HIV-1 integrase inhibitor 8

Names

[ Name ]:
HIV-1 integrase inhibitor 8

[Synonym ]:
2,2',3,3'-Tetrahydro-3,3,3',3'-tetramethyl-1,1'-spirobi<1H-indene>-6,6'-diol
6,6'-dihydroxy-3,3,3',3'-tetramethyl-1,1'-spirobisindane
(2,2,3,3-tetrafluoropropoxy)acetic acid
6,6'-dihydroxy-3,3,3',3'-tetramethyl-1,1'-spirobiindane
2,2,3,3-Tetrafluor-propyloxy-essigsaeure
3,3,3',3'-tetramethyl-1,1'-spirobisindane-6,6'-diol
6,6'-dihydroxy-3,3,3',3'-tetramethyl-1,1'-spirobiindan
SPIROBIINDANE

Biological Activity

[Description]:

HIV-1 integrase inhibitor 8 is a HIV-1 integrase inhibitor, compound 8[1].

[Related Catalog]:

Research Areas >> Infection

Signaling Pathways >> Metabolic Enzyme/Protease >> HIV Integrase

[In Vitro]

HIV-1 integrase inhibitor 8 is against 3′-processing (TC) and strand-transfer (ST) activities in the presence of Mn2+ as the cationic cofactor by gel assay with IC50 values of 275 µM and 200 µM, respectively. It inhibits the strand-transfer (ST) activity with an IC50 value of 200 µM[1]. The DNA relaxation activity of MCV topoisomerase is monitored by gel electrophoresis, while DNA cleavage and religation activities were monitored using a microtiter assay. HIV-1 integrase inhibitor 8 inhibits MCV topoisomerase and DNA religation with IC50 values of 500 µM and 200 µM, respectively. This result demonstrates that compound 8 is inactive against topoisomerase in both assays[1]. HIV-1 integrase inhibitor 8 induces cell cytotoxicity and yields a LD50 (dose at which the signal is reduced 50% due to cell death) of 20 μM in HeLa cells[1].

[References]

[1]. Molteni, et al. A New Class of HIV-1 Integrase Inhibitors: The 3,3,3', 3'-tetramethyl-1,1'-spirobi(indan)-5,5',6,6'-tetrol Family.J Med Chem

Chemical & Physical Properties

[ Density]:
1.21±0.1 g/cm3(Predicted)

[ Boiling Point ]:
478.5℃ at 760 mmHg

[ Melting Point ]:
213-214 °C

[ Molecular Formula ]:
C₂₁H₂₄O₂

[ Molecular Weight ]:
308.41400

[ Flash Point ]:
220.4℃

[ Exact Mass ]:
308.17800

[ PSA ]:
40.46000

[ LogP ]:
4.74650

[ Vapour Pressure ]:
8.84E-10mmHg at 25°C

Safety Information

[ HS Code ]:
2906299090

Synthetic Route

Click to get detail synthetic route

Precursor & DownStream

Precursor

DownStream

Customs

[ HS Code ]: 2906299090

[ Summary ]:
2906299090 other aromatic alcohols。Supervision conditions:None。VAT:17.0%。Tax rebate rate:9.0%。MFN tariff:5.5%。General tariff:30.0%