| Literature DB >> 31226469 |
Amna Kamal1, Mansoureh Nazari V2, Muhammad Yaseen3, Muhammad Adnan Iqbal4, Mohamed B Khadeer Ahamed5, Aman Shah Abdul Majid6, Haq Nawaz Bhatti7.
Abstract
Three benzimidazolium salts (III-V) and respective selenium adducts (VI-VIII) were designed, synthesized and characterized by various analytical techniques (FT-IR and NMR 1H, 13C). Selected salts and respective selenium N-Heterocyclic carbenes (selenium-NHC) adducts were tested in vitro against Cervical Cancer Cell line (Hela), Breast Adenocarcinoma cell line (MCF-7), Retinal Ganglion Cell line (RGC-5) and Mouse Melanoma Cell line (B16F10) using MTT assay and the results were compared with standard drug 5-Fluorouracil. Se-NHC compounds and azolium salts showed significant anticancer potential. Molecular docking studies of compounds (VI, VII and VIII) showed strong binding energies and ligand affinity toward following angiogenic factors: VEGF-A (vascular endothelial growth factor A), EGF (human epidermal growth factor), HIF (Hypoxia-inducible factor) and COX-1 (Cyclooxygenase-1) suggesting that the anticancer activity of adducts (VI, VII and VIII) may be due to their strong anti-angiogenic effect. In addition, compounds III-VIII were screened for their antibacterial and antifungal potential. Adduct VI was found to be potent anti-fungal agent against A. Niger with zone of inhibition (ZI) value 27.01 ± 0.251 mm which is better than standard drug Clotrimazole tested in parallel.Entities:
Keywords: Breast cancer (MCF-7); Cervical cancer (Hela); N-Heterocyclic carbenes; NHC; Retinal Ganglion cancer (RGC-5); Se-NHC; Selenium
Year: 2019 PMID: 31226469 DOI: 10.1016/j.bioorg.2019.103042
Source DB: PubMed Journal: Bioorg Chem ISSN: 0045-2068 Impact factor: 5.275