1239953-66-2
Chemical Structure
DM-1157
- CAS No.: 1239953-66-2
- Formula:C28H31ClN6
- Molecular Weight:487.04
InChIKey: QRCZXFIANKOFOR-UHFFFAOYSA-N
SMILES: ClC1=CC2=NC=CC(NCCCN3CCC(CC3)NC(C4=NC=CC=C4)C5=NC=CC=C5)=C2C=C1
Biological Activity: DM-1157 is an orally active asymmetric bisquinoline heme inhibitor with a IC50 of 1.6 μM and a Kd of 1.7 μM. DM-1157 binds to heme dimers in solution, inhibits β-hematin formation, suppresses hemozoin formation in the digestive vacuole of Plasmodium falciparum, accumulates in the digestive vacuole of Plasmodium falciparum, induces enlargement of the digestive vacuole of Plasmodium falciparum, and inhibits the growth of Chloroquine (HY-17589A)-sensitive and resistant Plasmodium falciparum strains. DM-1157 can be used for the research of malaria and Plasmodium falciparum-type malaria[1][2].
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DM-1157 | DM-1157 is an orally active asymmetric bisquinoline heme inhibitor with a IC50 of 1.6 μM and a Kd of 1.7 μM. DM-1157 binds to heme dimers in solution, inhibits β-hematin formation, suppresses hemozoin formation in the digestive vacuole of Plasmodium falciparum, accumulates in the digestive vacuole of Plasmodium falciparum, induces enlargement of the digestive vacuole of Plasmodium falciparum, and inhibits the growth of Chloroquine (HY-17589A)-sensitive and resistant Plasmodium falciparum strains. DM-1157 can be used for the research of malaria and Plasmodium falciparum-type malaria. | |||||||||||||||||||||
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- [1]. Burgess SJ, et al. Synthesis, structure-activity relationship, and mode-of-action studies of antimalarial reversed chloroquine compounds. J Med Chem. 2010;53(17):6477-6489. [Content Brief]
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[2]. Liebman KM, et al. Unsymmetrical Bisquinolines with High Potency against P. falciparum Malaria. Molecules. 2020 May 10;25(9):2251.
[Content Brief]
Keywords
