Apoptozole

Apoptozole
Clinical data
Trade names	Apoptozole
Identifiers
	IUPAC name 4-[[2-[3,5-bis(trifluoromethyl)phenyl]-4,5-bis(4-methoxyphenyl)imidazol-1-yl]methyl]benzamide;
CAS Number	1054543-47-3 ;
PubChem CID	24894064;
ChemSpider	29340758;
UNII	WD0EH16QCD;
ChEMBL	ChEMBL3416503;
CompTox Dashboard (EPA)	DTXSID201027756 ;
Chemical and physical data
Formula	C33H25F6N3O3
Molar mass	625.571 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES COC1=CC=C(C=C1)C2=C(N(C(=N2)C3=CC(=CC(=C3)C(F)(F)F)C(F)(F)F)CC4=CC=C(C=C4)C(=O)N)C5=CC=C(C=C5)OC;
	InChI InChI=1S/C33H25F6N3O3/c1-44-26-11-7-20(8-12-26)28-29(21-9-13-27(45-2)14-10-21)42(18-19-3-5-22(6-4-19)30(40)43)31(41-28)23-15-24(32(34,35)36)17-25(16-23)33(37,38)39/h3-17H,18H2,1-2H3,(H2,40,43); Key:ZIMMTPFXOMAJTQ-UHFFFAOYSA-N;

Apoptozole is a drug that acts as a potent and selective inhibitor of the heat shock protein Hsp70, and was one of the first compounds developed to act at this target. It induces apoptosis in susceptible cells, and displays anti-cancer, anti-malarial and antiviral activity. The promising results in animal studies makes it likely that either apoptozole or compounds with similar modes of action will be further researched as potential therapeutics in the future.^[1]^[2]^[3]^[4]^[5]

References

^ Ko SK, Kim J, Na DC, Park S, Park SH, Hyun JY, et al. (March 2015). "A small molecule inhibitor of ATPase activity of HSP70 induces apoptosis and has antitumor activities". Chemistry & Biology. 22 (3): 391–403. doi:10.1016/j.chembiol.2015.02.004. PMID 25772468.
^ Park SH, Kim WJ, Li H, Seo W, Park SH, Kim H, et al. (June 2017). "Anti-leukemia activity of a Hsp70 inhibitor and its hybrid molecules". Scientific Reports. 7 (1): 3537. Bibcode:2017NatSR...7.3537P. doi:10.1038/s41598-017-03814-6. PMC 5471252. PMID 28615625.
^ Chen Y, Murillo-Solano C, Kirkpatrick MG, Antoshchenko T, Park HW, Pizarro JC (July 2018). "Repurposing drugs to target the malaria parasite unfolding protein response". Scientific Reports. 8 (1): 10333. Bibcode:2018NatSR...810333C. doi:10.1038/s41598-018-28608-2. PMC 6037779. PMID 29985421.
^ Park SH, Baek KH, Shin I, Shin I (October 2018). "Subcellular Hsp70 Inhibitors Promote Cancer Cell Death via Different Mechanisms". Cell Chemical Biology. 25 (10): 1242–1254.e8. doi:10.1016/j.chembiol.2018.06.010. PMID 30057298.
^ Yang J, Xu Y, Yan Y, Li W, Zhao L, Dai Q, et al. (February 2020). "Small Molecule Inhibitor of ATPase Activity of HSP70 as a Broad-Spectrum Inhibitor against Flavivirus Infections". ACS Infectious Diseases. 6 (5): 832–843. doi:10.1021/acsinfecdis.9b00376. PMID 31967789.

[1] Ko SK, Kim J, Na DC, Park S, Park SH, Hyun JY, et al. (March 2015). "A small molecule inhibitor of ATPase activity of HSP70 induces apoptosis and has antitumor activities". Chemistry & Biology. 22 (3): 391–403. doi:10.1016/j.chembiol.2015.02.004. PMID 25772468.

[2] Park SH, Kim WJ, Li H, Seo W, Park SH, Kim H, et al. (June 2017). "Anti-leukemia activity of a Hsp70 inhibitor and its hybrid molecules". Scientific Reports. 7 (1): 3537. Bibcode:2017NatSR...7.3537P. doi:10.1038/s41598-017-03814-6. PMC 5471252. PMID 28615625.

[3] Chen Y, Murillo-Solano C, Kirkpatrick MG, Antoshchenko T, Park HW, Pizarro JC (July 2018). "Repurposing drugs to target the malaria parasite unfolding protein response". Scientific Reports. 8 (1): 10333. Bibcode:2018NatSR...810333C. doi:10.1038/s41598-018-28608-2. PMC 6037779. PMID 29985421.

[4] Park SH, Baek KH, Shin I, Shin I (October 2018). "Subcellular Hsp70 Inhibitors Promote Cancer Cell Death via Different Mechanisms". Cell Chemical Biology. 25 (10): 1242–1254.e8. doi:10.1016/j.chembiol.2018.06.010. PMID 30057298.

[5] Yang J, Xu Y, Yan Y, Li W, Zhao L, Dai Q, et al. (February 2020). "Small Molecule Inhibitor of ATPase Activity of HSP70 as a Broad-Spectrum Inhibitor against Flavivirus Infections". ACS Infectious Diseases. 6 (5): 832–843. doi:10.1021/acsinfecdis.9b00376. PMID 31967789.

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