Aurones and furoaurones: Biological activities and synthesis

Aurones, (Z)-2-benzylidenebenzofuran-3(2H)-ones, have proved to be promising bioactive compounds with a broad spectrum of activities including anticancer, antioxidant, antiparasitic and antibacterial activities. Aurones exhibited strong antiproliferative properties against cancer cells by acting on variable targets through different modes of action. Furoaurones, (Z)-2-benzylidenefurano[3,2-f] benzofuran-3(2H)-ones, is a class of semi synthetic compounds derived from naturally furanochromones extracted from of Ammi visnaga (L.) fruits. So, this literature review includes different biological activities of aurones and furoaurones and different methods for their synthesis. Keywords: Aurones, Furoaurone

Synthesis and antitumor activity of certain 2,3,6-trisubstituted quinazolin-4(3H)-one derivatives

The synthesis of different series of 6-iodo-2-phenoxymethyl 3-substituted quinazolin-4(3H)-ones 5–17 is described. The structures of the newly synthesized compounds have been confirmed on the basis of elemental analyses, IR, 1H NMR and mass spectral data. Preliminary testing for the in vitro antitumor activity of the synthesized compounds against MCF-7 breast cell line was carried out using Doxorubicin (IC50: 5.46 μmol/ml) as a reference drug. Compound 5b exhibited a remarkable antitumor activity (IC50: 5.49 μmol/ml) almost similar to that expressed by the reference drug, whereas compounds 7d, 12b and 6c (IC50: 6.23, 6.55 and 6.80 μmol/ml, respectively) showed a considerable activity

Synthesis, biological evaluation and molecular modeling study of new (1,2,4-triazole or 1,3,4-thiadiazole)-methylthio-derivatives of quinazolin-4(3H)-one as DHFR inhibitors

A new series of 2-mercapto-quinazolin-4-one analogues was designed, synthesized and evaluated for their in vitro DHFR inhibition, antitumor and antimicrobial activity. Compound 17 proved to be the most active DHFR inhibitor with IC value of 0.01 lM, eight fold more active than methotrexate (MTX). Compounds 16 and 24 showed antitumor activity against human Caco2 colon and MCF-7 breast tumor cell lines with IC 50 50 values of 25.4 and 9.5 lg/ml, respectively. Compounds 15, 20, 21 and 30 showed considerable activity against the Gram-positive bacteria Staphylococcus aureus while 24 and 30 proved active against Bacillus subtilis with a magnitude of potency comparable to the broad spectrum antibiotic Ciprofloxacin. Strong activity was observed for 13, 14, 19, 20 and 24 against Candida albicans and Aspergillus flavus. Compound 17 shared a similar molecular docking mode with MTX and made a critical hydrogen bond and arene-arene interactions via Ala9 and Phe34 amino acid residues, respectively

Additional file 1 of Discovery of a new potent oxindole multi-kinase inhibitor among a series of designed 3-alkenyl-oxindoles with ancillary carbonic anhydrase inhibitory activity as antiproliferative agents

Additional file 1. S1. Spectral data. S2. Molecular docking study. S3. In Vitro biological activity