Synthesis, Biological Evaluation, and Docking Studies of New 2‐Furylbenzimidazoles as Anti‐Angiogenic Agents: Part II. Issue 4 (5th February 2014)

• Record Type: Journal Article
• Authors: Temirak, Ahmed; Shaker, Yasser M.; Ragab, Fatma A. F.; Ali, Mamdouh M.; Soliman, Salwa M.; Mortier, Jeremie; Wolber, Gerhard; Ali, Hamed I.; Diwani, Hoda I. El
• Is Part Of: Archiv der Pharmazie. Volume 347:Issue 4(2014:Apr.)
• Page Start: 291
• Page End: 304
• Publication Date: 2014-02-05
• Subjects: Pharmaceutical chemistry -- Periodicals; Pharmacology -- Periodicals; 615.19
• DOI: 10.1002/ardp.201300356
• Languages: English
• ISSNs: 0365-6233

Abstract

<abstract abstract-type="main"> <title> <x xml:space="preserve">Abstract</x> </title> <sec id="ardp201300356-sec-0001" sec-type="section"> <p>The 2‐(5‐methyl‐2‐furyl)‐1<italic>H</italic>‐benzimidazole moiety has shown promising activity against vascular endothelial growth factor (VEGF)‐induced angiogenesis. In part I of this study, we have synthesized new analogs and tested their anti‐angiogenic potentials. Here, we continue our previous study with different new analogs. Some compounds show promising cytotoxic activity against the human breast cancer cell line MCF‐7, with IC₅₀ in the range of 7.80–13.90 µg/mL, and exhibited remarkable <italic>in vitro</italic> inhibition against VEGF in the MCF‐7 cancer cell line, with 95–98% of inhibition in comparison to tamoxifen as reference (IC₅₀: 8.00 µg/mL, % of inhibition = 98%). Additionally, a molecular docking study was carried out to gain insight into plausible binding modes and to understand the structure–activity relationships of the synthesized compounds.</p> </sec> </abstract>