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Keywords = β-enaminoesters

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20 pages, 4940 KiB  
Article
Designing Potent Anti-Cancer Agents: Synthesis and Molecular Docking Studies of Thieno[2,3-d][1,2,4]triazolo[1,5-a]pyrimidine Derivatives
by Eman S. M. Elsenbawy, Zafer S. Alshehri, Nouf A. Babteen, Adel A.-H. Abdel-Rahman, Mai A. El-Manawaty, Eman S. Nossier, Reem K. Arafa and Nasser A. Hassan
Molecules 2024, 29(5), 1067; https://doi.org/10.3390/molecules29051067 - 29 Feb 2024
Cited by 3 | Viewed by 2978
Abstract
A new series of thieno[2,3-d][1,2,4]triazolo[1,5-a]pyrimidines was designed and synthesized using readily available starting materials, specifically, β-enaminoester. Their cytotoxicity was screened against three cancer cell lines, namely, MCF-7, HCT-116, and PC-3. 2-(4-bromophenyl)triazole 10b and 2-(anthracen-9-yl)triazole 10e afforded excellent potency [...] Read more.
A new series of thieno[2,3-d][1,2,4]triazolo[1,5-a]pyrimidines was designed and synthesized using readily available starting materials, specifically, β-enaminoester. Their cytotoxicity was screened against three cancer cell lines, namely, MCF-7, HCT-116, and PC-3. 2-(4-bromophenyl)triazole 10b and 2-(anthracen-9-yl)triazole 10e afforded excellent potency against MCF-7 cell lines (IC50 = 19.4 ± 0.22 and 14.5 ± 0.30 μM, respectively) compared with doxorubicin (IC50 = 40.0 ± 3.9 μM). The latter derivatives 10b and 10e were further subjected to in silico ADME and docking simulation studies against EGFR and PI3K and could serve as ideal leads for additional modification in the field of anticancer research. Full article
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11 pages, 271 KiB  
Communication
Efficient Synthesis of β-Enaminones and β-Enaminoesters Catalyzed by Gold (I)/Silver (I) under Solvent-Free Conditions
by Ming Zhang, Ablimit Abdukader, Yong Fu and Chengjian Zhu
Molecules 2012, 17(3), 2812-2822; https://doi.org/10.3390/molecules17032812 - 6 Mar 2012
Cited by 22 | Viewed by 7857
Abstract
An efficient method for the synthesis of β-enaminones and β-enaminoesters using a combination of [(PPh3)AuCl]/AgOTf as catalyst has been developed. The reaction between 1,3-dicarbonyl compounds and primary amines was carried out under solvent-free conditions with low catalyst loading in good to [...] Read more.
An efficient method for the synthesis of β-enaminones and β-enaminoesters using a combination of [(PPh3)AuCl]/AgOTf as catalyst has been developed. The reaction between 1,3-dicarbonyl compounds and primary amines was carried out under solvent-free conditions with low catalyst loading in good to excellent yields at room temperature. Full article
(This article belongs to the Section Organic Chemistry)
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