Hypoxia-targeted drug delivery

Abstract

Hypoxia is a state of low oxygen tension found in numerous solid tumours.

Recent advances in construction of small molecule-based fluorophore-drug conjugates

“…Azo bond, nitroaromatic heterocyclics (nitrobenzyl, nitrofuran, etc. ), trimethyl-locked quinone systems and indolequinone can all be dubbed as hypoxia-sensitive linkers [ [55] , [56] , [57] ]. The Kim group [ 58 ] developed a hypoxia-response N , N -bis(2-chloroethyl)-1,4-benzene-diamine prodrug 9 ( Fig.…”

Molecular recognition of pyrazine N,N′-dioxide using aryl extended calix[4]pyrroles

“…1 In this context, efforts have been made to synthesise derivatives of quinoxaline 1,4-di-N-oxides and phenazine N,N 0 -dioxides and study their biological activities. 2,3 Notably, pyrazine N,N 0 -dioxide (PZDO) is the redox-active motif embedded in these two types of heterocyclic N-oxides and is thought to account for the antitumoral activities towards hypoxic cells. Creating articial receptors for PZDO and its analogues might inform the development of improved supramolecular drug delivery systems and sensors for this class of biologically active species.…”

Pro-organic radical contrast agents (“pro-ORCAs”) for real-time MRI of pro-drug activation in biological systems

“…[10][11][12][13][14][15][16][17][18][19][20][21][22][23][24] "Smart" or "reporter" theranostics that leverage their imaging component to elucidate material-disease tissue interactions such as drug release kinetics, efficacy, or acquired therapeutic resistance are especially powerful. 3,[25][26][27][28] Elegant work using fluorescence-or FRET-based reporters of cellular apoptosis or drug release within the tumor microenvironment have been developed. [29][30][31][32][33][34][35][36] Despite the highly innovative nature of these approaches and their immense utility as research tools, the translational potential of fluorescence imaging may be limited by light penetration depth and tissue autofluorescence.…”