTYPE MEMBER OF A NEW FAMILY OF AMlNOTHIOL RADIOPROTECTORS
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Paragraph 0019, (2014/05/07)
The synthesis, growth inhibition and radioprotective activity of the PrC-210 aminothiol, 3-(methyl-amino)-2-((methylamino)methyl)propane-1-thiol, and its polyamine and thiolated polyamine progenitors are reported. All of the molecules significantly inhibi
Synthesis and growth regulatory activity of a prototype member of a new family of aminothiol radioprotectors
Copp, Richard R.,Peebles, Daniel D.,Fahl, William E.
scheme or table, p. 7426 - 7430 (2012/02/13)
The synthesis, growth inhibition and radioprotective activity of the PrC-210 aminothiol, 3-(methylamino)-2-((methylamino)methyl)propane-1-thiol, and its polyamine and thiolated polyamine progenitors are reported. All of the molecules significantly inhibit
Synthesis and evaluation of unsymmetrical polyamine derivatives as antitumor agents
Wang, Jianhong,Xie, Songqiang,Li, Yanjie,Guo, Yongjun,Ma, Yuanfang,Zhao, Jin,Phanstiel IV, Otto,Wang, Chaojie
, p. 7005 - 7012 (2008/12/22)
A series of unsymmetrically substituted polyamine derivatives were prepared and their cytotoxicities in mouse leukemia L1210, melanoma B16, and HeLa cells were investigated. The in vitro cytotoxicity revealed that these conjugates could recognize the poly
AMINO THIOL COMPOUNDS AND COMPOSITIONS FOR USE IN CONJUNCTION WITH CANCER THERAPY
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Page/Page column 57, (2010/02/10)
The invention provides novel polyamine and amino thiol compounds and pharmaceutical compositions for administration in conjunction with cancer chemotherapy or radiation therapy. The compounds are administered locally to provide protection against the adve
Cycloalkyl substituted polyamines for cancer therapy and methods of synthesis therefor
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Page/Page column 11, (2010/01/31)
Conformationally restricted polyamine compounds useful in treatment of cancer and other diseases marked by abnormal cell proliferation are disclosed. Improved methods of synthesizing such compounds are also disclosed. In one method of the invention, a carbene-bearing or carbene equivalent-bearing compound is reacted with the double bond of an alkene compound to form a cyclopropyl ring as the first step in the synthesis.
Cis-unsaturated analogues of 3,8,13,18,23-pentaazapentacosane (BE-4-4-4-4): Synthesis add growth inhibitory effects on human prostate cancer cell lines
Reddy,Sarkar,Valasinas,Marton,Basu,Frydman
, p. 404 - 417 (2007/10/03)
From the results of our previous physicochemical studies of polyamine - Nucleic acid interactions, we concluded that polyamine analogues in cisoidal conformation are capable of wrapping around the major groove of the double helix, of displacing natural po
A comparison of structure-activity relationships between spermidine and spermine analogue antineoplastics
Bergeron, Raymond J.,Feng, Yang,Weimar, William R.,McManis, James S.,Dimova, Hristina,Porter, Carl,Raisler, Brian,Phanstiel, Otto
, p. 1475 - 1494 (2007/10/03)
A systematic investigation of the impact of spermidine analogues both in vitro and in vivo is described. The study characterizes the effects of these analogues on L1210 cell growth, polyamine pools, ornithine decarboxylase, S- adenosyl-L-methionine decarboxylase, spermidine/spermine N1- acetyltransferase, the maintenance of cellular charge, i.e., cationic equivalence associated with the polyamines and their analogues, and compares their ability to compete with spermidine for transport. The findings clearly demonstrate that the activity of the linear polyamine analogues is highly dependent on the length of the triamines and the size of the N(α),N(ω)- substituents. It appears that there is an optimum chain length for various activities and that the larger the N(α)N(ω)-alkyls, the less active the compound. Metabolic transformation including N-dealkylation of these compounds is also evaluated. While there is no monotonic relationship between chain length and the ability of the analogue to be metabolized, the dipropyl triamines are clearly more actively catabolized than the corresponding methyl and ethyl systems. A comparison of the triamines with the corresponding tetraamines is made throughout the text regarding both in vitro activity against L1210 cells and in vivo toxicity measurements, suggesting that several triamine analogues may offer therapeutic advantages over the corresponding tetraamines.
