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BO-1392 is a preclinical-stage DNA-directed alkylating agent developed by Academia Sinica. Chemically, it is an N-mustard-quinoline conjugate bearing a hydrazinecarboxamide linker. This design aims to enhance DNA-specific cross-linking and reduce the chemical reactivity of the nitrogen mustard warhead, thereby improving plasma stability and half-life. In preclinical studies, BO-1392 demonstrated significant in vitro cytotoxicity against human lymphoblastic leukemia (CCRF-CEM) and various solid tumor cell lines (including breast, colon, lung, prostate, and ovarian cancers). In animal models, BO-1392 induced complete tumor remission in human breast carcinoma MX-1 xenografts and significantly suppressed the growth of human ovarian SK-OV3 xenografts with relatively low toxicity.
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