Abstract: A method of increasing the fluorous nature of a compound includes the step of reacting the compound with at least one second compound having the formula: wherein Rf is a fluorous group and m is 0, 1 or 2.

Abstract: The present invention provides an efficient synthetic strategy for the preparation of analogs that incorporate important structural elements of the marine natural product curacin A, the compositions and various uses of the compositions. The most active of these compounds at nanomolar concentrations inhibit tubulin polymerization, show growth inhibition activity, inhibited colchicines binding to tubulin and block mitotic progression. The compounds of the present invention represent some of the most potent synthetic curacin A analogs synthesized, with an activity profile rivaling that of the natural product despite the simplified structure, greater water solubility, and increased chemical stability.

Abstract: Oxidative cyclization of bis-naphthyl ethers allows concise total syntheses of palmarumycin CP, and deoxypreussomerin A in 8-9 steps and 15-35% overall yield from 5-hydroxy-8-methoxy-1 -tetralone. A small library of palmarumycin analogs was created. Biological evaluation of these naphthoquinone spiroketals against MCF-7 and MDA-MB-23 1 human breast cancer cells revealed several low-micromolar growth inhibitors. A number of the analogs inhibit the thioredoxin -thioredoxin reductase system.

Abstract: The present invention provides an efficient synthetic strategy for the preparation of analogs that incorporate important structural elements of the marine natural product curacin A, the compositions and various uses of the compositions. The most active of these compounds at nanomolar concentrations inhibit tubulin polymerization, show growth inhibition activity, inhibited colchicines binding to tubulin and block mitotic progression. The compounds of the present invention represent some of the most potent synthetic curacin A analogs synthesized, with an activity profile rivaling that of the natural product despite the simplified structure, greater water solubility, and increased chemical stability.

Abstract: The present invention provides several methods of synthesis and separation in which organic/fluorous phase separation techniques are used to effect separations. The present invention also provides novel compositions of matter comprising fluorous Si, Sn and Ge compounds.

Abstract: The present invention is directed to compounds having the formula: ##STR1## The invention further provides a method of making the compounds. The compounds are useful as inhibitors of protein phosphatases, for example PP1, PP2A, PP3, CDC25A and CDC25B. The invention is further directed to a method of inhibiting a protein phosphatase, a method of inhibiting cell proliferation, and pharmaceutical compositions comprising the subject compounds.

Abstract: Peptidyl prodrugs of therapeutic agents having an activating function are sclosed. These therapeutic agents having activating functions include those having an amino, thiol, or hydroxyl function. Methods of making and using these prodrugs are also disclosed.

Abstract: The present invention is directed to compounds having the formula: ##STR1## The invention further provides a method of making the compounds. The compounds are useful as inhibitors of protein phosphatases, for example PP1, PP2A, PP3, CDC25A and CDC25B. The invention is further directed to a method of inhibiting a protein phosphatase, a method of inhibiting cell proliferation, and pharmaceutical compositions comprising the subject compounds.

Abstract: The present invention provides several methods of synthesis and separation in which organic/fluorous phase separation techniques are used to effect separations. The present invention also provides novel compositions of matter comprising fluorous Si, Sn and Ge compounds.

Abstract: The present invention is directed to compounds having the formula: ##STR1## The invention further provides a method of making the compounds. The compounds are useful as inhibitors of protein phosphatases, for example PP1, PP2A, PP3, CDC25A and CDC25B. The invention is further directed to a method of inhibiting a protein phosphatase, a method of inhibiting cell proliferation, and pharmaceutical compositions comprising the subject compounds.

Abstract: The present invention is directed to compounds having the formula: ##STR1## The invention further provides a method of making the compounds. The compounds are useful as inhibitors of protein phosphatases, for example PP1, PP2A, PP3, CDC25A and CDC25B. The invention is further directed to a method of inhibiting a protein phosphatase, a method of inhibiting cell proliferation, and pharmaceutical compositions comprising the subject compounds.