7-Ethyl-10-hydroxycamptothecin

7-Ethyl-10-hydroxycamptothecin: a potent topoisomerase I inhibitor
7-Ethyl-10-hydroxycamptothecin (SN-38), as a highly active topoisomerase (Topo) I inhibitor, is the active metabolic product of its prodrug irinotecan (CPT-11) commercially available as Camptosar. By combining with the Topo I-DNA covalent conjugate, the camptothecin analogue forms a ternary complex that blocks the repolymerization of the DNA strands during their replication, eventually leading to the cell apoptosis. Although SN-38 is about 100- to 1000-fold more potent than irinotecan, its clinical application is limited by its poor solubility and nonspecific toxicity[1].

ChEBI: LSM-6189 is a pyranoindolizinoquinoline.

[1] Shuangxi Liu. “Co-Prodrugs of 7-Ethyl-10-hydroxycamptothecin and Vorinostat with in Vitro Hydrolysis and Anticancer Effects.” ACS Omega 5 1 (2019): 350–357.