An article Derivatisation of parthenolide to address chemoresistant chronic lymphocytic leukaemia WOS:000481437100010 published article about NF-KAPPA-B; WATER-SOLUBLE PARTHENOLIDE; SESQUITERPENE LACTONE; IN-VITRO; AMINO-DERIVATIVES; BIOLOGICAL EVALUATION; ANTICANCER AGENTS; CRYSTAL-STRUCTURE; CANCER CELLS; FEVERFEW in [Li, Xingjian; Payne, Daniel T.; Dutton, Mark J.; Quy, Alex S.; Fossey, John S.] Univ Birmingham, Sch Chem, Birmingham B15 2TT, W Midlands, England; [Ampolu, Badarinath; Bland, Nicholas; Brown, Jane T.; Hamza, Daniel; Jones, Geraint; Lane, Rebecca; Merisor, Elena G.; Schulz-Utermoehl, Timothy; Stevenson, Brett] BioCity, Sygnat Discovery, Discovery Bldg,Pennyfoot St, Nottingham NG1 1GR, England; [Fitton, Catherine A.; Scarll, Rosanna; Stankovic, Tatjana; Agathanggelou, Angelo] Univ Birmingham, Inst Canc & Genom Sci, Birmingham B15 2TT, W Midlands, England; [Gulliver, Abigail; Hale, Lee] Univ Birmingham, Winterbourne Bot Garden, 58 Edgbaston Pk Rd, Birmingham B15 2RT, W Midlands, England; [Leach, Andrew G.] Liverpool John Moores Univ, Sch Pharm & Biomol Sci, Byrom St, Liverpool L3 3AF, Merseyside, England; [Male, Louise] Univ Birmingham, Sch Chem, Xray Crystallog Facil, Birmingham B15 2TT, W Midlands, England; [Morton, Michael J.; Roberts, Ruth] ApconiX Ltd, Alderly Pk, Nether Alderly SK10 4TG, Cheshire, England; [Roberts, Ruth] Univ Birmingham, Sch Biosci, Birmingham B15 2TT, W Midlands, England in 2019, Cited 143. The Name is 1,4-Dioxa-8-azaspiro[4.5]decane. Through research, I have a further understanding and discovery of 177-11-7. Recommanded Product: 177-11-7
Parthenolide is a natural product that exhibits anti-leukaemic activity, however, its clinical use is limited by its poor bioavailability. It may be extracted from feverfew and protocols for growing, extracting and derivatising it are reported. A novel parthenolide derivative with good bioavailability and pharmacological properties was identified through a screening cascade based on in vitro anti-leukaemic activity and calculated drug-likeness properties, in vitro and in vivo pharmacokinetics studies and hERG liability testing. In vitro studies showed the most promising derivative to have comparable anti-leukaemic activity to DMAPT, a previously described parthenolide derivative. The newly identified compound was shown to have pro-oxidant activity and in silico molecular docking studies indicate a prodrug mode of action. A synthesis scheme is presented for the production of amine 7 used in the generation of 5f.
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