Design, Synthesis, and Biological Evaluation of Aromatic Amide-Substituted Benzimidazole-Derived Chalcones. The Effect of Upregulating TP53 Protein Expression

A series of benzimidazole-derived chalcones containing aromatic amide substituent were designed and synthesized. All of the chalcone compounds were tested for their in vitro antitumor activity against human cancer cell lines (HCT116, HepG2, A549, and CRL-5908). The antiproliferative activity of comp...

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Veröffentlicht in:	Molecules (Basel, Switzerland) Switzerland), 2020-03, Vol.25 (5), p.1162
Hauptverfasser:	Wu, Lintao, Yang, Yuting, Wang, Zhijun, Wu, Xi, Su, Feng, Li, Mengyao, Jing, Xiaobi, Han, Chun
Format:	Artikel
Sprache:	eng
Schlagworte:	5-Fluorouracil Amides - chemistry Antineoplastic Agents - chemical synthesis Antineoplastic Agents - chemistry Antineoplastic Agents - pharmacology antiproliferative activities Antitumor activity Apoptosis aromatic amide-substituted Aromatic compounds Benzimidazoles Benzimidazoles - chemistry Cancer Cell adhesion & migration Cell cycle Cell Cycle - drug effects Cell Line, Tumor Cell Proliferation - drug effects chalcones Chalcones - chemical synthesis Chalcones - chemistry Chalcones - pharmacology Chemistry Techniques, Synthetic Dose-Response Relationship, Drug Drug Design Drug dosages Gene Expression Regulation, Neoplastic Humans MDM2 protein Medical research Molecular Structure Mutants Mutation NMR Nuclear magnetic resonance p53 Protein Protein expression Proteins Structure-Activity Relationship tp53 protein Tumor cell lines Tumor cells Tumor Suppressor Protein p53 - genetics Tumor Suppressor Protein p53 - metabolism Tumors upregulating
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Beschreibung
Zusammenfassung:	A series of benzimidazole-derived chalcones containing aromatic amide substituent were designed and synthesized. All of the chalcone compounds were tested for their in vitro antitumor activity against human cancer cell lines (HCT116, HepG2, A549, and CRL-5908). The antiproliferative activity of compounds , , , , , against HCT116 cells was significantly better than that that of 5-Fluorouracil (IC50: 94.63 µM). The antitumor activity of these compounds showed obvious differences between the wild type HCT116 and mutant HCT116 ( ) cells. A preliminary mechanistic study suggested that these compounds act by upregulating the expression of protein in tumor cells without inhibiting the MDM2- interaction.
ISSN:	1420-3049 1420-3049
DOI:	10.3390/molecules25051162