Abstract: The tetracycline class of antibiotics has played a major role in the treatment of infectious diseases for the past 50 years. However, the increased use of the tetracyclines in human and veterinary medicine has led to resistance among many organisms previously susceptible to tetracycline antibiotics. The recent development of a modular synthesis of tetracycline analogs through a chiral enone intermediate has allowed for the efficient synthesis of novel tetracycline analogs never prepared before. The present invention provides a more efficient route for preparing the enone intermediate.

Abstract: Disclosed herein are analogs of Salinosporamide A, having the Formula I as follows: Like Salinosporamide A, the compounds of the present invention will inhibit the proteasome, an intracellular enzyme complex that destroys proteins the cell no longer needs. Without the proteasome, proteins would build up and clog cellular machinery. Fast-growing cancer cells make especially heavy use of the proteasome, so thwarting its action is a compelling drug strategy.

Abstract: The present invention provides methods and systems for the identification of a biological target of a chemical compound, such as saframycin A, known to bind a polynucleotide. The invention also provides methods of screening chemical compounds for those which act in a similar method and may be more potent than known compounds. The inventive methods are particularly useful in the high-throughput screening of chemical compounds that target GAPDH. The invention also provides kits useful in the practice of the inventive method. Compounds identified by inventive methods are also included in the invention.

Abstract: In recognition of the need to develop novel therapeutic agents and efficient methods for the synthesis thereof, the present invention provides novel compounds of general formula (I), and methods for the synthesis thereof. In another aspect, the present invention provides pharmaceutical compositions comprising a compound of formula (I) and a pharmaceutically acceptable carrier. In yet another aspect, the present invention provides methods for treating cancer comprising administering a therapeutically effective amount of a compound of formula (I) to a subject in need thereof.

Abstract: The present invention provides methods and systems for the identification of a biological target of a chemical compound, such as saframycin A, known to bind a polynucleotide. The invention also provides methods of screening chemical compounds for those which act in a similar method and may be more potent than known compounds. The inventive methods are particularly useful in the high-throughput screening of chemical compounds that target GAPDH. The invention also provides kits useful in the practice of the inventive method. Compounds identified by inventive methods are also included in the invention.

Abstract: In recognition of the need to develop novel therapeutic agents and efficient methods for the synthesis thereof, the present invention provides novel compounds of general formula (I), and methods for the synthesis thereof. In another aspect, the present invention provides pharmaceutical compositions comprising a compound of formula (I) and a pharmaceutically acceptable carrier. In yet another aspect, the present invention provides methods for treating cancer comprising administering a therapeutically effective amount of a compound of formula (I) to a subject in need thereof.

Abstract: In recognition of the need to develop novel therapeutic agents and efficient methods for the synthesis thereof, the present invention provides novel compounds of general formula (I), and methods for the synthesis thereof.

Abstract: In recognition of the need to develop novel therapeutic agents and efficient methods for the synthesis thereof, the present invention provides novel compounds of general formula (I), and methods for the synthesis thereof.

Abstract: A practical synthesis of the potential chemotherapeutic agent L-azatyrosine is described. The key step involved the alkylation of (R,R)-(-)-pseudoephedrine glycinamide with 5-benzenesulfonyloxy-2-iodomethylpyridine and proceeded in 70-95% yield and 89-95% de. Simultaneous hydrolysis of the auxiliary and the benzenesulfonate protecting group afforded L-azatyrosine of .gtoreq.99% ee in 73% yield on multigram scale (recovery yield of (R,R)-(-)-pseudoephedrine: 90%).

Abstract: A method for synthesizing enantiomerically enriched chemical intermediates with predetermined chirality is described. The method comprises formation of a pseudoephedrine amide, followed by stereoselective alkylation at the alpha carbon. The chiral auxiliary can then be cleaved off, affording chiral end products useful for further transformations. The enantiomeric enrichment of the chiral end products may exceed 98%, and the chiral auxiliary can be recovered. Novel amides of pseudoephedrine used in this method are also disclosed.