A Rapid and Efficient Protocol for the Synthesis of Cinnamils

Ahmad, Hafiz Adnan; Gillani, Syeda Shaista; Babar, Rabia; Munawar, Munawar Ali; Gulb, Salman

doi:10.32931/io2002a

Cited by 2 publications

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“…[ 1 ] To overcome this obstacle, some optimal conditions were tested, including different solvents or base catalysts; however, only moderate yields were obtained. [ 17 ]…”

Section: Introductionmentioning

confidence: 99%

“…[1] To overcome this obstacle, some optimal conditions were tested, including different solvents or base catalysts; however, only moderate yields were obtained. [17] The quinoxaline moiety is composed of a benzene ring and a pyrazine ring (Figure 1b). The most common strategy for the synthesis of quinoxalines is to use cinnamils to condense two equivalents of 1,2-diaminobenzene derivatives in acidic conditions to afford the target molecules in high yields.…”

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confidence: 99%

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Synthesis of cinnamils and quinoxalines and their biological evaluation as anticancer agents

Wang

Cho

et al. 2022

Archiv der Pharmazie

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We synthesized multiple cinnamils and quinoxalines to evaluate their anticancer activity. Cinnamils were used as precursors for quinoxalines via condensation with 1,2-diaminobenzene. Among the 26 synthesized compounds reported in this article, we found that cinnamil 3l exhibited its inhibitory effect with an IC 50 value of 1.45 ± 0.98 μM, significantly higher than doxorubicin (8.5 ± 0.85 μM) against pancreatic cancer cells (PANC-1). Additionally, cinnamil 3l (IC 50 10.98 ± 3.63 μM)showed less cytotoxicity than doxorubicin to Hs68 cells (0.92 ± 1.11 μM). The colony formation assay demonstrated that 3l obviously decreased the PANC-1 cell viability, and Western blot assays confirmed that 3l markedly induced apoptosis of PANC-1 cells through Bax, Bcl-2, and caspase 3 signaling cascades. These results demonstrate that cinnamil 3l has great potential to be further developed as a promising chemotherapeutic agent for pancreatic cancer.

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“…[ 1 ] To overcome this obstacle, some optimal conditions were tested, including different solvents or base catalysts; however, only moderate yields were obtained. [ 17 ]…”

Section: Introductionmentioning

confidence: 99%

mentioning

confidence: 99%

Synthesis of cinnamils and quinoxalines and their biological evaluation as anticancer agents

Wang

Cho

et al. 2022

Archiv der Pharmazie

View full text Add to dashboard Cite

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Synthesis of 1,2,3-benzotriazin-4(3H)-one derivatives as α-glucosidase inhibitor and their in-silico study

et al. 2022

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α-Glucosidase inhibition is considered as an effective strategy for the treatment of diabetes mellitus.Currently, three α-glucosidase inhibitors are being used as drugs; Acarbose, Voglibose and Miglitol. The side effects of these drugs are forcing researchers to search for new and effective molecules. In this research work, novel 1,2,3-benzotriazin-4(3H)-one sulfonamides were synthesized and investigated for their α-glucosidase inhibition activity. TCT: DMF adduct have been utilized for the direct synthesis of targeted sulfonamides. All reactions were performed at room temperature under mild conditions. In-vitro enzyme inhibition studies led us to discover many potent inhibitors demonstrating good to excellent activity. The compound 5c with dimethyl substituent was found to be more potent inhibitor than acarbose with the IC 50 value of 29.75±0.14 μM. Compounds 5a, 5b, 5d, 5e, 5f and 5m showed good inhibition results with IC 50 value 31.97±0.03, 33.24±0.01, 33.76±1.05, 35.98±0.03, 30.87±0.51 and 37.24±0.04 µM respectively. Further structure activity relationship was analyzed by molecular docking studies.

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A Rapid and Efficient Protocol for the Synthesis of Cinnamils

Cited by 2 publications

References 0 publications

Synthesis of cinnamils and quinoxalines and their biological evaluation as anticancer agents

Synthesis of cinnamils and quinoxalines and their biological evaluation as anticancer agents

Synthesis of 1,2,3-benzotriazin-4(3H)-one derivatives as α-glucosidase inhibitor and their in-silico study

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