Design, Synthesis and Anti-Tumor Activity of Novel Benzimidazole-Chalcone Hybrids as Non-Intercalative Topoisomerase II Catalytic Inhibitors

Zhou, Wei; Zhang, Wenjin; Peng, Yi; Jiang, Zhi‐Hong; Zhang, Lanyue; Du, Zhiyun

doi:10.3390/molecules25143180

Cited by 35 publications

(16 citation statements)

References 35 publications

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“…Chalcones have been shown to exhibit anticancer activity through their inhibitory potential against various targets, such as 5α-reductase [ 187 ], aromatase [ 188 ], histone deacetylase inhibitors (HDAC) [ 189 , 190 ], proteasome [ 191 , 192 ], JAK/STAT signaling pathways [ 193 ], cell division cycle 25 (CD25) [ 194 ], cathepsin-K [ 72 , 195 ], topoisomerase-II [ 196 , 197 ], Wnt [ 198 , 199 ], ROS/MAPK [ 200 ], p38 [ 201 , 202 ] and mTOR [ 203 , 204 ]. However, these studies are not covered in this review because not enough evidence has been provided to indicate that these proteins or pathways are direct targets of chalcones.…”

Section: Representative Mechanisms Of Anticancer Action Of Chalconesmentioning

confidence: 99%

Chalcone Derivatives: Role in Anticancer Therapy

et al. 2021

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Chalcones (1,3-diaryl-2-propen-1-ones) are precursors for flavonoids and isoflavonoids, which are common simple chemical scaffolds found in many naturally occurring compounds. Many chalcone derivatives were also prepared due to their convenient synthesis. Chalcones as weandhetic analogues have attracted much interest due to their broad biological activities with clinical potentials against various diseases, particularly for antitumor activity. The chalcone family has demonstrated potential in vitro and in vivo activity against cancers via multiple mechanisms, including cell cycle disruption, autophagy regulation, apoptosis induction, and immunomodulatory and inflammatory mediators. It represents a promising strategy to develop chalcones as novel anticancer agents. In addition, the combination of chalcones and other therapies is expected to be an effective way to improve anticancer therapeutic efficacy. However, despite the encouraging results for their response to cancers observed in clinical studies, a full description of toxicity is required for their clinical use as safe drugs for the treatment of cancer. In this review, we will summarize the recent advances of the chalcone family as potential anticancer agents and the mechanisms of action. Besides, future applications and scope of the chalcone family toward the treatment and prevention of cancer are brought out.

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Section: Representative Mechanisms Of Anticancer Action Of Chalconesmentioning

confidence: 99%

Chalcone Derivatives: Role in Anticancer Therapy

et al. 2021

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“…Further biological evaluation of these compounds showed that they induced apoptosis and inhibited human topoisomerase II α as a possible intracellular target. Zhou et al (2020) designed and synthesized a novel series of benzimidazole-chalcone hybrids (BCHs). These BCHS showed good inhibition in the Topo II-mediated DNA relaxation assay and good anti-proliferative effects in four tumor cell lines (A549, HePG-2, MG63, LNCaP), with 4h and 4i being the most potent with IC50 values <5 µM, superior to Etoposide.…”

Section: Dna Topoisomerase Inhibitorsmentioning

confidence: 99%

Recent progress of research on anti‐tumor agents using benzimidazole as the structure unit

Peng

Chen

et al. 2022

Chem Biol Drug Des

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With the development of exploration for disease‐related proteins or receptors, more and more novel structural lead compounds are required to designed and synthesized. The benzimidazole is an effective structural unit in which the benzene ring is fused at the 4 and 5 positions of the imidazole ring and wildly used in drug design. Here, we introduce some recent progress of research for anti‐tumor agents which was target to various target proteins such as DNA topoisomerase, angiogenesis, serine/threonine protein kinase, and tyrosine protein kinase. These anti‐tumor agents are all introduced benzimidazole as the structure unit. Further docking study showed that the benzimidazole group was not only act as a skeleton to expand the structure of molecule but also as an excellent ligand unit to form hydrogen bond or π–π conjugation and hydrophobic interaction with target proteins or receptors. We expect that introducing benzimidazole in the chemical structure could be a reasonable and priority strategy in novel anti‐tumor agents' design.

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“…Chalcones occur in the cis or trans form, of which the trans isomer is more thermodynamically stable than the cis form. Chalcones have been reported to have biological properties such as anticancer [ 3 ] antimicrobial [ 4 ], antiviral [ 5 ], antioxidant [ 6 ], anti-Alzheimer’s [ 7 ], antitumor [ 8 ], antidiabetic [ 9 ], anti-Parkinson’s [ 10 ], anti-inflammatory [ 11 ], and anti-nociceptive [ 12 ] effects ( Figure 1 ). After a careful literature search, it has been found that in the past decade many scientific developments took place in chalcone chemistry, which is scattered in nature.…”

Section: Introductionmentioning

confidence: 99%

Chalcone: A Promising Bioactive Scaffold in Medicinal Chemistry

et al. 2022

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Chalcones are a class of privileged scaffolds with high medicinal significance due to the presence of an α,β-unsaturated ketone functionality. Numerous functional modifications of chalcones have been reported, along with their pharmacological behavior. The present review aims to summarize the structures from natural sources, synthesis methods, biological characteristics against infectious and non-infectious diseases, and uses of chalcones over the past decade, and their structure–activity relationship studies are detailed in depth. This critical review provides guidelines for the future design and synthesis of various chalcones. In addition, this could be highly supportive for medicinal chemists to develop more promising candidates for various infectious and non-infectious diseases.

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Design, Synthesis and Anti-Tumor Activity of Novel Benzimidazole-Chalcone Hybrids as Non-Intercalative Topoisomerase II Catalytic Inhibitors

Cited by 35 publications

References 35 publications

Chalcone Derivatives: Role in Anticancer Therapy

Chalcone Derivatives: Role in Anticancer Therapy

Recent progress of research on anti‐tumor agents using benzimidazole as the structure unit

Chalcone: A Promising Bioactive Scaffold in Medicinal Chemistry

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