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

Autor: Ahmed HB; Chemistry Department, Faculty of Science, Helwan University, Ain-Helwan, Cairo 11795, Egypt. Electronic address: hananbasiony@gmail.com., Mikhail MM; Chemistry Department, Faculty of Science, Helwan University, Ain-Helwan, Cairo 11795, Egypt., Abdallah AEM; Chemistry Department, Faculty of Science, Helwan University, Ain-Helwan, Cairo 11795, Egypt., El-Shahat M; Photochemistry Department, Chemical Industries Research Institute, National Research Centre, 33 EL Buhouth St., Dokki, Giza 12622, Egypt., Emam HE; Department of Pretreatment and Finishing of Cellulosic Fibers, Textile Research and Technology Institute, National Research Centre, 33 EL Buhouth St., Dokki, Giza 12622, Egypt. Electronic address: hossamelemam@yahoo.com.
Jazyk: angličtina
Zdroj: Bioorganic chemistry [Bioorg Chem] 2023 Dec; Vol. 141, pp. 106902. Date of Electronic Publication: 2023 Oct 01.
DOI: 10.1016/j.bioorg.2023.106902
Abstrakt: 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, 1 HNMR, 13 CNMR & 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.
Competing Interests: Declaration of Competing Interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper.
(Copyright © 2023 Elsevier Inc. All rights reserved.)
Databáze: MEDLINE
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