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: 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: Sulfones of formula I are useful as antiproliferative agents, including, for example, anticancer agents: 1

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

Abstract: (Z)-styryl benzylsulfones of formula I are useful as anticancer agents: wherein R1 is selected from the group consisting of hydrogen, chloro and nitro; R2 is selected from the group consisting of hydrogen, lower alkyl, lower alkoxy, chloro, bromo, iodo and fluoro; and R3 and R4 are independently selected from the group consisting of hydrogen, lower alkyl, nitro, chloro, bromo, iodo and fluoro; provided that at least one of R1 or R2 is hydrogen. The corresponding (Z)-styryl benzylsulfides are useful as intermediates in the preparation of the biologically active (Z)-styryl benzyl sulfones.

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

Abstract: &agr;, &bgr;-Unsaturated sulfones of the following formulae are provided, which are useful as antiproliferative agents, including, for example, anticancer agents:

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: Styryl benzylsulfones of formula I are useful as antiproliferative agents, including, for example, anticancer agents: 1

Abstract: Styryl benzylsulfones of formula I are useful as antiproliferative agents, including, for example, anticancer agents: wherein (a) (i) at least three of R1, R2, R3, R4 and R5 are independently selected from the group consisting of halogen, C1-C6 alkyl, C1-C6 alkoxy, nitro, cyano, carboxyl, hydroxyl, phosphonato, amino, sulfamyl, acetoxy, dimethylamino(C2-C6 alkoxy) and trifluoromethyl, and the balance of said 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, phosphonato, amino, sulfamyl, acetoxy, dimethylamino(C2-C6 alkoxy) and trifluoromethyl; and (ii) R6, R7, R8, R9 and R10 are independently selected from the group consisting of hydrogen, halogen, C1-C6 alkyl, C1-C6 alkoxy, nitro, cyano, carboxyl, hydroxyl, phosphonato, amino, sulfamyl, acetoxy, dimethylamino(C2-C6 alkoxy) and trifluoromethyl; or (b) (i) at least three of R6, R7, R8, R9 and R10 are independently selected from the

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: 1

Abstract: (Z)-styryl benzylsulfones of formula I are useful as anticancer agents: wherein R1 is selected from the group consisting of hydrogen, chloro and nitro; R2 is selected from the group consisting of hydrogen, lower alkyl, lower alkoxy, chloro, bromo, and fluoro; and R3 and R4 are independently selected from the group consisting of hydrogen, lower alkyl, nitro, chloro, bromo, and fluoro; provided that at least one of R1 or R2 is hydrogen. The corresponding (Z)-styryl benzylsulfides are useful as intermediates in the preparation of the biologically active (Z)-styryl benzyl sulfones.

Abstract: Transgenic non-human animals and transgenic non-human stem cells are described having a functionally disrupted A-myb locus. Targeting constructs used to produce such transgenic stem cells and animals, and methods and targeting constructs for inactivating an endogenous A-myb gene locus, are also provided. Also provided are methods for generating transgenic sperm and transgenic nonhuman animals harboring a desired transgene.

Abstract: Compounds of the formula wherein: X is selected from the group consisting of trihalomethyl, C1-C6 alkyl, and a group of formula II: wherein: R3 and R4 are independently selected from the group consisting of hydrogen; halogen; hydroxyl; nitro; C1-C6 alkyl; C1-C6 alkoxy; carboxy; C1-C6 trihaloalkyl; and cyano; Z is selected from the group consisting of substituted and unsubstituted aryl; or a pharmaceutically acceptable salt thereof. The compounds are inhibitors of cyclooxygenase-2 activity. They are useful for treating cyclooxygenase-mediated disorders, including, for example, inflamation, neoplastic disorders and angiogenesis-mediated disorders.

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

Abstract: Sulfones of formula I are useful as antiproliferative agents, including, for example, anticancer agents: 1

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

Abstract: (Z)-styryl benzylsulfones of formula I are useful as anticancer agents: wherein R1 is selected from the group consisting of hydrogen, chloro and nitro; R2 is selected from the group consisting of hydrogen, lower alkyl, lower alkoxy, chloro, bromo, and fluoro; and R3 and R4 are independently selected from the group consisting of hydrogen, lower alkyl, nitro, chloro, bromo, and fluoro; provided that at least one of R1 or R2 is hydrogen. The corresponding (Z)-styryl benzylsulfides are useful as intermediates in the preparation of the biologically active (Z)-styryl benzyl sulfones.

Abstract: A novel multi-unit ribozyme is provided which is capable of selectively cleaving the mRNA transcript of a hybrid oncogene resulting from a chromosomal translocation. Specialized delivery vehicles such as liposomes, and growth factor conjugates for cellular uptake by receptor-mediated endocytosis, are also described. The multi-unit ribozyme is used for the treatment of neoplasms characterized by expression of the oncogene. In one embodiment, a multi-unit ribozyme is provided which cleaves the mRNA transcript of Philadelphia chromosome-positive cells, thereby blocking production of the tumorigenic p210.sup.bcr-abl fusion protein.