Synthesis of Artemisinin-Estrogen Hybrids Highly Active against HCMV, P. falciparum, and Cervical and Breast Cancer.

ABSTRACT: Artemisinin-estrogen hybrids were for the first time both synthesized and investigated for their in vitro biological activity against malaria parasites (Plasmodium falciparum 3D7), human cytomegalovirus (HCMV), and a panel of human malignant cells of gynecological origin containing breast (MCF7, MDA-MB-231, MDA-MB-361, T47D) and cervical tumor cell lines (HeLa, SiHa, C33A). In terms of antimalarial efficacy, hybrid 8 (EC₅₀ = 3.8 nM) was about two times more active than its parent compound artesunic acid (7) (EC₅₀ = 8.9 nM) as well as the standard drug chloroquine (EC₅₀ = 9.8 nM) and was, therefore, comparable to the clinically used dihydroartemisinin (6) (EC₅₀ = 2.4 nM). Furthermore, hybrids 9-12 s

SUBMITTER: Frohlich T 

PROVIDER: S-EPMC6231177 | biostudies-literature | 2018 Nov

REPOSITORIES: biostudies-literature