Abstract: A method for treating cancer in a subject, comprising administering to a subject having cancer a therapeutically effective amount of (i) a fluoroquinolone derivative that inhibits tyrosyl-DNA-phosphodiesterase 1 (Tdp1) activity or (ii) a sulfonamide moiety-containing compound that inhibits tyrosyl-DNA-phosphodiesterase 1 (Tdp1) activity, thereby treating the cancer in the subject. In certain embodiments, the fluoroquinolone derivative or sulfonamide moiety-containing compound is co-administered with a topoisomerase I (TopI) inhibitor.

Abstract: The present invention is directed towards lasonolide derivatives, methods of inducing premature chromosome condensation using lasonolide derivatives, and methods of treating disorders, such as cancer, in a subject, the method comprising administering to the subject a lasonolide derivative.

Abstract: A method for treating cancer in a subject, comprising administering to a subject having cancer a therapeutically effective amount of (i) a fluoroquinolone derivative that inhibits tyrosyl-DNA-phosphodiesterase 1 (Tdp1) activity or (ii) a sulfonamide moiety-containing compound that inhibits tyrosyl-DNA-phosphodiesterase 1 (Tdp1) activity, thereby treating the cancer in the subject. In certain embodiments, the fluoroquinolone derivative or sulfonamide moiety-containing compound is co-administered with a topoisomerase I (TopI) inhibitor.

Abstract: Novel quinoline inhibitors of retroviral integrase, particularly HIV-1 integrase. The quinoline inhibitors are oxoquinolines that can be used for preventing or treating AIDS or HIV infection in a subject.

Abstract: Treatment of cells or subjects (e.g., humans, animals) carrying or infected with a virus capable of causing an immunodeficiency disease by administration of one or more compounds that inhibit integrase.

Abstract: Described herein are Chk2-inhibitor compounds and derivatives thereof, and methods of treating or preventing disease and disease symptoms using the compounds and compositions thereof.

Abstract: The present invention is directed towards lasonolide derivatives, methods of inducing premature chromosome condensation using lasonolide derivatives, and methods of treating disorders, such as cancer, in a subject, the method comprising administering to the subject a lasonolide derivative.

Abstract: The instant invention is directed towards compounds, including diamidines, that inhibit Tdp1 and are useful in the treatment and/or prevention of cancer and parasitic disease.

Abstract: The instant invention is directed towards tetracycline compositions, and methods of inhibiting Tdp1 activity, and methods of treating Tdp1-associated disorders.

Abstract: Provided herein are Compounds having the following structure: wherein A, L, X and ring B are as defined herein, compositions comprising an effective amount of a Compound and methods for treating or preventing cancer, hypoxia, diabetes, stroke, autoimmune disease or a condition treatable or preventable by inhibition of Chk2, the ATM-Chk2 pathway or RSK2 comprising administering an effective amount of a Compound to a patient in need thereof.

Abstract: Novel quinoline inhibitors of retroviral integrase, particularly HIV-1 integrase. The quinoline inhibitors are oxoquinolines that can be used for preventing or treating AIDS or HIV infection in a subject.

Abstract: The synthesis and biological activity of benzoisoindoloisoquinolone compounds are described. The synthesis and biological activity of C-11-substituted indenoisoquinolones are also described. Indenoisoquinolones substituted at C-11 are prepared by McMurry reactions of 11-ketoindenoisoquinolones with aldehydes.

Abstract: The present invention relates to compounds of formula I: useful HIV infection, AIDS, and other similar diseases. These compounds include inhibitors of the retroviral integrase enzyme that are useful in the treatment of HIV infection, AIDS, and other similar diseases characterized by integration of a retroviral genome into a host chromosome. The compounds of the invention are useful in pharmaceutical compositions and methods of treatment to reduce incorporation of a donor DNA into a receiving DNA.

Abstract: The present invention discloses non-catechol compounds, such as thiazolothiazepines, and analogs and derivatives thereof, which are anti-integrase inhibitors. The compounds, which are useful as treatments for HIV disease, include compounds (I), (II), (III), or pharmaceutically acceptable salts thereof wherein A is thiazole, benzene, naphthalene, pyridine, pyrimidine, pyrazine, or quinoline; R is one or more of H, halogen, lower alkyl, lower alkoxy, NO2, lower ester or carboxylic acid; X—Y is CH2—S, S—CH2, CH2—O, CH2—S(O). S(O)—CH2, CH2—CH2, CH2—CH2—CH2, or CH2—CH2—CH2—CH2; R4 is H or hydroxy; R5 is H, phenyl, or alkylamine; W is S or O; and R6 is H, substituted or unsubstituted alkyl or amine; and Z is S, O, CH2, CH2CH2, or C?O.

Abstract: Indenoisoquinolines and dihydroindenoisoquinolines are described. In particular, such compounds possessing one or more electron withdrawing substituents are described. The in vitro anticancer activities of these molecules tested in the National Cancer Institute's screen of 55 cell lines is described. The compounds tested for topoisomerase I (top1) inhibition is described.

Abstract: Camptothecin compounds which are effective anti-tumor compounds are disclosed. These conjugates inhibit the enzyme topoisomerase I and enhance the stability of the topoisomerase I-DNA cleavable complex.

Abstract: A method and compositions for treating viral infection (IV) vitro and in vivo using a guanosine-rich oligonucleotide. The oligonucleotides have sufficient guanosine to form a guanosine tetrad. Also provided are oligonucleotides of at least two runs of at least two guanosines. Also provided are guanosine-rich oligonucleotides and methods for treating viral infections in humans, and a method for designing guanosine-rich oligonucleotides having anti-viral activity and integrase inhibition activity.

Abstract: Camptothecin and homocamptothecin analogs and derivatives are provided incorporating alkylamine and polyalkylamine moieties.

Abstract: Azatoxin and derivatives thereof are illustrative of a new class of antitumor drugs that are topoisomerase II (top 2) inhibitors. The pharmacophore inhibits the catalytic activity of the purified enzyme but does not unwind relaxed or supercoiled DNA. It is nonintercalative and has at least two domains: a quasi-planar polycyclic ring system, which may bind between DNA base pairs, and a pendant substituent thought to interact with the enzyme, with the DNA grooves or with both. In SV40 and c-myc DNA, azatoxin induces numerous double-strand breaks according to a cleavage pattern which differs from those of known top 2 inhibitors. Azatoxin also is a potent inhibitor of tubulin polymerization.

Abstract: Azatoxin and derivatives thereof are illustrative of a new class of antitumor drugs that are topoisomerase II (top 2) inhibitors. The pharmacophore inhibits the catalytic activity of the purified enzyme but does not unwind relaxed or supercoiled DNA. It is nonintercalative and has at least two domains: a quasi-planar polycyclic ring system, which may bind between DNA base pairs, and a pendant substituent thought to interact with the enzyme, with the DNA grooves or with both. In SV40 and c-myc DNA, azatoxin induces numerous double-strand breaks according to a cleavage pattern which differs from those of known top 2 inhibitors. Azatoxin also is a potent inhibitor of tubulin polymerization.