| Literature DB >> 29129514 |
Mariana Ingold1, Rosina Dapueto1, Sabina Victoria2, Germán Galliusi3, Carlos Batthyàny3, Mariela Bollati-Fogolín2, David Tejedor4, Fernando García-Tellado4, José M Padrón5, Williams Porcal6, Gloria V López7.
Abstract
A one-pot efficient, practical and eco-friendly synthesis of tocopherol analogues has been developed using water or solvent free conditions via Passerini and Ugi multicomponent reactions. These reactions can be optimized using microwave irradiation or ultrasound as the energy source. Accordingly, a small library of 30 compounds was prepared for biological tests. The evaluation of the antiproliferative activity in the human solid tumor cell lines A549 (lung), HBL-100 (breast), HeLa (cervix), SW1573 (lung), T-47D (breast), and WiDr (colon) provided lead compounds with GI50 values between 1 and 5 μM. A structure-activity relationship is also discussed. One of the studied compounds comes up as a future candidate for the development of potent tocopherol-mimetic therapeutic agents for cancer.Entities:
Keywords: Antiproliferative; Green conditions; Microwaves; Multicomponent reactions; Ultrasound; Water
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Year: 2017 PMID： 29129514 DOI： 10.1016/j.ejmech.2017.11.003
Source DB: PubMed Journal: Eur J Med Chem ISSN： 0223-5234 Impact factor: 6.514