Anticancer activity, spectroscopic and molecular docking of some new synthesized sugar hydrazones, Arylidene and α-Aminophosphonate derivatives

• Main Authors: Hamada H. Amer, Saad H. Alotaibi, Amer H. Trawneh, Ahmed M. Metwaly, Ibrahim H. Eissa
• Format: Article
• Language: English
• Published: Elsevier 2021-10-01
• Series: Arabian Journal of Chemistry
• Subjects: 4-Hydroxybenzaldehyde; Nucleosides; Arylidene derivatives; Molecular docking; Anticancer agents
• Online Access: http://www.sciencedirect.com/science/article/pii/S1878535221003634
• ISSN: 1878-5352

In this work, we design and then synthesis of new derivatives of nucleosides, oxadiazoline derivatives containing acetylated sugars and α-aminophosphonate derivatives. The synthesized compounds have been elucidated by different spectroscopic analysis, such as, elemental analysis, 13C NMR, infrared (IR) and 1H NMR. The compounds previously synthesized were purified and then tested against breast cancer cells (MCF-7). The results showed that the compounds 5d, 6b, 7a and 9h showed moderate to very high activity against breast cancer, with incidence rates of 78.45%, 84.60%, 93.45% and 95.78%, respectively. The reference ratio of 5-fluorouracil was inhibitory of 96.02%. The binding potential of synthesized compounds against thymidylate synthase (TS) and Cathepsin B (CB) has been investigated and the compounds 7a and 9h exhibits highly binding with thymidylate synthase (TS) and Cathepsin B (CB).