Unknown

Dataset Information

0

Synthesis and Biological Activity Screening of Newly Synthesized Trimethoxyphenyl-Based Analogues as Potential Anticancer Agents.

ABSTRACT: A group of novel trimethoxyphenyl (TMP)-based analogues were synthesized by varying the azalactone ring of 2-(3,4-dimethoxyphenyl)-4-(3,4,5-trimethoxybenzylidene)oxazolone 1 and characterized using NMR spectral data as well as elemental microanalyses. All synthesized compounds were screened for their cytotoxic activity utilizing the hepatocellular carcinoma (HepG2) cell line. Compounds 9, 10 and 11 exhibited good cytotoxic potency with IC50 values ranging from 1.38 to 3.21 μM compared to podophyllotoxin (podo) as a reference compound. In addition, compounds 9, 10 and 11 exhibited potent inhibition of β-tubulin polymerization. DNA flow cytometry analysis of compound 9 shows cell cycle disturbance at the G2/M phase and a significant increase in Annexin-V-positive cells compared with the untreated control. Compound 9 was further studied regarding its apoptotic potential in HepG2 cells; it decreased the level of MMP and Bcl-2 as well as boosted the level of p53 and Bax compared with the control HepG2 cells.

SUBMITTER: Al-Warhi T 

PROVIDER: S-EPMC9322052 | biostudies-literature | 2022 Jul

REPOSITORIES: biostudies-literature

Json Xml
altmetric image

Publications

Synthesis and Biological Activity Screening of Newly Synthesized Trimethoxyphenyl-Based Analogues as Potential Anticancer Agents.

Al-Warhi Tarfah T   Abualnaja Matokah M   Abu Ali Ola A OA   Althobaiti Fayez F   Alharthi Fahad F   Elsaid Fahmy G FG   Shati Ali A AA   Fayad Eman E   Elghareeb Doaa D   Abu Almaaty Ali H AH   Zaki Islam I  

Molecules (Basel, Switzerland) 20220720 14

A group of novel trimethoxyphenyl (TMP)-based analogues were synthesized by varying the azalactone ring of 2-(3,4-dimethoxyphenyl)-4-(3,4,5-trimethoxybenzylidene)oxazolone <b>1</b> and characterized using NMR spectral data as well as elemental microanalyses. All synthesized compounds were screened for their cytotoxic activity utilizing the hepatocellular carcinoma (HepG2) cell line. Compounds <b>9</b>, <b>10</b> and <b>11</b> exhibited good cytotoxic potency with IC<sub>50</sub> values ranging f  ...[more]

Similar Datasets

Unknown Design, synthesis and antiproliferative screening of newly synthesized acrylate derivatives as potential anticancer agents.
| S-EPMC10402871 | biostudies-literature
Unknown Synthesis and Biological Screening of Pyrano[3,2-c]quinoline Analogues as Anti-inflammatory and Anticancer Agents.
| S-EPMC5846041 | biostudies-literature
Unknown Design, synthesis, and biological evaluation of callophycin A and analogues as potential chemopreventive and anticancer agents.
| S-EPMC3207488 | biostudies-literature
Unknown Synthesis of Marine Cyclopeptide Galaxamide Analogues as Potential Anticancer Agents.
| S-EPMC8949366 | biostudies-literature
Unknown Synthesis and biological evaluation of 2-substituted-4-(3',4',5'-trimethoxyphenyl)-5-aryl thiazoles as anticancer agents.
| S-EPMC3535304 | biostudies-literature
Unknown Design, synthesis and antiproliferative screening of newly synthesized coumarin-acrylamide hybrids as potential cytotoxic and apoptosis inducing agents.
| S-EPMC10626558 | biostudies-literature
Unknown Design, Synthesis and Cytotoxic Activity Evaluation of Newly Synthesized Amides-Based TMP Moiety as Potential Anticancer Agents over HepG2 Cells.
| S-EPMC9227250 | biostudies-literature
Unknown Design, synthesis and evaluation of novel enzalutamide analogues as potential anticancer agents.
| S-EPMC8035491 | biostudies-literature
Unknown Pyridine-Ureas as Potential Anticancer Agents: Synthesis and In Vitro Biological Evaluation.
| S-EPMC6100082 | biostudies-other
Unknown Novel pyrrolizines bearing 3,4,5-trimethoxyphenyl moiety: design, synthesis, molecular docking, and biological evaluation as potential multi-target cytotoxic agents.
| S-EPMC8221158 | biostudies-literature