In this patent we describe the purification of prenylated benzophenones from the fruit rinds of Garcinia species and its evaluation as an inhibitor for Histone acetyltransferases p300 and PCAF. We have found that prenylated benzophenones are potent HAT inhibitors of p300 (IC.sub.50-1 .mu.M) and pCAF (IC.sub.50-15 .mu.M). The inhibitors significantly repress the p300 HAT dependent transcriptional activation from in vitro assembled chromatin template but had no effect on transcription from DNA. Th...

Analogs of combretastatin have been discovered which demonstrate impressive cytotoxicity as well as a remarkable ability to inhibit tubulin polymerization. Such compounds are excellent clinical candidates for the treatment of cancer in humans. In addition, certain of these ligands, as pro-drugs, may well prove to be tumor selective vascular targeting chemotherapeutic agents or to have vascular targeting activity resulting in the selective prevention and/or destruction of nonmalignant proliferati...

Disclosed are novel, synthetic analogues of (1E,6E)-1,7-Bis(4-hydroxy-3-methoxyphenyl)-1,6-heptadiene-3,5-dione and the therapeutic applications for cystic fibrosis thereof in correcting altered CFTR trafficking and the associated impaired chloride (Cl.sup.-) ion transport. Introduction of branched-alkyl groups ortho to the phenolic groups gave rise to clinical compounds with vastly improved trafficking of delF508CFTR and with no cytotoxicity.

A diarylheptanoide derivative of the following formula (1), ##STR1## and a drug composition comprising this compound, such as a 5-lipoxygenase inhibitor, an antiinflammatory agent, and the like. The diarylheptanoide derivative (1) is effective for treating and preventing various inflammatory diseases due to its strong 5-lipoxygenase inhibiting effect.

The present invention relates to improved methods for achieving the synthesis of 1,7-diaryl-1,6-heptadiene-3,5-diones, and in particular curcumin and its analogues. The invention provides a process for synthesizing such compounds in substantial yield and purity using environmentally benign processes and materials. The invention also relates to the use of such synthesized products in the treatment of Alzheimer's Disease and other diseases.

A process for the purification of 1,3-diketones comprising reacting a 1,3-diketone with an earth metal or alkaline earth metal complexing agent in an organic solvent, isolating, washing and decomposing the resulting complex, and isolating the purified 1,3-diketone.

2-Benzyloxyalkyl halophenones of the formula (3): ##STR1## wherein X.sup.1 and X.sup.2 are each independently H, Cl or F, provided that at least one of X.sup.1 and X.sup.2 is Cl or F; one of R.sup.3 and R.sup.4 is H and the other is optionally substituted benzyloxy; and R.sub.5 is an unsubstituted alkyl, preferably a C.sub.1-6 alkyl group. The compounds are useful as intermediates for preparing 2-hydroxyalkyl halophenones.

Catalyst compositions for preparing polyketones comprising (a) a Group VIII metal compound, containing at least one ligand capable of coordinating to the Group VIII metal, and (b) a boron hydrocarbyl compound are disclosed, in particular catalyst compositions wherein the boron hydrocarbyl compound is a Lewis acid of the formula BXYZ where at least one of X, Y and Z is a monovalent hydrocarbyl group. A preferred catalyst composition comprises a palladium complex and B(C.sub.6 F.sub.5).sub.3.

The present invention relates to compounds capable of acting as androgen receptor antagonists, pharmaceutical formulations containing the same, and methods of use thereof. Such uses include, but are not limited to, use as antitumor agents, particularly for the treatment of cancers such as colon, skin and prostate cancer and to induce androgen receptor antagonist activity in a subject afflicted with an androgen-related affliction. Examples of androgen-related afflictions include, but are not limi...

The present invention relates to chalcone and chalcone derivatives and analogs which are useful as angiogenesis inhibitors. The present compounds, which are inexpensive to synthesize, exhibit unexpectedly good activity as angiogenesis inhibitors. The present invention also relates to the use of chalcone and its analogs as antitumor/anticancer agents and to treat a number of conditions or disease states in which angiogenesis is a factor, including angiongenic skin diseases such as psoriasis, acne...