Abstract: Formulations are provided for parenteral administration of (amino substituted (e)-2,6-dialkoxystyryl 4-substituted benzylsulfones and the sodium and potassium salts thereof for the prevention and/or treatment of conditions mediated by abnormal cell proliferation. Composition for parenteral administration are provided which comprise an effective amount of compound of formula I or a compound of formula IIa and at least about 50% by weight of at least one water soluble polymer selected from the group consisting essentially of polyethylene glycol (PEG), poly-oxyethylene, poly-oxyethylene-poly-oxypropylene copolymers, polyglycerol, polyvinylalcohol, polyvinylpyrrolidone (PVP), polyvinylpyridine N-oxide, copolymer of vinylpyridine N-oxide and vinylpyridine.

Abstract: The invention provides drug screening methods and methods for determining efficacy of a therapeutic regimen in humans. In particular, the invention provides screening methods to determine efficacy of a therapeutic regimen to protect human subjects from deleterious effects of cytotoxic agents. The inventive method comprises i) extracting target cells from the human subject prior to exposure to a cytotoxic agent, ii) treating the subject with a cytotoxic protective drug; iii) extracting the target cells from the subject after treatment with the cytotoxic protective drug of step ii); iv) exposing the target cells of steps i) and iii) to the cytotoxic agent; and v) analyzing and comparing one or more parameters indicative of viability and growth conditions in target cells of step i) and step iii), wherein a favorable viability and growth condition of the target cells of step iii) as compared to target cells of step i) is indicative of the efficacy of the therapeutic regimen in the human subject.

Abstract: Substituted phenol derivatives of Formula (I) are useful as antiproliferative agents including, for example, anticancer agents, and as radioprotective and chemoprotective agents.

Abstract: A pharmaceutical composition is provided for administration prior to or after exposure to ionizing radiation for reducing toxic effects of the radiation in a subject. An effective amount of the pharmaceutical composition provided comprising an effective amount of at least one radioprotective ?, ? unsaturated aryl sulfone, and at least one component selected from the group consisting of a) at least one water soluble polymer in an amount between about 0.5% and about 90% w/v, b) at least one chemically modified cyclodextrin in an amount between about 20% and about 60% w/v, and c) DMA in an amount between about 10% and about 50% w/v.

Abstract: Activated cytotoxic compounds are described for attachment to targeting molecules for the treatment of a mammalian disease condition which comprise, an activator, a spacer linker, a linker (e.g., self-immolative), and a cytotoxic drug selected from the group consisting of AMINO-SUBSTITUTED (E)-2,6-DIALKOXYSTYRYL 4-SUBSTITUTED BENZYLSULFONES, AMINO-AND-HYDROXY SUBSTITUTED STYRYLSULFONANILIDES, and SUBSTITUTED PHENOXY- AND PHENYLTHIO-STYRYLSULFONE DERIVATIVES. Activated cytotoxic compound attached to a targeting molecule are described wherein the targeting molecule is selected from the group consisting essentially of an antibody, a receptor, a ligand, a cytokine, a hormone, and a signal transduction molecule. The invention is further directed to a method of treatment of disease conditions.

Abstract: Methods of treating cancer using compounds according to Formula (I) are disclosed herein, wherein X, X1, X2, Ra, R1, R2, R3, R4, R5, R6, R7, g, M, y, a, b, d, e, V, W, Z and Q are as defined herein.

Abstract: Compounds useful as antiproliferative agents, including, for example, anticancer agents, are provided according to formula (I); wherein: X, X1, X2, Ra, R1, R2,R3, R4, R5, R6, R7, g, M, y, a, b, d, e, V, W, Z and Q are as defined herein.

Abstract: Solution and suspension formulations are provided for administration prior to or after exposure to ionizing radiation for reducing toxic effects of the radiation in a subject which comprises an effective amount of at least one radioprotective ?,? unsaturated aryl sulfone wherein the composition has a pH within the range of about 8 to about 9.

Abstract: ?,?-Unsaturated sulfides, sulfones, sulfoxides and sulfonamides according to Formula I: wherein Ar1, Ar2, X, n, * and R are as defined herein, are prepared by dehydration of ?-hydroxy sulfides, sulfones, sulfoxides or sulfonamides.

Abstract: Formulations are provided for parenteral administration of (amino substituted (e)-2,6-dialkoxystyryl 4-substituted benzylsulfones and the sodium and potassium salts thereof for the prevention and/or treatment of conditions mediated by abnormal cell proliferation. Composition for parenteral administration are provided which comprise an effective amount of compound of formula I or a compound of formula IIa and at least about 50% by weight of at least one water soluble polymer selected from the group consisting essentially of polyethylene glycol (PEG), poly-oxyethylene, poly-oxyethylene-poly-oxypropylene copolymers, polyglycerol, polyvinylalcohol, polyvinylpyrrolidone (PVP), polyvinylpyridine N-oxide, copolymer of vinylpyridine N-oxide and vinylpyridine.

Abstract: Substituted phenol derivatives of Formula (I) are useful as antiproliferative agents including, for example, anticancer agents, and as radioprotective and chemoprotective agents.

Abstract: Compounds useful as antiproliferative agents, including, for example, anticancer agents, are provided according to formula I: wherein: Ar, X, X1, g, R and R3 are as defined herein.

Abstract: Provided are compounds, processes and synthetic intermediates useful for the preparation of compounds of the formula I and IX wherein R1 is selected from the group consisting of hydrogen, trihalomethyl, C1–C6 alkyl and substituted or unsubstituted phenyl; Y is a group of the formula wherein R2 is selected from the group consisting of C1–C6 alkyl, C1–C6 alkanoylamino and amino; and R5 is selected from the group consisting of hydrogen, amino, halogen, hydroxyl, nitro, C1–C6 alkyl, C1–C6 alkoxy, carboxy, C1–C6 trihaloalkyl, cyano, phosphonato, and hydroxyalkyl; and Z is selected from the group consisting of substituted and unsubstituted aryl. Also provided are certain N-acylated analogs of compounds of the formula I and IX, and processes for their preparation.

Abstract: Provided are compounds, processes and synthetic intermediates useful for the preparation of compounds of the formula I and IX wherein R1 is selected from the group consisting of hydrogen, trihalomethyl, C1-C6 alkyl and substituted or unsubstituted phenyl; Y is a group of the formula wherein R2 is selected from the group consisting of C1-C6 alkyl, C1-C6 alkanoylamino and amino; and R5 is selected from the group consisting of hydrogen, amino, halogen, hydroxyl, nitro, C1-C6 alkyl, C1-C6 alkoxy, carboxy, C1-C6 trihaloalkyl, cyano, phosphonato, and hydroxyalkyl; and Z is selected from the group consisting of substituted and unsubstituted aryl. Also provided are certain N-acylated analogs of compounds of the formula I and IX, and processes for their preparation.

Abstract: Compounds useful as antiproliferative agents, including, for example, anticancer agents, are provided according to formula (I); wherein: X, X1, X2, Ra, R1, R2,R3, R4, R5, R6, R7, g, M, y, a, b, d, e, V, W, Z and Q are as defined herein.

Abstract: Provided are processes and chemical intermediates useful for preparing a compound of the formula I wherein X is selected from the group consisting of C1-C6 trihalomethyl; C1-C6 alkyl; and an optionally substituted or di-substituted phenyl group of formula II: Y and Z are independently selected from the group consisting of substituted and unsubstiotuted aryl

Abstract: Provided are compounds, processes and synthetic intermediates useful for the preparation of compounds of the formula I and IX wherein R1 is selected from the group consisting of hydrogen, trihalomethyl, C1-C6 alkyl and substituted or unsubstituted phenyl; Y is a group of the formula wherein R2 is selected from the group consisting of C1-C6 alkyl, C1-C6 alkanoylamino and amino; and R5 is selected from the group consisting of hydrogen, amino, halogen, hydroxyl, nitro, C1-C6 alkyl, C1-C6 alkoxy, carboxy, C1-C6 trihaloalkyl, cyano, phosphonato, and hydroxyalkyl; and Z is selected from the group consisting of substituted and unsubstituted aryl. Also provided are certain N-acylated analogs of compounds of the formula I and IX, and processes for their preparation.

Abstract: Provided are processes for the preparation of the compound of the formula wherein R1, R3 and R4 are independently selected from the group consisting of hydrogen, halogen, hydroxyl, nitro, lower alkyl, lower alkoxy, carboxy, C1-C6 trihaloalkyl, and cyano; and R2 is amino or lower alkyl. Also provided are synthetic intermediates that are useful as intermediates in the preparation of the compound of the formula 1.

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: 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.