BO-1012

BO-1012 is a synthetic bifunctional alkylating agent belonging to the 3a-aza-cyclopenta[a]indene derivative class. It exerts its antineoplastic activity by inducing DNA interstrand cross-links (ICLs), which results in significant G2/M cell cycle arrest and the induction of apoptosis. Preclinical studies have highlighted its potential in treating various malignancies, including lung cancer, prostate cancer, and cisplatin-resistant bladder carcinoma. Notably, its efficacy is enhanced when combined with arsenic trioxide (ATO), which impairs the DNA repair response—specifically by inhibiting Rad51 translocation through the suppression of AKT signaling—thereby sensitizing tumor cells to BO-1012-induced genomic damage.

Other names

3a-aza-cyclopenta[a]indene derivative