harmine has been researched along with 1-3-4-oxadiazole* in 2 studies
2 other study(ies) available for harmine and 1-3-4-oxadiazole
| Article | Year |
|---|---|
Design, synthesis, and biological evaluation of β-carboline 1,3,4-oxadiazole based hybrids as HDAC inhibitors with potential antitumor effects.
A series of novel β-carboline 1,3,4-oxadiazole based hybrids were designed, synthesized, and tested for cytotoxicity and HDAC inhibition. Among the target compounds, compound ZDLT-1 displayed high inhibitory activity for class I HDACs 1, 2, and 3, and potent anti-proliferative activity against HCT116 cells with an IC Topics: Antineoplastic Agents; Carbolines; Cell Line, Tumor; Cell Proliferation; Drug Design; Drug Screening Assays, Antitumor; Histone Deacetylase Inhibitors; Humans; Molecular Structure; Oxadiazoles; Structure-Activity Relationship | 2022 |
Harmine-inspired design and synthesis of benzo[d]imidazo[2,1-b]thiazole derivatives bearing 1,3,4-oxadiazole moiety as potential tumor suppressors.
Standard chemotherapy and personalized target therapies are commonly used in patients with advanced non-small cell lung cancer (NSCLC). However, multidrug resistance (MDR) and tumor metastasis lead to the decline of therapeutic efficacy, which are closely related to epithelial-mesenchymal transition (EMT). Twist1, an EMT transcription factor, plays an essential role in promoting EMT, MDR and tumor metastasis. In view of the essential role of Twist1 in the tumorigenesis of NSCLC, developing antitumor small molecules that can suppress the expression of Twist1 is of far-reaching significance for the treatment of NSCLC. A series of novel benzo[d]imidazo[2,1-b]thiazole derivatives possessing 1,3,4-oxadiazole moiety were designed based on the structure of the first-in-class Twist1 inhibitor harmine. Among the synthetic twenty-two compounds, the compound containing 2-(piperidine-1-yl) ethyl exhibited remarkable anti-proliferative activity with IC Topics: Antineoplastic Agents; Cell Line, Tumor; Cell Proliferation; Dose-Response Relationship, Drug; Drug Design; Drug Screening Assays, Antitumor; Harmine; Humans; Imidazoles; Molecular Structure; Oxadiazoles; Structure-Activity Relationship; Thiazoles | 2021 |