Described herein are markers, conjugates, compositions and methods for hypoxia imaging, mapping, and therapy. A compound comprising bio-reductively activated (BA) arm,
linker arm and a mapping click wherein BA contains one for more of substituted or unsubstituted 2 / 4 / 5-substituted nitroimidazoles, or substituted benzotriazene-1,4-dioxides, or substituted 1,2,3 / 1,2,4-triazoles, or substituted 1,4-benzoquinones, or a combination of two homo-or hetero BA moieties, wherein
linker arm contains C1-16
alkane,
alkene,
alkyne, alicyclic or aromatic linkers with or without hetero atoms as in ethers, amine, esters, acid, amides, 5 and 6 membered
sugar sings with the substitution as described above, both monosaccharides and disaccharides, wherein mapping click contains one of substituted or unsubstituted —N3-, CN, SCN, substituted alkynes for
click chemistry. Said compound undergoes in situ click reaction after its distribution in cells or tissues to link to a reporting group which may be unchelated or chelated with a
metal-radioactive or non-radioactive-, or a radiohalogen for PET / SPECT, or a dye for fluorescent / optical reporting group, thus accomplishing hypoxia imaging.