Abstract
One-pot efficient synthesis of novel chromone derivatives 4a–h and that of 5a–h were described in a simple method via four-component reaction between furochromone carbaldehyde, amine, isocyanate derivatives, and benzoic acid derivatives or nicotinic acid, respectively. Also, oxazocine derivatives 7a, b were prepared via reaction of visnagine carbaldehyde, ethyl acetoacetate and isocyanate derivatives 2a, b. The obtained derivatives of novel furochromone and oxazocine derivatives were evaluated as promising antitumor agents against panel of two human cell lines, hepatocellular carcinoma (HEPG2) and breast carcinoma (MCF7). The antitumor results suggested that furochromone derivatives 5a–h have activity against MCF7 in comparison with doxorubicin as the standard drug. Furthermore, the molecular docking studies of these novel derivatives of furochromone and oxazocine showed good agreement with the biological results when their binding pattern and affinity towards the active site of EGFR was investigate.
Highlights
Cancer is uncontrolled growth of abnormal cells, one of the most widespread serious diseases and its growth and metastasis depends on angiogenesis [1,2,3,4]
Some work by affecting the cells’ genetic “makeup” and others work by blocking cells from using nutrients needed to divide and multiply. e choice of cytotoxic drugs depends on the type and stage of cancer [9]
Cells were seeded in 96 wells plates. e newly synthesized compounds were applied on the two cell lines to test their anticancer activity. e compounds were tested in two distinct concentrations (0.05 μg/ml and 5 μg/ml). e two working solutions were prepared using the complete medium. ree technical replicates were carried out for each concentration. e treated cells were incubated for 48 h at 37°C and 5% CO2
Summary
Cancer is uncontrolled growth of abnormal cells, one of the most widespread serious diseases and its growth and metastasis depends on angiogenesis [1,2,3,4]. Treatment of cancer using cytotoxic drugs (antineoplastics that preventing replication of cells) has many side effects [7, 8] they are toxic to cancer cells. They all tend to work by interfering with some aspect of how the cells divide and multiply. E choice of cytotoxic drugs depends on the type and stage of cancer [9]. Survey and research to get safe novel drugs with less side effects are still in continuation [10, 11]
Sign-in/Register to view highlights & summary Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Schedule a callDisclaimer: All third-party content on this website/platform is and will remain the property of their respective owners and is provided on "as is" basis without any warranties, express or implied. Use of third-party content does not indicate any affiliation, sponsorship with or endorsement by them. Any references to third-party content is to identify the corresponding services and shall be considered fair use under The CopyrightLaw.
