Abstract: Disclosed herein are novel bifunctional compounds and their uses for the treatment and/or prophylaxis of cancers.

Abstract: Disclosed herein are novel bifunctional compounds and their uses for the treatment and/or prophylaxis of cancers. The bifunctional compound disclosed herein has the structure of formula (I).

Abstract: Method of using ureidomustine (BO-1055), a water-soluble NDA cross-linking agent, in the treatment of small lung cell carcinoma (SCLC).

Abstract: Method of using ureidomustine (BO-1055), a water-soluble NDA cross-linking agent, in the treatment of a cancer, selected from the group consisting of various types of human leukemia [such as acute myeloid leukemia (ALL) and acute B Lymphoblastic leukemia (B-ALL)], lymphomas, small lung cell carcinoma (SCLC), sarcomas, and others.

Abstract: A method for treating small cell lung cancer (SCLC). In the method, a therapeutically effective amount of a compound of Formula I: wherein R1, R2 and R3 have the definitions disclosed in the specification is administered alone or in combination with one or more anticancer agents, or surgery, radiation therapy, chemotherapy, and/or targeted therapy.

Abstract: Method of using ureidomustine (BO-1055), a water-soluble NDA cross-linking agent, in the treatment of a cancer, selected from the group consisting of various types of human leukemia [such as acute myeloid leukemia (ALL) and acute B Lymphoblastic leukemia (B-ALL)], lymphomas, small lung cell carcinoma (SCLC), sarcomas, and others.

Abstract: Compounds, pharmaceutical compositions, and methods for treating anemia ?-thalassemia anemia or sickle cell anemia.

Abstract: Compounds, pharmaceutical compositions, and methods for treating anemia (?-thalassemia anemia or sickle cell anemia.

Abstract: Compounds, pharmaceutical compositions, and methods for treating anemia ?-thalassemia anemia or sickle cell anemia.

Abstract: The present disclosure relates to new DNA-directed alkylating agents and water-soluble N-mustard agents with improved chemical stability and anti-tumor therapeutic efficacy.

Abstract: A pharmaceutical composition for treating cancer, in particular drug resistant cancer, comprising an effective amount of bifunctional alkylating agent, an effective amount of a DNA repair inhibitor, and a pharmaceutically acceptable carrier.

Abstract: The present invention provides a series of 2,3-bis(hydroxymethyl)-4H-benzo[d]pyrrolo-[1,2-a]thiazoles and 1,2-bis(hydroxymethyl)indolizino[6,7-b]indole derivatives and their bis(alkylcarbamates) derivatives. These derivatives were designed as bi-functional DNA cross-linking agents. The in vitro cytotoxicity study of these compounds revealed that they exhibit significant anti-proliferative activity in inhibiting human lymphoblastic leukemia and various solid tumor cell growth. The compounds also exhibit therapeutic efficacy against human breast carcinoma and lung cancer in xenograft model. The compounds generally possess potent antitumor activity to kill various human solid tumors and have high potential for clinical applications.

Abstract: A pharmaceutical composition for treating cancer, in particular drug resistant cancer, comprising an effective amount of bifunctional alkylating agent, an effective amount of a DNA repair inhibitor, and a pharmaceutically acceptable carrier.

Abstract: The present disclosure relates to new DNA-directed alkylating agents and water-soluble N-mustard agents with improved chemical stability and anti-tumor therapeutic efficacy.

Abstract: The present invention provides a series of 2,3-bis(hydroxymethyl)-4H-benzo[d]pyrrolo-[1,2-a]thiazoles and 1,2-bis(hydroxymethyl)indolizino[6,7-b]indole derivatives and their bis(alkylcarbamates) derivatives. These derivatives were designed as bi-functional DNA cross-linking agents. The in vitro cytotoxicity study of these compounds revealed that they exhibit significant anti-proliferative activity in inhibiting human lymphoblastic leukemia and various solid tumor cell growth. The compounds also exhibit therapeutic efficacy against human breast carcinoma and lung cancer in xenograft model. The compounds generally possess potent antitumor activity to kill various human solid tumors and have high potential for clinical applications.

Abstract: The present disclosure relates to a series of bis(hydroxymethyl) and its bis(carbamate) of 8H-3a-azacyclopenta[a]indene-1-yl and 5,10-dihydropyrrolo-[1,2-b]isoquinolines derivatives (Formula I-Formula IV) as DNA di-alkylating agents. The preliminary antitumor studies indicated that compounds disclosed herein could exhibit potent cytotoxicity in vitro and antitumor therapeutic efficacy in human tumor xenografts and could have little or no cross-resistance to either Taxol or Vinblastine. The results demonstrated that compounds disclosed herein possess potent antitumor therapeutic efficacy and are expected to have potential for clinical applications.

Abstract: New aniline or phenol N-mustards linked to DNA-affinity carriers (such as 9-anilinoacridines, acridines and quinolines), aminobenzamides or aminophenol ethers by a urea, carbamic acid, carbanic acid ester, hydrazineurea, hydrazinecarbamic acid ester, phenoxyurea, phenoxycarbamic acid ester linkage with improved chemical stability and anti-tumor therapeutic efficacy are provided.

Abstract: The present disclosure relates to a series of bis(hydroxymethyl) and its bis(carbamate) of 8H-3a-azacyclopenta[a]indene-1-yl and 5,10-dihydropyrrolo-[1,2-b]isoquinolines derivatives (Formula I-Formula IV) as DNA di-alkylating agents. The preliminary antitumor studies indicated that compounds disclosed herein could exhibit potent cytotoxicity in vitro and antitumor therapeutic efficacy in human tumor xenografts and could have little or no cross-resistance to either Taxol or Vinblastine. The results demonstrated that compounds disclosed herein possess potent antitumor therapeutic efficacy and are expected to have potential for clinical applications.

Abstract: This invention relates to 9-anilinoacridine alkylating agents, their synthesis and their use in pharmaceutical compositions for treating diseases.

Abstract: New aniline or phenol N-mustards linked to DNA-affinity carriers (such as 9-anilinoacridines, acridines and quinolines), aminobenzamides or aminophenol ethers by a urea, carbamic acid, carbanic acid ester, hydrazineurea, hydrazinecarbamic acid ester, phenoxyurea, phenoxycarbamic acid ester linkage with improved chemical stability and anti-tumor therapeutic efficacy are provided.