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Chemical library in place

A focus on the NF- k B signaling cascade. Identify inhibitors of NF- k B activation. In collaboration with Prof . Ron Hay FRS Life Sciences Dundee. arthritis, sceptic shock, inflammatory bowel disease. Chemical library in place. Inhibitors already known. chemical tool.

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Chemical library in place

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  1. A focus on the NF-kB signaling cascade Identify inhibitors of NF-kB activation In collaboration with Prof. Ron Hay FRS Life Sciences Dundee arthritis, sceptic shock, inflammatory bowel disease Chemical library in place Inhibitors already known... chemical tool Robust HT screen Hit Identification Chemical and biological validation Used to study biological processes Potential therapeutic Bremner and Heinrich, 2002, J. Pharmacy and Pharmacol., 54, 453-46 72

  2. A focus on the NF-kB signaling cascade Natural Product collection from Professor Alan Harvey, SIDR University of Strathclyde Identify inhibitors of NF-kB activation Chemical library in place Robust HT screen Hit Identification Chemical and biological validation Used to study biological processes NF-kB Potential therapeutic Luc Luciferase based Reporter gene assay Raquel Frade, Ron Hay Nick Westwood

  3. A focus on the NF-kB signaling cascade Natural Product collection from Professor Alan Harvey, SIDR University of Strathclyde Identify inhibitors of NF-kB activation Tanacetum parthenium extract purification Raquel Frade Chemical library in place Robust HT screen Hit Identification structure assignment Dr Tomas Lebl Chemical and biological validation Luciferase based reporter gene assay Raquel Frade, Prof Ron Hay FRS Nick Westwood Used to study biological processes Potential therapeutic

  4. A sesquiterpene lactone? solvent

  5. Assignment of the structure of the major component in the purified bioactive extract MS : 279 [M + H]+ Tomas Lebl

  6. R = b-OAc (S), R1 = H R = a-OAc (R), R1 = H R = b-OMe (S), R1 = H R = a-OMe (R), R1 = H R = b-OH (S), R1 = OH R = a-OH (S), R1 = OH R = b-OAc (S), R1 = OH R = a-OAc(S), R1 = OH Structurally related compounds R = b-OH (S), R1 = H iso-secotanapartholide From Artemisia rutifolia no report of a-OH isomer Zdero, Bohlmann et al., 1986, Phytochem., 25, 883-889; Jia et al., 1991, Phytochem., 30, 3033-3035; Oksuz, 1990, Phytochem., 29, 887-890; Toth et al., 2003, Tet., 59, 3729-3735.

  7. Structurally related compounds R = b-OAc (S), R1 = H R = a-OAc (R), R1 = H R = b-OMe (S), R1 = H R = a-OMe (R), R1 = H R = b-OH (S), R1 = OH R = a-OH (S), R1 = OH R = b-OAc (S), R1 = OH R = a-OAc(S), R1 = OH R = b-OH (S), R1 = H iso-secotanapartholide secotanapartholides Knight et al., 1996, J.Chem.Soc., Perkin Trans. 1, 1979-1986 and references therein.

  8. A focus on the NF-kB signaling cascade Identify inhibitors of NF-kB activation Synthesis of authentic material to clarify stereochemistry issues at C3 Chemical library in place Robust HT screen Hit Identification Chemical and biological validation Used to study biological processes Potential therapeutic Edward Makiyi, Susan Cobb

  9. Proposed biosynthesis of the secotanapartholides and b-isomer and b-isomer Bohlmann and Zdero, 1982, Phytochem., 21, 2543-2549; Knight et al., 1996, J.Chem.Soc., Perkin Trans. 1, 1979-1986; Rucker et al., 1992, Planta Med., 58, 293.

  10. Proposed biosynthesis of secotanapartholide Bohlmann and Zdero, 1982, Phytochem., 21, 2543-2549; Knight et al., 1996, J.Chem.Soc., Perkin Trans. 1, 1979-1986; Rucker et al., 1992, Planta Med., 58, 293.

  11. A biomimetic approach to iso-secotanapartholides? Artabsin Geissman and Winters, 1968, Tet. Lett., 27, 3145-3147.

  12. A biomimetic approach to iso-secotanapartholides? Ji et al., 1991, Phytochem., 30, 583-587.

  13. An alternative semi-synthesis approach late stage oxidative cleavage with no protecting groups

  14. Synthesis of diastereomeric diols Buchi et al., 1966,J. Am. Chem. Soc., 88, 3403-3408. Prof. Alex Slawin

  15. ... and then diastereomeric triols Prof. Alex Slawin

  16. ... and then diastereomeric triols

  17. Synthesis of 3b-OH-iso-secotanapartholide Greico et al., 1974, J.Org.Chem., 39, 119-120

  18. Synthesis of epi-3a-iso-secotanapartholide .. and then for the comparison with the natural material Thanks to Professors Todorova, Marco, Lee, Ryu and Saliba Does anyone have any seco-tanapartholide?

  19. A comparison of iso-secotanapartholides with our isolated natural material 500MHz, CD3CN synthetic epi-3a-OH 3b-OH Natural source

  20. A focus on the NF-kB signaling cascade Identify key biological process Chemical library in place and 3b-isomer Robust HT screen Hit Identification Chemical and biological validation Used to study biological processes NF-kB Potential therapeutic Luc

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