4.7 Article

Pyrimidine-5-carbonitrile derivatives as sprout for CQDs proveniences: Antitumor and anti-inflammatory potentiality

Journal

BIOORGANIC CHEMISTRY
Volume 141, Issue -, Pages -

Publisher

ACADEMIC PRESS INC ELSEVIER SCIENCE
DOI: 10.1016/j.bioorg.2023.106902

Keywords

CQDs proveniences; CQDs; Fluorescence; Anti-tumor reagent; Anti-inflammatory drugs

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A comparative study was conducted to investigate the effect of variation in heteroatoms in the main skeleton of CQDs on their nucleation affinity, as well as their anti-inflammatory and anticancer properties. Three different CQDs were prepared and their chemical compositions and particle sizes were verified. Results showed that one of the CQDs exhibited the highest affinity as an anti-inflammatory and anticancer drug.
A comparative study is proposed to show the effect of variation in the heteroatoms in the main skeleton of CQDs proveniences, on their affinity for nucleation of CQDs, as anti-inflammatory and anticancer drugs. Heterocyclic-based CQDs sprout was successfully exploited for preparation of three CQDs proveniences, named as; 2-(2,5-dimethoxyphenyl)-4,6-dioxo-6,11-dihydro-4H-pyrimido[2,1-b] quinazoline-3-carbonitrile (compound A), 2-(2,5-dimethoxyphenyl)-4,6-dioxo-4H,6H-benzo[e]pyrimido[2,1-b][1,3]oxazine-3-carbonitrile (compound S) and 2-(2,5-dimethoxyphenyl)-4,6-dioxo-4H,6H-benzo[e]pyrimido[2,1-b][1,3] thiazine-3-carbonitrile (com-pound T). Chemical formulas of CQDs proveniences & CQDs were verified via FTIR, (HNMR)-H-1, (CNMR)-C-13 & XRD. Particle size of TM-CQDs, A-CQDs, S-CQDs & T-CQDs were estimated to be 3.7 +/- 1.4, 4.6 +/- 1.6, 5.9 +/- 1.6 nm and 3.0 +/- 1.3 nm, respectively. All of CQDs proveniences & CQDs were examined for their affinity as anti-inflammatory drugs via Griess assay. CQDs ingrained from TM (TM-CQDs) were detected with the highest NO inhibition% by increasing its concentration from 10 up to 100 mu M to be 40 % to 89 %, respectively. Moreover, their anti-tumor performance against MCF-7: breast Adenocarcinoma cell line was approved via sulforhodamine B assay, whereas, IC50 was evaluated for TM-CQDs, A-CQDs, S-CQDs and T-CQDs to be 38.16, 36.09, 100 and 100 mu g/ml, respectively.

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