Abstract: The present invention relates to pyrroloquinolinyl-pyrrole-2,5-dione compounds and pyrroloquinolinyl-pyrrolidine-2,5-dione compounds, and methods of preparation of these compounds. The present invention also relates to pharmaceutical compositions comprising pyrroloquinolinyl-pyrrole-2,5-dione compounds and pyrroloquinolinyl-pyrrolidine-2,5-dione compounds. The present invention provides methods of treating a cell proliferative disorder, such as a cancer, by administering to a subject in need thereof a therapeutically effective amount of a pyrroloquinolinyl-pyrrole-2,5-dione compound or pyrroloquinolinyl-pyrrolidine-2,5-dione compound of the present invention.

Abstract: The present invention relates to pyrroloquinolinyl-pyrrole-2,5-dione compounds and pyrroloquinolinyl-pyrrolidine-2,5-dione compounds, and methods of preparation of these compounds. The present invention also relates to pharmaceutical compositions comprising pyrroloquinolinyl-pyrrole-2,5-dione compounds and pyrroloquinolinyl-pyrrolidine-2,5-dione compounds. The present invention provides methods of treating a cell proliferative disorder, such as a cancer, by administering to a subject in need thereof a therapeutically effective amount of a pyrroloquinolinyl-pyrrole-2,5-dione compound or pyrroloquinolinyl-pyrrolidine-2,5-dione compound of the present invention.

Abstract: Administration of a modulator of cell cycle checkpoint activation, which is preferably ?-lapachone, or a pharmaceutically acceptable salt, prodrug, metabolite, analog or derivative thereof, protects normal cells against radiation injury. The invention includes methods of preventing radiation damage. The invention also provides methods for treating conditions such as cancer with radiotherapy, by administering a modulator of cell cycle checkpoint activation to a subject, prior to administration of radiotherapy.

Abstract: The present invention relates to polymer-modified quinone-containing and carbonyl-containing therapeutic agents, including polymer-modified ?-lapachone compounds, and methods of treating cancer by administering the polymer-modified therapeutic agents to a subject. Polymer-modification of therapeutic agents, such as ?-lapachone compounds, provides effective transport of polymer-modified therapeutic agents to tumor cells or tumor tissues by exploiting the EPR effect in tumor tissues.

Abstract: The invention provides lapachone analogs and derivatives as well as methods of use thereof. These compounds can be used in pharmaceutical compositions for the treatment or prevention of cell proliferation disorders. These compounds can also be used in the treatment or prevention of cancer or precancerous conditions.

Abstract: The present invention provides novel tricyclic spiro-oxathiine naphthoquinone derivatives, a synthetic method for making the derivatives, and the use of the derivatives to induce cell death and/or to inhibit proliferation of cancer or precancerous cells. The naphthoquinone derivatives of the present invention are related to the compound known as ?-lapachone (3,4-dihydro-2,2-dimethyl-2H-naphtho(1,2-b)pyran-5,6-dione).

Abstract: We have discovered that the administration of a G1 and/or S phase drug such as ?-lapachone in combination with a G2/M drug such as a taxane derivative such as paclitaxel resulted in a greater than additive (i.e., synergistic) reduction in the number of tumors (and tumor volume) as compared with the administration of these agents alone. In addition, no signs of toxicity or weight loss were observed. The present invention relates to a method for treating a mammalian tumor using combinations such as a taxane derivative, preferably paclitaxel, and a ?-lapachone, or a derivative or analog thereof.

Abstract: Disclosed herein are novel methods and compositions for Activated Checkpoint Therapy™. Also disclosed are methods of treating cancer and apoptosis-associated disorders using cell cycle checkpoint activation modulators. The invention further discloses methods for screening for cell cycle checkpoint activation modulators and the cell cycle checkpoint activation modulators identified by those screening methods.

Abstract: Disclosed herein are novel methods and compositions for Activated Checkpoint Therapy™. Also disclosed are methods of treating cancer and apoptosis-associated disorders using cell cycle checkpoint activation modulators. The invention further discloses methods for screening for cell cycle checkpoint activation modulators and the cell cycle checkpoint activation modulators identified by those screening methods.

Abstract: Disclosed herein are novel methods and compositions for Activated Checkpoint Therapy™. Also disclosed are methods of treating cancer and apoptosis-associated disorders using cell cycle checkpoint activation modulators. The invention further discloses methods for screening for cell cycle checkpoint activation modulators and the cell cycle checkpoint activation modulators identified by those screening methods.

Abstract: We have surprisingly discovered that the administration of a G1 and/or S phase drug such as &bgr;-lapachone in combination with a G2/M drug such as a taxane derivative such as paclitaxel resulted in an unexpected greater than additive (i.e., synergistic) reduction in the number of tumors (and tumor volume) as compared with the administration of these agents alone. In addition, no signs of toxicity or weight loss were observed. The present invention relates to a method for treating a mammalian tumor using combinations such as a taxane derivative, preferably paclitaxel, and a &bgr;-lapachone, or a derivative or analog thereof.

Abstract: We have surprisingly discovered that the administration of a G1 and/or S phase drug such as &bgr;-lapachone in combination with a G2/M drug such as a taxame derivative such as paclitaxel resulted in an unexpected greater than additive (i.e., synergistic) reduction in the number of tumors (and tumor volume) as compared with the administration of these agents alone. In addition, no signs of toxicity or weight loss were observed. The present invention relates to a method for treating a mammalian tumor using combinations such as a taxane derivative, preferably paclitaxel, and a &bgr;-lapachone, or a derivative or analog thereof.

Abstract: We have now discovered that unexpectedly compounds of the following formulae I or 11 can be used to selectively stimulate the death of mammalian prostate cells, including both epithelial cell and prostate cancer cells, and thus are useful in treating prostate diseases: wherein R and R1 are each independently selected from the group consisting of hydrogen, hydroxy, thio (SH), halogen, substituted and unsubstituted alkyl, substituted and unsubstituted alkenyl, substituted and unsubstituted aryl, and substituted and unsubstituted alkoxy, and salts thereof, wherein the dotted double bond between the ring carbons to which R and R1 are bonded represent an optional ring double bond. Preferred compounds of formula I include those in which at least one of the substituents R and R1 is hydrogen and/or at least one of said substituents is allyl. Specifically preferred compounds include &bgr;-lapachone (i.e., R and R1 both being hydrogen), allyl-&bgr;-lapachone, particularly 3-allyl-&bgr;-lapachone (i.e.