Development and Validation of Stability Indicating RP-HPLC Method for the Determination of Impurity Profile in Gamendazole: Experimental Male Oral Contraceptive

Dasari, Purnachand; Reddy, Arava Veera; Ramadevi, B.; ChVSL, Kameswarrao; Madhusudhanreddy, Bethi

doi:10.1080/10826076.2015.1042977

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2018

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“…This result is in accordance with the poor molecular docking results of compound 10 . Similarly, gamendazole in the form of analytical standard was subjected to the interaction studies as a positive control. As expected, binding of gamendazole with eEF1A1 was confirmed, although the interaction is much weaker than those of the 3-HQs (see the titration profile in SI).…”

Section: Resultsmentioning

confidence: 99%

Identification of Eukaryotic Translation Elongation Factor 1-α 1 Gamendazole-Binding Site for Binding of 3-Hydroxy-4(1H)-quinolinones as Novel Ligands with Anticancer Activity

et al. 2018

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Here, we have identified the interaction site of the contraceptive drug gamendazole using computational modeling. The drug was previously described as a ligand for eukaryotic translation elongation factor 1-α 1 (eEF1A1) and found to be a potential target site for derivatives of 2-phenyl-3-hydroxy-4(1 H)-quinolinones (3-HQs), which exhibit anticancer activity. The interaction of this class of derivatives of 3-HQs with eEF1A1 inside cancer cells was confirmed via pull-down assay. We designed and synthesized a new family of 3-HQs and subsequently applied isothermal titration calorimetry to show that these compounds strongly bind to eEF1A1. Further, we found that some of these derivatives possess significant in vitro anticancer activity.

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Section: Resultsmentioning

confidence: 99%