Bis-(10-deoxydihydroartemisinin)-phloroglucinol (9), has been synthesized in a one-step reaction and has demonstrated strong inhibition to cancer cell proliferation and immunosuppressive activity. The structure modification of the compound reduced its cytotoxicity, and among the analogs, bis-(10-deoxydihydroartemisinin)-phloroglucinol phenyl decanoate (16) showed significant reduction of ear swelling in a mouse model for DNFB-induced delayed-type hypersensitivity without observable toxicity in a dose-dependent manner.
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| http://dx.doi.org/10.1016/j.bioorg.2023.106705 | DOI Listing |
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Novel Bis-Artemisinin-Phloroglucinol hybrid molecules with dual anticancer and immunomodulatory Activities: Synthesis and evaluation.
Bioorg Chem
October 2023
School of Medicine, Shanghai Jiao Tong University, 280 South Chongqing Road, Shanghai 200025, China; School of Pharmacy, Shanghai University of Traditional Chinese Medicine, 1200 Cai Lun Road, Shanghai 201203, China. Electronic address:
Bis-(10-deoxydihydroartemisinin)-phloroglucinol (9), has been synthesized in a one-step reaction and has demonstrated strong inhibition to cancer cell proliferation and immunosuppressive activity. The structure modification of the compound reduced its cytotoxicity, and among the analogs, bis-(10-deoxydihydroartemisinin)-phloroglucinol phenyl decanoate (16) showed significant reduction of ear swelling in a mouse model for DNFB-induced delayed-type hypersensitivity without observable toxicity in a dose-dependent manner.
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