159542-04-8
Chemical Structure
Hapalosin
- CAS No.: 159542-04-8
- Formula:C28H43NO6
- Molecular Weight:489.64
InChIKey: NJNAHFYVTBZQHU-LFFUDGMSSA-N
SMILES: CN(C([C@@H](OC([C@H]([C@H](OC(C[C@H]1O)=O)CCCCCCC)C)=O)C(C)C)=O)[C@H]1CC2=CC=CC=C2
Biological Activity: Hapalosin is a multidrug resistance reversal agent and chemosensitizer with mild cytotoxicity against cancer cells. Hapalosin inhibits the ATP-dependent drug efflux pump function of P-glycoprotein and antagonizes multidrug resistance-associated proteins. Hapalosin reverses multidrug resistance mediated by P-glycoprotein and multidrug resistance-associated proteins, increases the intracellular accumulation of drugs transported by P-glycoprotein, and enhances the cytotoxicity of these drugs against cancer cells overexpressing P-glycoprotein. Hapalosin can be used in the research of multidrug-resistant cancers[1][2].
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Hapalosin | Hapalosin is a multidrug resistance reversal agent and chemosensitizer with mild cytotoxicity against cancer cells. Hapalosin inhibits the ATP-dependent drug efflux pump function of P-glycoprotein and antagonizes multidrug resistance-associated proteins. Hapalosin reverses multidrug resistance mediated by P-glycoprotein and multidrug resistance-associated proteins, increases the intracellular accumulation of drugs transported by P-glycoprotein, and enhances the cytotoxicity of these drugs against cancer cells overexpressing P-glycoprotein. Hapalosin can be used in the research of multidrug-resistant cancers. | |||||||||||||||||||||
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References
- [1]. Dinh TQ, et al. Design, synthesis, and evaluation of the multidrug resistance-reversing activity of D-glucose mimetics of hapalosin. J Med Chem. 1998;41(6):981-987. [Content Brief]
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[2]. Stratmann K, et al. Hapalosin, a cyanobacterial cyclic depsipeptide with multidrug-resistance reversing activity. The Journal of Organic Chemistry. 1994 Dec;59(24):7219-26.
