A compound of the following formula: wherein R 1 is -H, -OH, C 1-6 alkyl, C 1-6 alkoxyl, C 3-10 cycloalkyl, C 1-10 heterocycloalkyl, aryl, heteroaryl, or -NH-Z-R; in which R is H, or is a moiety selected from C 1-6 alkyl, C 3-10 cycloalkyl, C 1-10 heterocycloalkyl, aryl, and heteroaryl, each of which is optionally mono-, di-, or tri-substituted with halo, nitro, cyano, amino, C 1-6 alkyl, C 1-6 alkoxyl, C 2-6 alkenyl, C 2-6 alkynyl, aryl, or heteroaryl; and Z is -C -, -C O-, -C C O-, -C C NH-, -C NR'-, -OC -, - C NR'-, or -C O-, R' being H, C 1-6 alkyl, C 3-10 cycloalkyl, C 1-10 heterocycloalkyl, aryl, or heteroaryl; R 2 is H, or is a moiety selected from C 1-6 alkyl, C 3-10 cycloalkyl, C 1-10 heterocycloalkyl, aryl, and heteroaryl, each of which is optionally mono-, di-, or tri-substituted with halo, nitro, cyano, amino, C 1-6 alkyl, C 1-6 alkoxyl, C 2-6 alkenyl, C 2-6 alkynyl, aryl, or heteroaryl; A is N or CH; U is -O-, -NH-, -NH -, -NHSO-, or -NHSO 2 -; W is -(CH 2) m -, -NH(CH 2) n -, -(CH 2) n NH-, -O(CH 2) n -, -(CH 2) n O-, -S(CH 2) n -, -(CH 2) n S-, -SO-, -SO(CH 2) n -, -(CH 2) n SO-, -SO 2 (CH 2) n -, or -(CH 2) n SO 2 -, m being 1, 2, or 3 and n being 0, 1, or 2; X is -O-, -S-, or -NH-,; and Y is in which each of V and T, independently, is -CH- or -N-; each of A 1 and A 2, independently, is a moiety selected from C 4-10 cycloalkyl, C 1-10 heterocycloalkyl, aryl, and heteroaryl, each of which is optionally mono-, di-, or tri-substituted with halo, nitro, cyano, amino, C 1-6 alkyl, C 1-6 alkoxyl, C 2-6 alkenyl, C 2-6 alkynyl, aryl, or heteroaryl, or optionally fused with C 3-10 cycloalkyl, C 2-10 heterocycloalkyl, aryl, or heteroaryl; and R i is H, halo, nitro, cyano, or amino, or is a moiety selected from C 1-6 alkyl, C 1-6 alkoxyl, C 2-6 alkenyl, C 2-6 alkynyl, C 3-10 cycloalkyl, C 1-10 heterocycloalkyl, aryl, and heteroaryl, each of C 1-6 alkyl, C 1-6 alkoxyl, C 2-6 alkenyl, and C 2-6 alkynyl being optionally mono-, di-, or tri-substituted with halo, nitro, cyano, amino, C 1-6 alkyl, C 1-6 alkoxyl, C 2-6 alkenyl, C 2-6 alkynyl, C 3-10 cycloalkyl, C 1-10 heterocycloalkyl, aryl, or heteroaryl, and each of C 3-10 cycloalkyl, C 1-10 heterocycloalkyl, aryl, and heteroaryl being optionally mono-, di-, or tri-substituted with halo, nitro, cyano, amino, C 1-6 alkyl, C 1-6 alkoxyl, C 2-6 alkenyl, C 2-6 alkynyl, C 3-10 cycloalkyl, C 1-10 heterocycloalkyl, aryl, or heteroaryl, or optionally fused with C 3-10 cycloalkyl, C 1-10 heterocycloalkyl, aryl, or heteroaryl. R 1 is -H, -OH, C 1-6 alkyl, C 1-6 alkoxyl, C 3-10 cycloalkyl, C 1-10 heterocycloalkyl, aryl, heteroaryl, or -NH-Z-R; in which R is H, or is a moiety selected from C 1-6 alkyl, C 3-10 cycloalkyl, C 1-10 heterocycloalkyl, aryl, and heteroaryl, each of which is optionally mono-, di-, or tri-substituted with halo, nitro, cyano, amino, C 1-6 alkyl, C 1-6 alkoxyl, C 2-6 alkenyl, C 2-6 alkynyl, aryl, or heteroaryl; and Z is -C -, -C O-, -C C O-, -C C NH-, -C NR'-, -OC -, - C NR'-, or -C O-, R' being H, C 1-6 alkyl, C 3-10 cycloalkyl, C 1-10 heterocycloalkyl, aryl, or heteroaryl; R 2 is H, or is a moiety selected from C 1-6 alkyl, C 3-10 cycloalkyl, C 1-10 heterocycloalkyl, aryl, and heteroaryl, each of which is optionally mono-, di-, or tri-substituted with halo, nitro, cyano, amino, C 1-6 alkyl, C 1-6 alkoxyl, C 2-6 alkenyl, C 2-6 alkynyl, aryl, or heteroaryl; A is N or CH; U is -O-, -NH-, -NH -, -NHSO-, or -NHSO 2 -; W is -(CH 2) m -, -NH(CH 2) n -, -(CH 2) n NH-, -O(CH 2) n -, -(CH 2) n O-, -S(CH 2) n -, -(CH 2) n S-, -SO-, -SO(CH 2) n -, -(CH 2) n SO-, -SO 2 (CH 2) n -, or -(CH 2) n SO 2 -, m being 1, 2, or 3 and n being 0, 1, or 2; X is -O-, -S-, or -NH-,; and Y is in which each of V and T, independently, is -CH- or -N-; each of A 1 and A 2, independently, is a moiety selected from C 4-10 cycloalkyl, C 1-10 heterocycloalkyl, aryl, and heteroaryl, each of which is optionally mono-, di-, or tri-substituted with halo, nitro, cyano, amino, C 1-6 alkyl, C 1-6 alkoxyl, C 2-6 alkenyl, C 2-6 alkynyl, aryl, or heteroaryl, or optionally fused with C 3-10 cycloalkyl, C 2-10 heterocycloalkyl, aryl, or heteroaryl; and R i is H, halo, nitro, cyano, or amino, or is a moiety selected from C 1-6 alkyl, C 1-6 alkoxyl, C 2-6 alkenyl, C 2-6 alkynyl, C 3-10 cycloalkyl, C 1-10 heterocycloalkyl, aryl, and heteroaryl, each of C 1-6 alkyl, C 1-6 alkoxyl, C 2-6 alkenyl, and C 2-6 alkynyl being optionally mono-, di-, or tri-substituted with halo, nitro, cyano, amino, C 1-6 alkyl, C 1-6 alkoxyl, C 2-6 alkenyl, C 2-6 alkynyl, C 3-10 cycloalkyl, C 1-10 heterocycloalkyl, aryl, or heteroaryl, and each of C 3-10 cycloalkyl, C 1-10 heterocycloalkyl, aryl, and heteroaryl being optionally mono-, di-, or tri-substituted with halo, nitro, cyano, amino, C 1-6 alkyl, C 1-6 alkoxyl, C 2-6 alkenyl, C 2-6 alkynyl, C 3-10 cycloalkyl, C 1-10 heterocycloalkyl, aryl, or heteroaryl, or optionally fused with C 3-10 cycloalkyl, C 1-10 heterocycloalkyl, aryl, or heteroaryl.