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1.
Arch Pharm (Weinheim) ; 355(6): e2200051, 2022 Jun.
Artículo en Inglés | MEDLINE | ID: mdl-35385159

RESUMEN

Cancer, characterized by a deregulation of the cell cycle which mainly results in a progressive loss of cellular differentiation and uncontrolled cellular growth, remains a prominent cause of death across the world. Almost all currently available anticancer agents used in clinical practice have developed multidrug resistance, creating an urgent need to develop novel chemotherapeutics. Benzimidazole derivatives could exert anticancer properties through diverse mechanisms, inclusive of the disruption of microtubule polymerization, the induction of apoptosis, cell cycle (G2/M) arrest, antiangiogenesis, and blockage of glucose transport. Moreover, several benzimidazole-based agents have already been approved for the treatment of cancers. Hence, benzimidazole derivatives are useful scaffolds for the development of novel anticancer agents. In particular, benzimidazole hybrids could exert dual or multiple antiproliferative activities and had the potential to overcome drug resistance, demonstrating the potential of benzimidazole hybrids as potential prototypes for clinical deployment in the control and eradication of cancers. The purpose of the present review article is to provide a comprehensive landscape of benzimidazole hybrids as potential anticancer agents, and the structure-activity relationship as well as mechanisms of action are also discussed to facilitate the further rational design of more effective candidates, covering articles published from 2019 to 2021.


Asunto(s)
Antineoplásicos , Neoplasias , Antineoplásicos/farmacología , Antineoplásicos/uso terapéutico , Bencimidazoles/farmacología , Proliferación Celular , Ensayos de Selección de Medicamentos Antitumorales , Humanos , Estructura Molecular , Neoplasias/tratamiento farmacológico , Relación Estructura-Actividad
2.
Arch Pharm (Weinheim) ; 355(7): e2200052, 2022 Jul.
Artículo en Inglés | MEDLINE | ID: mdl-35419808

RESUMEN

Cancer, as a long-lasting and dramatic disease, affects almost one-third of human beings globally. Chemotherapeutics play an important role in cancer treatment, but multidrug resistance and severe adverse effects have already become the main causes of failure in tumor chemotherapy. Therefore, it is an urgent need to develop novel chemotherapeutics. Cinnamic acid contains a ubiquitous α,ß-unsaturated acid moiety presenting potential therapeutic effects in the treatment of cancer as these derivatives could act on cancer cells by diverse mechanisms of action. Accordingly, cinnamic acid derivatives are critical scaffolds in discovering novel anticancer agents. This review provides a comprehensive overview of cinnamic acid hybrids as anticancer agents. The structure-activity relationship, as well as the mechanisms of action, are also discussed, covering articles published from 2012 to 2021.


Asunto(s)
Antineoplásicos , Neoplasias , Antineoplásicos/farmacología , Antineoplásicos/uso terapéutico , Cinamatos/farmacología , Humanos , Neoplasias/tratamiento farmacológico , Neoplasias/patología , Relación Estructura-Actividad
3.
Hua Xi Kou Qiang Yi Xue Za Zhi ; 39(3): 347-354, 2021 Jun 01.
Artículo en Inglés, Chino | MEDLINE | ID: mdl-34041886

RESUMEN

Due to the complicated anatomical structures in the furcation area of multirooted mandibular first molars, dental hygiene is greatly compromised once the furcation is involved in the periodontitis, leading to the unfavorable prognosis of teeth with furcation involvement. A patient came to a dental office with the chief complaint of "mobile mandibular posterior tooth" 27 years ago. The periapical film showed alveolar bone resorption at the root furcation of the right mandibular first molar. Flap surgery and fine supportive therapy were conducted. The patient was diagnosed with "furcation involvement Class Ⅲ" during a revisit three years ago. Satisfactory and healthy periodontal statuses were observed 2, 9, 24, and 33 months after the periodontal flap surgery plus tunneling procedures. A follow-up of 27 years in the present case demonstrated that a favorable prognosis of furcation involvement can be achieved after adequate periodontal treatment.


Asunto(s)
Defectos de Furcación , Periodontitis , Estudios de Seguimiento , Defectos de Furcación/cirugía , Humanos , Mandíbula , Diente Molar
4.
Artículo en Chino | WPRIM (Pacífico Occidental) | ID: wpr-333860

RESUMEN

<p><b>OBJECTIVE</b>To investigate the aberrance of histone H3 lysine 4 trimethylation (H3K4me3) in patients with IgA nephropathy (IgAN).</p><p><b>METHODS</b>In 15 patients with IgAN and 15 healthy volunteers, H3K4me3 variations in peripheral blood mononuclear cells (PBMCs) were analyzed using chromatin immunoprecipitation and microarray analysis (ChIP-chip). ChIP real-time PCR was used to validate the microarray results. Quantitative real-time PCR (qRT-PCR) was carried out to examine the correlations between the mRNA expression profiles and H3K4me3 levels.</p><p><b>RESULTS</b>We identified 83 genes that displayed significant H3K4me3 differences in IgAN patients compared with healthy subjects. Among them, 39 genes showed increased H3K4me3 and 44 genes had decreased H3K4me3 levels. The results of ChIP real-time PCR were well consistent with the microarray data. Quantitative RT-PCR revealed the correlations between the mRNA expressions and the methylation levels of H3K4me3.</p><p><b>CONCLUSION</b>IgAN patients have significant alterations in H3K4me3, and the genes with aberrant H3K4me3 may provide insights into the pathogenesis of IgAN.</p>


Asunto(s)
Femenino , Humanos , Masculino , Estudios de Casos y Controles , Islas de CpG , Genética , Metilación de ADN , Glomerulonefritis por IGA , Genética , Metabolismo , Histonas , Genética , Metabolismo , Leucocitos Mononucleares , Metabolismo , Lisina , Genética , Metabolismo
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