Phosphoramide mustard
WebDescription: Phosphoramide mustard (PMC) is an alkylating agent and active metabolite of cyclophosphamide. It is formed from cyclophosphamide via the ring-opened tautomer of the cytochrome P450 (CYP) isoform-formed intermediate 4-hydroxycyclophosphamide. WebPhosphoramide mustard is a biologically active metabolite of Cyclophosphamide (HY-17420), with anticancer activitiy. Phosphoramide mustard induces DNA damage. For …
Phosphoramide mustard
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WebJul 18, 2024 · Cyclophosphamide (CPA) represents a widely used anti-cancer prodrug that is converted by liver cytochrome P450 (CYP) enzymes into the primary metabolite 4-hydroxycyclophosphamide (4-OH-CPA), followed by non-enzymatic generation of the bioactive metabolites phosphoramide mustard and acrolein. The use of human drug … WebPhosphoramide mustard prevents cell division by forming cross-linkages in DNA both between and within DNA strands at guanine N-7 positions. This is irreversible and leads to …
WebJun 15, 2016 · Both the chemical stability of the conjugates and the release of phosphoramide mustard from the conjugates upon proteolysis were impacted by the self … WebSep 16, 2024 · Phosphoramide mustard (PM) is the final cytotoxic metabolite formed from the parent compound cyclophosphamide through a complex metabolic pathway, primarily through hepatic metabolism.
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 … 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.
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 …
WebJun 30, 2024 · Abstract. A series of novel artemisinin-piperazine-phosphoramide mustard (PPM) hybrids were designed and synthesized by incorporating phosphoramide mustard … tru fit hill lokahndwalaWebDec 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 … philip levine poetryWebNov 1, 1993 · The Partitioning of Phosphoramide Mustard and Its Aziridinium Ions among Alkylation and P−N Bond Hydrolysis Reactions. Journal of Medicinal Chemistry 1998, 41 … trufit howellWebDec 19, 1995 · The local determinants for the formation of phosphoramide mustard-induced DNA interstrand cross-links were defined by using different pairs of synthetic … tru fit gym weslaco txWebAug 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... trufitgym new bern addressWebThis 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. tru fit health and supplementsWebPhosphoramide mustard C4H11Cl2N2O2P CID 96356 - structure, chemical names, physical and chemical properties, classification, patents, literature, biological activities, safety/hazards/toxicity information, … philip levine the two