- Synthesis and evaluation of macrocyclic diarylether heptanoid natural products and their analogs
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The macrocyclic diarylether heptanoid (MDEH) natural products have been used in folk medicine for centuries. MDEHs are reported to exert anti-tumor properties by inhibiting the activation of NF-κB. Here we report the synthesis of a small MDEH library (first reported synthesis of racemic platycarynol) using a Grubbs cross metathesis/Ullmann cyclization strategy. Evaluation of the library led to the identification of MDEH 9b which sensitizes pancreatic cancer cells to gemcitabine mediated growth inhibition and apoptosis.
- Bryant, Vashti C.,Kishore Kumar,Nyong, Abijah M.,Natarajan, Amarnath
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supporting information; experimental part
p. 245 - 248
(2012/03/10)
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- SUBSTITUTED ARYLALKANOIC ACID DERIVATIVE AND USE THEREOF
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A compound represented by the formula (I)[In the formula, Link represents a saturated or unsaturated straight hydrocarbon chain having 1 to 3 carbon atoms, C2 to C6 in the aromatic ring (E) independently represent a ring-constituting carbon atom, one of the ring-constituting carbon atoms may be replaced with V, V represents nitrogen atom, or carbon atom substituted with Zx, Zx represents a saturated alkyl group having 1 to 4 carbon atoms and the like, Rs represents -D-Rx etc., D represents a single bond, oxygen atom and the like, Rx represents a saturated alkyl group having 3 to 8 carbon atoms and the like, AR represents a partially unsaturated or completely unsaturated condensed bicyclic carbon ring or a heterocyclic ring, and Y represents hydrogen atom, a lower alkyl group having 1 to 4 carbon atoms and the like] or a salt thereof. A compound having prostaglandin production-suppressing action and leukotriene production-suppressing action is provided.
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Page/Page column 412-413
(2008/06/13)
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- INDENONCARBOXYLIC ACIDS DERIVATIVES AND THEIR USE FOR THE TREATMENT OF AND PREVENTING DIABETES AND DYSLIPIDAEMIA
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The present invention relates to a compound of the formula ((I): in which: n is an integer chosen from 1, 2 and 3; Y represents O; N-OR9, in which R9represents H or a saturated hydrocarbon-based aliphatic group; CR10R
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- Substituted phenylalkanoic acid derivatives and use thereof
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A compound represented by the formula (I) or a salt thereof: wherein n represents an integer of 1 to 3, R represents an alkyl group having 3 to 8 carbon atoms, a group represented by the following formula: R1(CH2)k— (wherein k represents 0 or an integer of 1 to 3; R1 represents a saturated cyclic alkyl group having 3 to 7 carbon atoms or a saturated condensed cyclic alkyl group having 6 to 8 carbon atoms, and the group R1 may be substituted with a lower alkyl group having 1 to 4 carbon atoms) and the like, and Ar represents a condensed bicyclic group such as naphthalen-1-yl group, which has suppressing action on prostaglandin and leukotriene production and is useful for prophylactic and/or therapeutic treatment of various inflammatory diseases and the like caused by these lipid mediators.
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- Regioselective intramolecular oxidation of phenols and anisoles by dioxiranes generated in situ
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A novel method for regioselective oxidation of phenols and anisoles has been developed in which dioxiranes, generated in situ from ketones and Ozone, oxidize phenol derivatives in an intramolecular fashion. A series of ketones with electron-withdrawing groups, such as CF3, COOMe, and CH2Cl, were attached to phenols, anisoles, or aryl rings via a C2 or C3 methylene linker. In a homogeneous solvent system of CH3CN and H2O, oxidation of phenol derivatives 1-10 afforded spiro 2-hydroxydienones in 24-55% yields regardless of the presence of other substituents (ortho Me, meta Me or Br) on the aryl ring and the length of the linker. Experimental evidences were provided to support the mechanism that involves a regioselective π bond epoxidation of aryl rings followed by epoxide rearrangement and hemiketal formation.
- Yang, Dan,Wong, Man-Kin,Yan, Zheng
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p. 4179 - 4184
(2007/10/03)
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- Benzocycloalkene compounds, their production and use
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A compound of the formula STR1 wherein R1 and R2 independently represent H or an optionally substituted hydrocarbon group; R3 represents an optionally substituted hydrocarbon group; R4 represents H or a hydrocarbon group; ring A represents a substituted benzene ring; X represents a C2-4 alkylene group etc.; and Y represents a bond or a lower alkylene group, or salts thereof is useful as prophylactic or therapeutic agents of diseases related with melatonin activity.
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