Phosphoramide mustard
WebSep 30, 2012 · It is very unstable and spontaneously decomposes into phosphoramide mustard by β-elimination of acrolein.[19,20,30,31] This conversion may be partly catalysed by albumin or other proteins.[32–34] Phosphoramide mustard is a bi-functional DNA alkylating agent and is considered to be the ultimate metabolite responsible for the … WebCyclophosphamide (CP) is a nitrogen mustard–containing prodrug that is inactive in the absence of metabolic activation that occurs via microsomal mixed function oxidases predominantly in the liver. 111 The activation of CP involves ring oxidation to 4-hydroxycyclophosphamide (4-OHCP), spontaneous and reversible ring opening to the …
Phosphoramide mustard
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WebJul 1, 2024 · Aldophosphamide spontaneously decomposes to the active alkylating metabolite, phosphoramide mustard, and the less active by-product acrolein. 1,3,8,10 Phosphoramide mustard has cytotoxic effects that are 4 to 10 times the cytoxic effects for 4-OHCP; however, phosphoramide mustard is highly reactive and intracellular, thereby … WebNov 9, 2012 · Cyclophosphamide is inactive until it undergoes hepatic transformation to form 4-hydroxycyclophosphamide, which then breaks down to form the ultimate alkylating agent, phosphoramide mustard. Sensitive and specific methods are now available for the measurement of cyclophosphamide, its metabolites and its stereoisomers in plasma and …
WebApr 18, 2006 · In contrast to 4-hydroxycyclophosphamide, phosphoramide mustard cannot enter target cells, and therefore only the intracellularly formed phosphoramide mustard fraction is considered to be cytotoxic. WebDec 19, 1995 · Phosphoramide mustard-induced DNA interstrand cross-links were studied both in vitro and by computer simulation. The local determinants for the formation of phosphoramide mustard-induced DNA interstrand cross-links were defined by using different pairs of synthetic oligonucleotide duplexes, each of which contained a single …
WebDec 12, 2024 · The synthesis of the phosphoramide mustards 1–3 are outlined in Scheme 1.Out first synthetic goal in the synthesis of 2-NIPAM, 3, was to produce the alkyne … WebNov 1, 1980 · Phosphoramide mustard, an active metabolite of cyclophosphamide, has been reacted separately with guanosine and deoxyguanosine in aqueous solution at pH 7.4. The major adduct which was formed in each case has been isolated by reverse-phase high-pressure liquid chromatography.
Webinvestigate if this novel 2-nitroimidazole phosphoramide nitrogen mustard (2-NIPAM) retained hypoxia selectivity and could be
WebJun 30, 2024 · A series of novel artemisinin-piperazine-phosphoramide mustard (PPM) hybrids were designed and synthesized by incorporating phosphoramide mustard (PM) into dihydroartemisinin (DHA) via an efficient, catalyst-free two-step sequential substitution. diabetic care technologyWebJan 14, 2024 · Phosphoramide mustard is the major metabolite for Cyclophosphamide (HY-17420), with anticancer activitiy. Phosphoramide mustard induces DNA adduct formation … cindy loo hoo picsWebAug 24, 2024 · In an effort to identify the factors affecting the reactivity of nitrogen mustards, we prepared two phosphoramide mustard derivatives in interaction with DNA. The activity of this drug was... diabetic care services eastlake ohdiabetic care services and pharmacyWebThis metabolite is only formed in cells that have low levels of ALDH. Phosphoramide mustard forms DNA crosslinks both between and within DNA strands at guanine N-7 positions (known as interstrand and intrastrand crosslinkages, respectively). This is irreversible and leads to cell death. cindy loo hoo picturesWebPhosphoramide mustard is the putative antineoplastic moiety and acrolein is the proximate toxic metabolite. There is wide interindividual variation in the metabolism of intravenously administered cyclophosphamide, which may contribute to the risk of SOS [125,126] . diabetic carers allowanceWebFeb 1, 2024 · Phosphoramide mustard-hemoglobin (PAM-Hb) The exposure of cyclophosphamide is determined via PAM-Hb, assessed from blood samples drawn after each course of each patient. An optimized and... diabetic care waukegan