Academia Sinica

Memorial Sloan Kettering Cancer Center

Te-Chang Lee

Tsann-Long Su

Ting-Chao Chou

Malcolm A Moore

Tai-Lin Chen

Jae-Hung Shieh

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), wherein, optionally substituted with one or more substituents independently selected from the group consisting of halo, alkyl, haloalkyl, alkenyl, C(O)H, OH, O(alkyl), O(CO)alkyl, O(aryl), aryl, and &#x2014;O(CH)N(R);

Substituted pyrrolo[2,1-a]phthalazines and benzo[g]pyrrolo[2,1-a]phthalazines for the treatment of cancer

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.

Use of ureidomustine (BO-1055) in cancer treatment

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.

Method of treating cancer using combination of a bifunctional alkylating agent and DNA repair inhibitors

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.

Growing community of inventors

Taipei, Taiwan

Te-Chang Lee