Recently I am researching about NF-KAPPA-B; WATER-SOLUBLE PARTHENOLIDE; SESQUITERPENE LACTONE; IN-VITRO; AMINO-DERIVATIVES; BIOLOGICAL EVALUATION; ANTICANCER AGENTS; CRYSTAL-STRUCTURE; CANCER CELLS; FEVERFEW, Saw an article supported by the MRCUK Research & Innovation (UKRI)Medical Research Council UK (MRC) [14/15]; EPSRCUK Research & Innovation (UKRI)Engineering & Physical Sciences Research Council (EPSRC) [ISF 2012, EP/J003220/1]; University of Birmingham; ERDF AWM II; School of Chemistry; Royal Society Industry Fellowship schemeRoyal Society of London [2012/R1]; Bloodwise [14031]; Liverpool John Moores University. Published in ROYAL SOC CHEMISTRY in CAMBRIDGE ,Authors: Li, XJ; Payne, DT; Ampolu, B; Bland, N; Brown, JT; Dutton, MJ; Fitton, CA; Gulliver, A; Hale, L; Hamza, D; Jones, G; Lane, R; Leach, AG; Male, L; Merisor, EG; Morton, MJ; Quy, AS; Roberts, R; Scarll, R; Schulz-Utermoehl, T; Stankovic, T; Stevenson, B; Fossey, JS; Agathanggelou, A. The CAS is 177-11-7. Through research, I have a further understanding and discovery of 1,4-Dioxa-8-azaspiro[4.5]decane. HPLC of Formula: C7H13NO2
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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Reference:
Piperidine – Wikipedia,
Piperidine | C5H7510N – PubChem