BO-2239

BO-2239 is a novel small molecule indolizino[8,7-b]indole hybrid developed by researchers at Academia Sinica for the treatment of small cell lung cancer (SCLC). It is synthesized by fusing β-carboline and bis(hydroxymethyl)pyrrole moieties. BO-2239 exhibits a dual mechanism of action, functioning as a potent inhibitor of DNA topoisomerase II and an inducer of DNA cross-linking. Preclinical studies have shown that the compound effectively inhibits the growth of SCLC cell lines (such as H526 and H211) by inducing G2/M phase cell cycle arrest and triggering apoptosis. In vivo, BO-2239 has demonstrated significant antitumor activity in SCLC xenograft models, showing potency comparable to irinotecan and superior to cisplatin.