Lead optimization focusing on oral bioavailabilityled to the discovery of compound 25, a N-acyl prodrugof 13, which demonstrated improved oral availabilityand excellent NCI-H446 SCLC xenografted tumor regression in mice.These results support the potential of 25 for furtherdevelopment as an anticancer drug targeting MYC-amplifiedmalignancies such as SCLC. Here, MYC is linked to small cell lung carcinoma.