Synthesis Of Novel Potent Cytotoxicy Podophyllotoxin-Naphthoquinone Compounds via Microwave-Assited Multicomponent Domino Reactions.

Synthesis Of Novel Potent Cytotoxicy Podophyllotoxin-Naphthoquinone Compounds via Microwave-Assited Multicomponent Domino Reactions.
Bioorg Med Chem Lett. 2021 Feb 05;:127841
Authors: Giang Nguyen Thi Q, Le-Nhat-Thuy G, Anh Dang Thi T, Hoang Thi P, Nguyen Tuan A, Ha Nguyen Thi T, Tra Nguyen T, Nguyen Ha T, Hoang Mai H, Van Nguyen T
Abstract
A series of novel podophyllotoxin-naphthoquinone compounds 5a-p were synthesized in good yields using microwave-assisted four-component reactions of 2-hydroxy-1,4-naphthoquinone, aromatic benzaldehydes, tetronic acid and ammonium acetate. All the synthezied compounds were fully characterized by spectral data and evaluated for their cytotoxicity activities against KB, HepG2, Lu1, MCF7, and non-cancerous Hek-293 cell lines. Among 16 new compounds screened, compounds 5a, 5d, 5h, and 5k displayed high potent inhibitory activities with IC50 < 40 nM against HepG2 and SK-Lu-1 cell lines, and showed lower toxicity for non-cancerous Hek-293 cell line, demonstrating the potential importance of these compounds in the development of potential anticancer agents.
PMID: 33556568 [PubMed - as supplied by publisher]

Source: Bioorganic and Medicinal Chemistry Letters - February 5, 2021 Category: Chemistry Authors: Giang Nguyen Thi Q, Le-Nhat-Thuy G, Anh Dang Thi T, Hoang Thi P, Nguyen Tuan A, Ha Nguyen Thi T, Tra Nguyen T, Nguyen Ha T, Hoang Mai H, Van Nguyen T Tags: Bioorg Med Chem Lett Source Type: research