Aim: Our previous study indicated that betulinic acid (BA) could inhibit lung cancer formation via inhibiting Sp1 level.Herein we try to screen BA derivative(s),which is more effective than BA itself.Methods: Various BA derivatives were used to treat the lung cancer cell lines at first to evaluate the therapeutic effect of these compounds, and then used the compound(s) effected in the cellular level to do the animal experiments including the xenograph and spontaneous induced lung cancer animal.Finally, the therapeutic molecular mechanism of the BAderivative in lung cancer will be addressed.