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Katowah, D., H. Hassaneen, and T. Farghaly, Novel Spiro-pyrrolizidine-Oxindole and Spiropyrrolidine-Oxindoles: Green synthesis Under Classical, Ultrasonic, and Microwave Conditions and Molecular Docking Simulation for antitumor and type 2 diabetes, , vol. 15, pp. 103930, 2022/04/01. Abstract

Novel spiropyrrolizine / pyrrolidineoxindole moieties were synthesized chemo-, and regio-selectively in high yields from knoevenagel reaction of bis[arylmethylidene]piperidin-4-ones, isatin and L-proline or sarcosine under classical, ultrasonic, and microwave conditions. Seven derivatives of the synthesized dispiro-pyrrolizidine-oxindole and spiropyrrolidine were screened for their antitumor activity against two cell lines MCF-7 (breast cancer) and HEPG2 (liver cancer). The results of biological activity indicated that the tested derivatives showed potent activity against breast cancer cell MCF-7. Molecular docking simulation screening studies of the synthesized products with each of the receptors of (3hb5) for breast cancer and (4k9g) for liver cancer and their interaction with 1H5U of glycogen phosphorylase B, type 2 diabetes drug were examined. The docking study of dispiro-pyrrolizidine-oxindole and spiropyrrolidine showed promising results with several derivatives.

Eid, E., H. Me, S. Loutfy, and T. Salaheldin, Preparation of pyrimido[4,5-b] [1,6]naphthyridin-4(1H)-one derivatives using a zeolite-nanogold catalyst and their in vitro evaluation as anticancer agent, , vol. 45, 2021/02/18. Abstract

Catalysis using supported gold nanoparticles has attracted significant research interest due to their unique properties and potential that is directly related to their particle size. An efficient one-pot, three-component procedure is developed for the preparation of pyrimido[4,5-b][1,6]naphthyridin-4(1H)-one derivatives (4a-h) by cyclocondensation of 6-amino-2-thioxo-2,3-dihydropyrimidin-4(1H)-one (1), aromatic aldehydes (2), and 1-benzylpiperidin-4-one (3) in the presence of zeolite-nano Au as a green catalyst in ethanol at 80 °C. The presented methodology has a number of advantages including a reusable catalyst, easy access, short reaction times, high yields, and an easy work-up. The nanogold catalyst is characterized by X-ray diffraction and transmission electron microscopy. The structures of the prepared compounds are established by elemental analyses and spectral data (infrared, mass spectrometry, 1 H, and 13 C NMR). While molecular docking studies show that products 4a and 4c have binding affinities with the active site of CDKs. A bio-evaluation assay revealed that some of the products exhibit strong to moderate effects against proliferation of Huh7 in an in vitro model of human liver cancer cells as confirmed by morphological alteration. Compounds 4c and 4a offer the lowest IC 50 values at 22.5 and 39 µM, respectively.

Thoraya A. Farghaly, and H. M. E. Hassaneen, "Synthesis of pyrido[2,3-d][1,2,4]triazolo[4,3-a]pyrimidin-5-ones as potential antimicrobial agents", Archives of Pharmacal Research, vol. 36, no. 5: Pharmaceutical Society of Korea, pp. 564-572, 2013. AbstractWebsite