LL01

LL01 is a small molecule tubulin polymerization inhibitor, specifically targeting the colchicine binding site of tubulin. It was rationally designed as an indenoprazole derivative, chemically described as 2-(6-ethoxy-3-(3-ethoxyphenylamino)-1-methyl-1,4-dihydroindeno[1,2-c]pyrazol-7-yloxy)acetamide. LL01 exhibits potent antiproliferative activity against a variety of tumor cell lines, including those with multidrug resistance, and inhibits tumor growth in hepatocellular carcinoma xenograft models more effectively than sorafenib. LL01 is not a P-glycoprotein substrate and displays acceptable pharmacokinetic properties in rat models, with oral bioavailability of about 41%.