62067-29-2
Chemical Structure
Bromotetrandrine
Synonym(s): 5-Bromotetrandrine; BrTet; W198
- CAS No.: 62067-29-2
- Formula:C38H41BrN2O6
- Molecular Weight:701.65
IUPAC Name: (11S,31S)-35-bromo-16,36,37,54-tetramethoxy-12,32-dimethyl-11,12,13,14,31,32,33,34-octahydro-2,6-dioxa-1(7,1),3(8,1)-diisoquinolina-5(1,3),7(1,4)-dibenzenacyclooctaphane
InChIKey: ANJMFZGRGHQXMA-VMPREFPWSA-N
SMILES: COC1=C2C3=C(CCN([C@@]3([H])CC4=CC=C(OC)C(OC5=CC=C(C[C@@]6([H])C7=CC(O2)=C(C=C7CCN6C)OC)C=C5)=C4)C)C(Br)=C1OC
Biological Activity: Bromotetrandrine is a potent inhibitor of P-glycoprotein (P-gp)-mediated multidrug resistance (MDR). Bromotetrandrine shows significant MDR reversal activity in vitro and in vivo, which may be related to the inhibition of P-gp overexpression and the increase in intracellular accumulation of anticancer agents. Bromotetrandrine is a brominated derivative of tetrandrine, which is promising for MDR modulator for tumor assessment[1][2].
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Bromotetrandrine | Bromotetrandrine is a potent inhibitor of P-glycoprotein (P-gp)-mediated multidrug resistance (MDR). Bromotetrandrine shows significant MDR reversal activity in vitro and in vivo, which may be related to the inhibition of P-gp overexpression and the increase in intracellular accumulation of anticancer agents. Bromotetrandrine is a brominated derivative of tetrandrine, which is promising for MDR modulator for tumor assessment. | |||||||||||||||||||||
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References
- [1]. Zheng L, et al. Pharmacokinetics and safety of bromotetrandrine (BrTet, W198) after single-dose intravenous administration in healthy Chinese volunteers. J Clin Pharm Ther. 2010 Feb;35(1):113-9. [Content Brief]
- [2]. Jin J, et al. Reversal of multidrug resistance of cancer through inhibition of P-glycoprotein by 5-bromotetrandrine. Cancer Chemother Pharmacol. 2005 Feb;55(2):179-88. [Content Brief]
