Zosuquidar

Zosuquidar

File:Zosuquidar.svg
Identifiers
IUPAC name (2R)-1-{4-[(1aR,6r,10bS)-1,1-difluoro-1,1a,6,10b- tetrahydrodibenzo[a,e]cyclopropa[c]cyclohepten-6-yl] piperazin-1-yl}-3-(quinolin-5-yloxy)propan-2-ol
CAS Number	167354-41-8
PubChem CID	153997
E number	{{#property:P628}}
ECHA InfoCard	{{#property:P2566}}
Chemical and physical data
Formula	C32H31F2N3O2
Molar mass	527.61 g/mol
3D model (JSmol)	Interactive image
SMILES C1CN(CCN1C[C@H](COC2=CC=CC3=C2C=CC=N3)O)C4C5=CC=CC=C5[C@H]6[C@H](C6(F)F)C7=CC=CC=C47.Cl.Cl.Cl

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Overview

Zosuquidar is a compound of antineoplastic drug candidates currently under development. It is now in "Phase 3" of clinical tests in the United States. Its action mechanism consists of the inhibition of P-glycoproteins; other drugs with this mechanism include tariquidar and laniquidar. P-glycoproteins are proteins which convert the energy derived from the hydrolysis of ATP to structural changes in protein molecules, in order to perform coupling, thus discharging medicine from cells. If P-glycoprotein coded with the MDR1 gene manifests itself in cancer cells, it discharges much of the antineoplastic drugs from the cells, making cancer cells medicine tolerant, and rendering antineoplastic drugs ineffective. This protein also manifests itself in normal organs not affected by the cancer (such as the liver, small intestine, and skin cells in blood vessels of the brain), and participates in the transportation of medicine. The compound Zosuquidar inhibits this P-glycoprotein, causing the cancer cells to lose their medicine tolerance, and making antineoplastic drugs effective.