Derivative of sarsasapogenin, pharmaceutical composition and use thereof
AssigneePhytovent Biopharma
InventorsShawn Mu, Na Wang
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Abstract
A derivative of sarsasapogenin is provided having a structure of formula I, A pharmaceutical composition of the aforementioned derivative of sarsasapogenin and use thereof are also provided. By systematic modification and derivatization of sarsasapogenin structure in combination with inhibitory activity assays on tumor cells, many derivative compounds are provided that have excellent inhibitory activity on tumor cells, particularly high inhibitory activity on the growth of various brain tumor cells, having potential wide application and tremendous value in treating various cancers.
Claims11
A derivative of sarsasapogenin having a structure of formula I,
- wherein, Z is selected from a monoheterocyclyl, a diheterocyclyl, and NR1R2, the monoheterocyclyl or diheterocyclyl containing one or two heteroatoms selected from sulfur, oxygen, NH and NRa;
- R1 and R2 are each independently selected from hydrogen and substituted or unsubstituted C1-C10 alkyl, or together form a 3-8 membered ring containing one or more substituents selected from C1-C10 alkyl, C3-C10 cycloalkyl, C6-C20 aryl, C3-C14 heteroaryl, halogen, hydroxyl, amino, nitro, cyano, formyl, carboxyl, alkoxy, —CF3, —SF5 and 3-8 membered heterocyclyl containing one or more heteroatoms selected from sulfur, oxygen, NH and NRa;
- X is selected from C(Rb)(Rc), C(O), and S(O)2, Rb and Rc together form a 3-8 membered carbocyclyl or a 3-8 membered heterocyclyl containing one or more heteroatoms selected from sulfur, oxygen, N, NH and NRa, the 3-8 membered carbocyclyl or the 3-8 membered heterocyclyl being optionally substituted with one or more substituents selected from C1-C10 alkyl, C3-C10 cycloalkyl, C6-C20 aryl, C3-C14 heteroaryl, halogen, hydroxyl, amino, nitro, cyano, formyl, carboxyl, alkoxy, —CF3, —SF5 and 3-8 membered heterocyclyl containing one or two heteroatoms selected from O, S and NRa;
- Y is selected from C(Rd)(Re), C(O), and S(O)2, and Rd and Re together form a 3-8 membered ring or a 3-8 membered heterocyclyl containing one or two heteroatoms selected from sulfur, oxygen, NH and NRa;
- Ra, Rb, Rc, Rd and Re are independently selected from C1-C10 alkyl, C3-C10 cycloalkyl, C6-C20 aryl and C3-C14 heteroaryl optionally substituted with at least one substituent selected from halogen, hydroxyl, amino, nitro, cyano, formyl, carboxyl, alkoxy, —CF3, and —SF5;
- X is C(Rb)(Rc), Y is C(Rd)(Re), and Rb and Rd are connected through a chemical bond;
- n is an integer selected from 0 to 10;
- and
- m is selected from 0 and 1.
Dependencies are inferred from the claim text.