6943-87-9Relevant articles and documents
Sulfonyl-containing aldophosphamide analogues as novel anticancer prodrugs targeted against cyclophosphamide-resistant tumor cell lines
Jain, Monish,Fan, Junying,Baturay, Nesrine Z.,Kwon, Chul-Hoon
, p. 3843 - 3852 (2007/10/03)
A series of sulfonyl-group containing analogues of aldophosphamide (Aldo) were synthesized as potential anticancer prodrugs that liberate the cytotoxic phosphoramide mustards (PM, IPM, and tetrakis-PM) via β-elimination, a nonenzymatic activation mechanism. Kinetic studies demonstrated that all these compounds spontaneously liberate phosphoramide mustards with half-lives in the range of 0.08-15.2 h under model physiological conditions in 0.08 M phosphate buffer at pH 7.4 and 37 °C. Analogous to Aldo, the rates of β-elimination in all compounds was enhanced in reconstituted human plasma under same conditions. The compounds were more potent than the corresponding phosphoramide mustards against V-79 Chinese hamster lung fibroblasts in vitro (IC50 = 1.8-69.1 μM). Several compounds showed excellent in vivo antitumor activity in CD2F1 mice against both P388/0 (Wild) and P388/CPA (CP-resistant) tumor cell lines.
2-iminobenzothiazoline derivatives, their preparation and pharmaceutical compositions containing them
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, (2008/06/13)
Compounds of the formula: STR1 in which - R1 denotes a polyfluoroalkoxy or polyfluoroalkyl radical, and - R2 denotes either a chain --CH2 --(CH(R4))n --R3, in which R3 denotes a dialkylamino, piperidino, 1-pyrrolidinyl, mercapto, acylthio, alkylthio, alkylsulphinyl or alkylsulphonyl radical, R4 denotes a hydrogen atom or an alkyl radical and n is equal to 0 or 1, or a residue of formula: STR2 the said alkyl and alkoxy radicals and portions containing 1 to 4 carbon atoms each in a straight or branched chain and said the acyl portions containing 2 to 4 carbon atoms each, and the salts of these compounds, are useful in the treatment of diseases in which glutamate is implicated.
Metallorganische Verbindungen aus Epoxiden
Bartmann, Ekkehard
, p. 629 - 631 (2007/10/02)
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