479630-08-5Relevant articles and documents
Derivatisation of parthenolide to address chemoresistant chronic lymphocytic leukaemia
Li, Xingjian,Payne, Daniel T.,Ampolu, Badarinath,Bland, Nicholas,Brown, Jane T.,Dutton, Mark J.,Fitton, Catherine A.,Gulliver, Abigail,Hale, Lee,Hamza, Daniel,Jones, Geraint,Lane, Rebecca,Leach, Andrew G.,Male, Louise,Merisor, Elena G.,Morton, Michael J.,Quy, Alex S.,Roberts, Ruth,Scarll, Rosanna,Schulz-Utermoehl, Timothy,Stankovic, Tatjana,Stevenson, Brett,Fossey, John S.,Agathanggelou, Angelo
, p. 1379 - 1390 (2019)
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.
Reformatsky and Blaise reactions in flow as a tool for drug discovery. One pot diversity oriented synthesis of valuable intermediates and heterocycles
Huck,Berton,De La Hoz,Díaz-Ortiz,Alcázar
supporting information, p. 1420 - 1424 (2017/05/12)
The application of Reformatsky and Blaise reactions for the preparation of a diverse set of valuable intermediates and heterocycles in a one-pot protocol is described. To achieve this goal, a greener activation protocol for zinc in flow conditions has been developed to introduce this metal efficiently into α-bromoacetates. The organozinc compounds were added to a diverse set of ketones and nitriles to obtain a wide range of functional groups and heterocyclic systems.
Compounds and methods for treating cancer by inhibiting the urokinase receptor
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Page/Page column 53; 54; 57, (2017/09/15)
Compounds and methods for treating or preventing cancer associated with binding to the urokinase receptor are provided. Biological processes affected by the compounds include cell migration, cell growth, cell adhesion, angiogenesis, cancer cell invasion, apoptosis, tumor formation, tumor progression, metastasis, degradation of the extracellular matrix, pericellular proteolysis, activation of plasminogen, changes in the levels of an extracellular protease, and changes in the levels of a VEGF receptor.
