ABG-SPS · Synthesis of natural product derived libraries employing enantioselective allylation on the polymeric support as key step
6РП — Действия „Мария Кюри“
- Период
- 2006-01-01 → 2006-09-30
- Финансиране от ЕС
- 113 426 €
- Участници
- 1
- Схема
- SCF
Линиите свързват координатора с партньорите. За проекти отпреди 2014 г. CORDIS не винаги дава точни координати. Тези точки са на ниво град или държава.
Накратко на български
Синтезират се библиотеки от химически съединения, подобни на природни вещества, като например производни на цитостатина. Тези структури помагат за откриването на нови лекарства и подобряват познанията за създаването на сложни молекули върху полимерни носители.
Кратко обяснение, генерирано от езиков модел по текста на CORDIS. Оригиналът е по-долу.
Цел на проекта
This proposal falls into the area of construction of diversity-oriented natural product-like libraries for chemical biology and drug discovery purposes. The synthesis of such libraries requires the availability of efficient and practical methods, including asymmetric transformations with high degree of stereoselectivity, for the multistep solid-phase synthesis of frameworks of biologically promising natural products. The objectives are:1) Solid-phase synthesis of 5- and 6-membered ring lactones (compounds c losely related to some biologically active natural products),2) solid-phase synthesis of a Cytostatin-derived compound library. Cytostatin is a natural product isolated from a Streptomyces strain that inhibits the serine/threonine phosphatase 2A at submicr omolar concentration,3) biological evaluation of the compound libraries in biochemical screens (in vitro inhibition assays) by me in close collaboration with specialised scientists in the field.Targets 1 and 2 will be achieved by means of an enantioselecti ve allylation or crotylation reaction of chiral polymer-supported aldehydes as the key step (which has no precedents to the date, only previous studies in Waldmann group but still unpublished), followed by a lactonization process. This presumably will lead to a library of 5- and 6-membered ring lactones with a side chain in the ring. The points of generation of molecular diversity will be: modification in the size and variation in the substitution pattern of the lactone ring. Concerning the side chain, it w ill be modified mainly by using the alkene reactivity.The main aim is to increase the knowledge and interest of the scientific community in the use of asymmetric strategies in solid-phase synthesis and drug discovery. In addition, I expect to acquire new s kills and expertise in chemical biology to complement my research background.
Оригинален текст от CORDIS (на английски).
Участници
- MAX PLANCK INSTITUTE FUER MOLEKULARE PHYSIOLOGIE · DORTMUNDКоординаторНиво градГермания
Връзки
Данни: CORDIS, © Европейски съюз