Design, synthesis and biological evaluation of acyl hydrazones-based derivatives as RXRα-targeted anti-mitotic agents

Wang, Qi‐Qiang; Tu, Xuhuang; Wang, Xin; Cai, Qi; Yu, Liangfa; Zhang, Xuan; Yi, Jiajin; Wu, Yuhang; Xie, Guobin; Yuan, Hang; Li, Mingyu; Zhang, Xiaokun; Zeng, Zhiping; Su, Ying

doi:10.1016/j.bioorg.2022.106069

Cited by 2 publications

(1 citation statement)

References 58 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…[16] This discovery has had a substantial impact on medical chemistry. These compounds' acetylcholinesterases, [17] anticancer, [18] α-glucosidase, [19] antitubercular, [20] anti-mitotic, [21] antimicrobial, [22] and antifungal [23] properties are also of great interest.…”

Section: Introductionmentioning

confidence: 99%

Imidazole‐hydrazone derivatives: Synthesis, characterization, X‐ray structures and evaluation of anticancer and carbonic anhydrase I–II inhibition properties

et al. 2023

View full text Add to dashboard Cite

The nine new imidazole-hydrazone derivatives of Schiff base were synthesized from the condensation reactions of 1-methyl-1H-imidazole-2-carbaldehyde with various substitutedhydrazide derivatives. Structures of the final compounds (1 a-1 i) were characterized by using 1 H NMR, 13 C NMR spectroscopic techniques, elemental analysis, and crystal X-ray diffraction. The in vitro carbonic anhydrase I and II potentials of these synthesized were evaluated. The result suggests that compound 1 a, a 4-methoxy substituted analog with an IC 50 of 0.949 μM, was found to have the most potent hCA I inhibitory activity. Compounds 1 c, 1 d, and 1 h were the most potent compounds on hCA II with IC 50 values of 3.330, 4.454, and 5.66 μM, respectively. All compounds were examined for their cytotoxicity towards human colorectal adenocarcinoma cell (HT29) and rat glioma cell line (C6) compared to mouse fibroblast normal cell line (L929) using the MTT assay method. The compounds 1 a, 1 d, and 1 i exhibited significant antiproliferative activity with less toxicity to a health cell line. Consequently, compound 1 a could be the potential lead for emerging selective cytotoxic compounds directing hCA I. Compound 1 d could be the potential lead for emerging selective cytotoxic compounds directing hCA II.

show abstract