نتایج جستجو برای: cryptolepine isosteres

تعداد نتایج: 248  

Journal: :Journal of Chemistry 2022

The Plasmodium falciparum dihydrofolate reductase (PfDHFR) and dihydroorotate dehydrogenase (PfDHODH) are essential for growth development, have been validated as targets the development of new antimalarial agents. Several alkaloids isolated from Cryptolepis sanguinolenta reported to antiplasmodial activity, but their protein unknown. Therefore, molecular docking dynamics simulations were used ...

Journal: :Journal of medicinal chemistry 2005
Onyeka Onyeibor Simon L Croft Hilary I Dodson Mohammad Feiz-Haddad Howard Kendrick Nicola J Millington Silvia Parapini Roger M Phillips Scott Seville Steven D Shnyder Donatella Taramelli Colin W Wright

A series of analogues of cryptolepine (1) have been synthesized and evaluated for their in vitro antiplasmodial and cytotoxic properties. The IC(50) values of several compounds (11a, 11k-m, 11o, 13) against Plasmodium falciparum (strain K1) were <0.1 muM, 5-10-fold lower than that of 1 but their cytotoxicities were only 2-4 times greater than that of 1. Compounds with a halogen in the quinoline...

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