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

被引:27
作者
Ahmed, Hanan B. [1 ]
Mikhail, Mary M. [1 ]
Abdallah, Amira E. M. [1 ]
El-Shahat, Mahmoud [2 ]
Emam, Hossam E. [3 ]
机构
[1] Helwan Univ, Fac Sci, Chem Dept, Cairo 11795, Egypt
[2] Chem Ind Res Inst, Natl Res Ctr, Photochem Dept, 33 EL Buhouth St, Dokki 12622, Giza, Egypt
[3] Text Res & Technol Inst, Natl Res Ctr, Dept Pretreatment & Finishing Cellulos Fibers, 33 EL Buhouth St, Dokki 12622, Giza, Egypt
关键词
CQDs proveniences; CQDs; Fluorescence; Anti-tumor reagent; Anti-inflammatory drugs; FLUORESCENT CARBON DOTS; GRAPHENE QUANTUM DOTS; GREEN SYNTHESIS; MAILLARD REACTION; KAPPA-B; CANCER; CYTOTOXICITY; INFLAMMATION; NANODOTS;
D O I
10.1016/j.bioorg.2023.106902
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
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.
引用
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页数:21
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