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

Abstract

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 (compound T). Chemical formulas of CQDs proveniences & CQDs were verified via FTIR, ¹HNMR, ¹³CNMR & 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 μM 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 μg/ml, respectively.

Keywords: Anti-inflammatory drugs; Anti-tumor reagent; CQDs; CQDs proveniences; Fluorescence.