Abstract: Novel tubulin binding compounds (SPIKETS) having potent tubulin depolymerization activity and inhibitory activity against tubulin polymerization. The compounds are effective agents for inhibiting cellular proliferation, for example, in cancer cells. The compounds are adapted to interact favorably with a novel SP binding pocket on tubulin, which pocket is useful for screening of anti-tubulin, anti-proliferation, and anti-cancer drugs.

Abstract: The present invention is directed to derivatives of piperidinylethyl, phenoxyethyl, and fluorophenethyl bromopyridyl thioureas, which have been found to be effective non-nucleoside inhibitors (NNRTI) of NNI-resistant and multi-drug resistant human immunodeficiency virus (HIV)-1 reverse transcriptase (RT). The present invention is further directed to methods of using the above derivatives to treat patients with NNI-resistant or multi-drug resistant human immunodeficiency virus (HIV)-1.

Abstract: A method for the preparation of 5′-hydroxy phosphorylated nucleoside derivatives in a single reaction vessel is provided. The method includes contacting phosphorous oxychloride with a halophenyl moiety followed by contacting the resulting halophenylphosphorodichloridate with a carboxy-protected amino acid and finally contacting the resulting halophenyl carboxy-protected amino acid phosphorochloridate with a nucleoside.

Abstract: Vanadium (IV) complexes containing a substituted or unsubstituted catecholate ligand, and the spermicidal activity of such compounds. Preferred compounds are vanadocene (IV) complexes containing alkyl substituted catecholate ligands.

Abstract: Quinazoline compounds and methods for the treatment of cancer and for the treatment of allergic reactions.

Abstract: Methods for increasing the elimination half-life of key metabolites such as d4T by administering an aryl phosphate derivative of d4T having an electron withdrawing substituent on the aryl group and an amino acid substituent on the phosphate group are described. A preferred aryl phosphate derivative of d4T is HI-113 (d4T-5′-[p-bromophenyl methoxyalaninyl phosphate]). The administration of HI-113 results in more prolonged systemic exposure to the key metabolites, Ala-d4T-MP and d4T, than administration of an equimolar dose of either metabolite. Each metabolite has a significantly longer elimination half life when formed in vivo from the administration of HI-113 than when the metabolite is administered directly.

Abstract: Inhibitors of JAK3 kinase for the treatment of allergy inhibit mast cell degranulation an dmediator release.

Abstract: Pharmaceutical compositions for parenteral administration of poorly soluble quinazoline compounds in the form of microemulsions or micellar solutions are described. The compositions are useful in treating patients suffering from cancer or having allergic reactions.

Abstract: The invention provides methods for treating cancer and vanadium compounds that are useful for the treatment of tumors, as well as pharmaceutical compositions comprising the compounds, and synthetic methods and intermediates useful for preparing the compounds.

Abstract: Novel compounds and pharmaceutical compositions useful as EGFR tyrosine kinase inhibitors. Methods of the invention include administration of the EGFR TK inhibitors to treat diseases characterized by enhanced expression of EGF, including cancers, particularly breast cancer. Additionally, a homology model representing the structure of EGFR kinase domain is provided, which model is useful for the rationally design and screening of compounds predicted to bind favorably to EGFR and to inhibit EGFR TK.

Abstract: This invention provides combinatorial chemistry libraries containing thiourea and urea compounds. In addition, the invention relates to methods for constructing combinatorial chemistry libraries containing thiourea and urea compounds. Furthermore, this invention relates to methods for the identification of bioactive thiourea and urea compounds as well as compositions and therapeutic methods for treating cancer.

Abstract: Novel spermicidal compounds which are organometallic cyclopentadienyl metal complexes, particularly vanadium IV complexes, are described including corresponding contraceptive and therapeutic compositions and method for providing contraception and selective killing of testicular germ cells. Included among the vanadium complexes are vanadocene dichloride, vanadocene dibromide, bis (methyl cyclopentadienyl) vanadium dichloride, vanadocene diiodide, vanadocene di-pseudohalides, and others. Most active found was vanadocene diselenocyanate.

Abstract: A novel carbonyl-substituted quinazoline, preferably 4-(3′-bromobenzoyl)-6,7-dimethoxyquinazoline (WHI-P164), and methods for lowering blood cholesterol, including reducing total cholesterol and LDL-cholesterol levels by administration of the carbonyl quinazolines and compositions thereof.

Abstract: Novel phenylethyl-thiourea (PHET) compounds as inhibitors of reverse transcriptase and effective agents for the treatment of HIV infection, including mutant, drug-sensitive, drug-resistant, and multi-drug resistant strains of HIV.

Abstract: 2,4,6-trihydroxy-&agr;-p-methoxyphenylacetophenone (also identified herein as “D-58”), or its pharmaceutically acceptable derivatives such as salt and ester forms, is administered for inhibiting inflammatory reactions. The treatment can be remedial or prophylactic. Examples of the conditions that can be treated include acute inflammatory reactions and allergic inflammatory reactions, and specific examples include allergy, asthma, arthritis, psoriasis, skin sunburn, inflammatory pelvic disease, inflammatory bowel disease, urethritis, uvitis, senusitis, pneumonitis, encephalitis, meningitis, myocarditis, nephritis, osteomyelitis, myositis, hepatitis, gastritis, enteritis, dermatitis, gingivitis, appendicitis, pancreatitis, cholocystitis and cholangitis. The 2,4,6-trihydroxy-&agr;-p-methoxyphenylacetophenone can be administered by various routes as needed.

Abstract: Inhibitors of JAK3 kinase for the treatment of allergy inhibit mast cell degranulation an dmediator release.

Abstract: A method for preventing and treating ALS by administering a phytoestrogen, preferably genistein.

Abstract: Novel phenethyl-5-bromopyridylthiourea (PBT) and dihydroalkoxybenzyloxopyrimidine (DABO) derivatives exhibiting spermicidal activity as well as anti-viral activity. These novel compounds can be incorporated within contraceptive compositions to provide for spermicidal or sperm-immobilizing activity.

Abstract: Novel tubulin binding compounds having potent tubulin depolymerization activity and inhibitory activity against tubulin polymerization. The compounds are effective agents for inhibiting cellular proliferation, for example, in cancer cells. The compounds are adapted to interact favorably with a novel tubulin binding pocket, which pocket is useful for screening of anti-tubulin, anti-proliferation, and anti-cancer drugs.

Abstract: The present invention provides a novel biotherapeutic agent comprising a monoclonal antibody TXU-7, which is specific to the CD7 antigen, conjugated to the pokeweed antiviral protein (PAP). This immunoconjugate was designated TXU-7-PAP. The CD7 antigen is present on the surface of the majority of T-lymphocytes, including those that are the cellular target of the human immunodeficiency virus (HIV). The pokeweed antiviral protein displays broad spectrum antiviral activity toward various plant, animal, and human viruses, including HIV. Prior attempts to generate PAP immunoconjugates with anti-HIV activity have been unsuccessful due to the poor stability of the immunoconjugate in vivo. However, the TXU-7-PAP immunoconjugate described herein displayed potent antiviral activity against HIV-1 and low toxicity in various animal models. Preliminary clinical studies in HIV-1-infected patients demonstrated that the immunoconjugate was well-tolerated and reduced the HIV-1 viral load.