2a-B

2a-B is a synthetic, symmetric curcuminoid derivative featuring a boron difluoride (BF2) complexed beta-diketone moiety and 2-(morpholin-4-yl)ethoxy substitutions at the 4-position of the phenyl rings. Developed to address the poor bioavailability and instability of natural curcumin, 2a-B exhibits enhanced water solubility and photostability. In preclinical studies, it demonstrated potent cytotoxic activity against human bladder cancer cell lines, including 5637 (grade II carcinoma) and SCaBER (squamous cell carcinoma), with IC50 values in the low micromolar range (1.2 µM and 2.2 µM, respectively). Its mechanism of action is characterized by microtubule targeting and potentially lysosome-specific accumulation due to the basicity of the morpholine groups, which protonate in acidic environments.

Other names

4-(2-{4-[(1E)-2-{2,2-difluoro-6-[(1E)-2-{3-methoxy-4-[2-(morpholin-4-yl)ethoxy]phenyl}ethenyl]-1,3,2-dioxaborinin-4-yl}ethenyl]-2-methoxyphenoxy}ethyl)morpholineBF2-complexed morpholinated curcuminoidBF-2-complexed morpholinated curcuminoidBF 2-complexed morpholinated curcuminoid