Abstract: This invention relates to a radiodiagnostic agent to image tumors. A composition for a tumor imaging agent, a method and kit for preparing a tumor imaging agent, and a radiolabeling reagent for preparing the tumor imaging agent are provided.

Abstract: (E)-styryl benzylsulfones of formula I are useful as anticancer agents: 1

Abstract: This invention relates to the identification, purification, and characterization of a novel heterodimeric disintegrin, EC-3, from Echis carinatus viper venom. EC-3 inhibits &agr;4 integrins in an RGD-independent manner. The invention further relates to methods of using EC-3, or a biologically active fragment or derivative thereof, to inhibit the interaction between cells expressing &agr;4 integrins and cellular ligands.

Abstract: The invention provides prognostic methods which comprise determining the level of expression of the gene c-fyn, or the level of activated STAT-3 protein. Because the relative level of c-fyn expression and level of activated STAT-3 protein correlate with the presence of malignant potential and therefore patient prognosis, these markers may be used to make treatment decisions, to predict patient outcome, and to predict the risk of cancer in disease-free individuals. The invention further provides a method for identifying anticancer drugs in which inhibitors of cell proliferation are identified as inhibitors of Src-mediated STAT phosphorylation.

Abstract: (E)-styryl benzylsulfones of formula I are useful as anticancer agents: wherein R1, R2, R3, and R4 are independently selected from the group consisting of hydrogen, fluoro, chloro, iodo, bromo, C1-C6 alkyl, C1-C4 alkoxy, nitro, cyano and trifluoromethyl, with the proviso that (a) R1, R2 , and R3 not all hydrogen when R4 is 2-chloro or 4-chloro; (b) when R1 and R3 are hydrogen and R2 is 4-bromo or 4-chloro, then R4 may not be 4-chloro, 4-fluoro or 4-bromo; (c) when R1 and R3 are hydrogen and R2 is 4-fluoro, then R4 may not be 4-fluoro or 4-bromo, (d) when R1 is hydrogen, and R4 is 2-fluoro, the R2 and R3 may not be 4-fluoro; and (e) when R1 is hydrogen and R3 is 4-hydrogen, 4-chloro, 4-bromo, 4-methyl or 4-methoxy, and R4 is 2-hydrogen, 2-chloro, or 2-fluoro; then R2 may not be 4-hydrogen, 4-chloro, 4-fluoro, or 4-bromo.

Abstract: Pre-treatment with &agr;,&bgr; unsaturated aryl sulfones protects normal cells from the cytotoxic side effects of two classes of anticancer chemotherapeutics. Administration of a cytoprotective sulfone compound to a patient prior to anticancer chemotherapy with a mitotic phase cell cycle inhibitor or topoisomerase inhibitor reduces or eliminates the cytotoxic side effects of the anticancer agent on normal cells. The cytoprotective effect of the &agr;,&bgr; unsaturated aryl sulfone allows the clinician to safely increasing the dosage of the anticancer chemotherapeutic.

Abstract: Two-chain high molecular weight kininogen, and peptide analogs thereof having homology to sites within kininogen domain 5, are potent inhibitors of angiogenesis. The peptides have the formula X1-His-Lys-X-Lys-X2 wherein X is any amino acid, X1 is from zero to twelve amino acids, more preferably from zero to six amino acids, most preferably from zero to three amino acids, and X2 is from zero to twelve amino acids, more preferably from zero to six amino acids, most preferably from zero to three amino acids. X is preferably an amino acid having a nonpolar side chain, or a polar side chain which is uncharged at pH 6.0 to 7.0. X is most preferably Asn, Phe or His. Methods of inhibiting endothelial cell proliferation and angiogenesis are provided.

Abstract: (E)-styryl benzylsulfones of formula I are useful as anticancer agents: wherein R1, R2, R3, and R4 are independently selected from the group consisting of hydrogen, fluoro, chloro, iodo, bromo, C1-C6 alkyl, C1-C4 alkoxy, nitro, cyano and trifluoromethyl, with the proviso that (a) R1, R2, and R3 not all hydrogen when R4 is 2-chloro or 4-chloro; (b) when R1 and R3 are hydrogen and R2 is 4-bromo or 4-chloro, then R4 may not be 4-chloro, 4-fluoro or 4-bromo; (c) when R1 and R3 are hydrogen and R2 is 4-fluoro, then R4 may not be 4-fluoro or 4-bromo; (d) when R1 is hydrogen, and R4 is 2-fluoro, the R2 and R3 may not be 4-fluoro; and (e) when R1 is hydrogen and R3 is 4-hydrogen, 4-chloro, 4-bromo, 4-methyl or 4-methoxy, and R4 is 2-hydrogen, 2-chloro, or 2-fluoro; then R2 may not be 4-hydrogen, 4-chloro, 4-fluoro, or 4-bromo.

Abstract: Ligation of the Fc&ggr; receptor type I (Fc&ggr;RI) on IL-10-producing cells leads to a selective upregulation of IL-10 production, which in turn induces a marked suppression of IL-12 biosynthesis by IL-12-producing cells, particularly macrophages. The ligation of the Fc&ggr;RI receptor thus downmodulates IL-12 production via a mechanism that is dependent on macrophage-derived IL-10. Agents for ligating Fc&ggr;RI comprise, for example, multivalent antibodies which bind the Fc&ggr;RI receptor, immune complexes comprising antibodies which contain the Fc region of IgG, and IgG multimers, preferably IgG dimers and trimers. The ligating agent may be administered to therapeutically inhibit proinflammatory immune responses. In particular, the ligating agent may be administered to treat or prevent endotoxic shock associated with bacterial endotoxemia, and to treating autoimmune disorders.

Abstract: Pre-treatment with &agr;,&bgr; unsaturated aryl sulfones protects normal cells from the toxic side effects of ionizing radiation. Administration of a radioprotective &agr;,&bgr; unsaturated aryl sulfone compound to a patient prior to anticancer radiotherapy reduces the cytotoxic side effects of the radiation on normal cells. The radioprotective effect of the &agr;,&bgr; unsaturated aryl sulfone allows the clinician to safely increase the dosage of anticancer radiation. In some instances, amelioration of toxicity following inadvertent radiation exposure may be mitigated with administration of &agr;,&bgr; unsaturated arylsulfone.

Abstract: Ligation of the Fc&ggr; receptor type I (Fc&ggr;RI) on IL-10-producing cells leads to a selective upregulation of IL-10 production, which in turn induces a marked suppression of IL-12 biosynthesis by IL-12-producing cells, particularly macrophages. The ligation of the Fc&ggr;RI receptor thus downmodulates IL-12 production via a mechanism that is dependent on macrophage-derived IL-10. Agents for ligating Fc&ggr;RI comprise, for example, multivalent antibodies which bind the Fc&ggr;RI receptor, immune complexes comprising antibodies which contain the Fc region of IgG, and IgG multimers, preferably IgG dimers and trimers. The ligating agent may be administered to therapeutically inhibit proinflammatory immune responses. In particular, the ligating agent may be administered to treat or prevent endotoxic shock associated with bacterial endotoxemia, and to treating autoimmune disorders.

Abstract: Provided are the compound (E)-4-carboxystyryl-4-chlorobenzyl sulfone, pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof.

Abstract: Compounds of the formula are provided wherein R1, R2, R3 and R4 are independently selected from the group consisting of hydrogen, halogen, hydroxyl, C1-C8 alkyl, C1-C6 alkoxy, nitro, cyano, acetoxy, amino, carboxy, sulfamyl, lower acylsulfamyl and trifluoromethyl. The compounds are inhibitors of cyclooxygenase-2 activity, useful for treating inflammation and cyclooxygenase-mediated disorders.

Abstract: (E)-styryl benzylsulfones of formula I are useful as anticancer agents: 1

Abstract: N-(Aryl)-2-arylethenesulfonamides and pharmaceutically acceptable salts and compositions thereof are useful as antiproliferative agents, including, for example, anticancer agents. They are also useful as radioprotective agents.

Abstract: Styryl benzylsulfones of formula I are useful as antiproliferative agents, including, for example, anticancer agents: wherein R1 through R10 are defined herein; or a pharmaceutically acceptable salt thereof.

Abstract: A novel class of non-RGD disintegrins is described. These disintegrins have the core sequence KTS, and selectively inhibit the binding of &agr;1&bgr;1 integrin to its adhesive ligands. Two KTS-disintegrins, obtustatin and viperisrastatin, are also described. KTS-disintegrins can be used to treat diseases and modulate biological conditions associated with &agr;1&bgr;1 integrin.

Abstract: A mutant modified cyclin dependent kinase protein, or biologically active fragment, derivative, homolog or analog thereof is provided, which reversibly induces continual growth in cultured cells when administered to the cells exogenously in culture. Methods of reversibly inducing continual growth in cultured cells, and methods of screening cancer-causing agents with the continual growth-induced cells, are also provided.

Abstract: Sulfones of formula I are useful as antiproliferative agents, including, for example, anticancer agents: wherein: Q1 is selected from the group consisting of (a) a phenyl radical according to formula II  wherein R1, R2, R3, R4 and R5 are independently selected from the group consisting of hydrogen, halogen, C1-C6 alkyl, C1-C6 alkoxy, nitro, cyano, carboxyl, hydroxyl, amino, C1-C6 trifluoroalkoxy and trifluoromethyl; (b) an aromatic radical selected from the group consisting of 1-naphthyl, 2-naphthyl and 9-anthryl; and (c) an aromatic radical according to formula III  wherein n1 is 1 or 2, Y1 and Y2 are independently selected from the group consisting of hydrogen, halogen, and nitro, and X1 is selected from the group consisting of oxygen, nitrogen, sulfur and and Q2 is selected from the group consisting of (d) a phenyl radical according to formula II, as defined above; (e) an aromatic radical selected from the group co

Abstract: Styryl sulfone compounds of the invention selectively inhibit proliferation of tumor cells, and induce apoptosis of tumor cells, while sparing normal cells.