A new series of N-sec/tert-butyl 2-arylbenzimidazole derivatives was synthesised in 85-96% yields within 2-3.5 min by condensing ethyl 3-amino-4-butylamino benzoate with various substituted metabisulfite adducts of benzaldehyde under focused microwave irradiation. The benzimidazole analogues were characterised using (1)H NMR, (13)C NMR, high resolution MS and melting points. Evaluation of antiproliferative activity of the benzimidazole analogues against MCF-7 and MDA-MB-231 revealed several compounds with unexpected selective inhibitions of MDA-MB-231 in micromolar range. All analogues were found inactive towards MCF-7. The most potent inhibition against MDA-MB-231 human breast cancer cell line came from the unsubstituted 2-phenylbenzimidazole 10a.
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http://dx.doi.org/10.3109/14756366.2012.729828 | DOI Listing |
Curr Pharm Biotechnol
January 2025
Department of Clinical Oncology, Queen Elizabeth Hospital, Hong Kong SAR, China.
Introduction: Iron oxide nanozyme was synthesized from the fruit peel extract of pomegranate, which served as a reducing agent during the green synthesis. The scavenging of reactive oxygen species is often accompanied by immunomodulation following antiproliferative effects due to the crosstalk between the proteins involved in the inter-related signaling pathways.
Method: In the current study, the green synthesized nanozyme was studied for its ability to induce apoptosis in breast cancer cell lines.
J Cancer
January 2025
Department of Pharmacology, The Yancheng Clinical College of Xuzhou Medical University, The First people's Hospital of Yancheng, Yancheng, China.
Longikaurin A (LK-A), a naturally occurring ent-kaurane diterpenoid, has been identified as a promising anti-cancer agent. This study aims to elucidate the anti-tumorigenic effects of LK-A on oral squamous cell carcinoma (OSCC) cells and to unravel its underlying mechanisms. assays, including CCK-8 and EdU, were performed to assess cell viability and proliferation.
View Article and Find Full Text PDFTurk J Chem
October 2024
Department of Chemical Engineering, Faculty of Engineering and Natural Sciences, Uşak University, Uşak, Turkiye.
A new nonperipheral zinc(II) phthalocyanine bearing octa carboxylic acid ethyl ester derivative substituted triazole attached propylmercaptothiobenzylmercapto derivative was synthesized via the tetramerization reaction of phthalonitrile. The photochemical in vitro photodynamic activity of zinc(II) phthalocyanine (), such as human nonsmall cell lung carcinoma cell lines, was investigated in this study. The singlet oxygen generation property of novel zinc(II) phthalocyanine () was also examined due to the significantly high singlet oxygen quantum yield of (F = 0.
View Article and Find Full Text PDFCarbohydr Polym
March 2025
National Glycoengineering Research Center and Shandong Key Laboratory of Carbohydrate Chemistry and Glycobiology, Shandong University, Qingdao, Shandong 266237, China; Suzhou Research Institute of Shandong University, Suzhou, Jiangsu 215123, China. Electronic address:
Camptothecin (CPT) exhibits potent anticancer activity, but its clinical application is limited by poor solubility and severe side effects. Hyaluronic acid (HA) is gaining attention in drug delivery systems due to its excellent biocompatibility and tumor-targeting properties. In this study, we conjugated CPT to the reducing end of ultra-low molecular weight HA to create a series of HA-decorated CPT conjugates.
View Article and Find Full Text PDFBioorg Chem
December 2024
Department of Medicinal Chemistry, Faculty of Pharmacy, Mazandaran University of Medical Sciences, Sari, Iran. Electronic address:
In the current study, a novel series of 1,2,4-oxadiazoles were designed, synthesized, and evaluated for their biological activities. A cell-based antiproliferative screening was accomplished on the newly synthesized 1,2,4-oxadiazoles along with our previously reported aryl(alkyl)azoles (AAAs) containing middle heterocyclic cores thiazole and oxazole. Among the tested compounds, naphthyl- thiazoles demonstrated higher antiproliferative activity and B3 was identified as the most potent compound with IC values in the range of 2.
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