Quinazoline–benzimidazole hybrid as dual optical sensor for cyanide and Pb2+ ions and Aurora kinase inhibitor

Binding and energy transfer of an erbium ion with rhaponticin (RH) was investigated and a simple spectrofluorimetric method was developed for determination of RH using an Er 3+ probe. Results using spectra, chromatography and density functional theory (DFT) indicated that binding of Er 3+ to RH occurred at the hydroxyl group of C-11 and at the methoxy group at C-12 of the conjugated aromatic ring through hydrogen bonding. Resonance energy transfer (RET) occurred from intramolecular charge transfers (ICT), the binding of RH to Er 3+ ion induced fluorescence enhancement (FE) of the Er 3+ ion. This method was applied to the pharmacokinetic detection of RH. The main advantages of the proposed method compared with previously reported ones are its simplicity and lower cost.

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“…The binding constant of interactions between RH and Er 3 + was calculated using the Benesi–Hildebrand equation :…”

Section: Resultsmentioning

confidence: 99%

Study of the binding and energy transfer of erbium ion with rhaponticin and its pharmacokinetics application

et al. 2016

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“…Another group reported the synthesis of quinazoline‐benzimidazole hybrids 3a and 3b as aurora kinase inhibitors with IC 50 of 7.5 and 0.53 μM, respectively (Figure 2) (Luxami et al, 2015). Molecular docking in the active site of Aurora kinase (pdb ID 2WTV) revealed that compound 3a binds to the active site via three interactions: H ‐bond with nitrogen atom of benzimidazole ring, NH bridge (linking between benzimidazole and quinazoline rings), and amino group of o ‐phenylenediamine with T556, L560, and D520 amino acid residues, respectively.…”

Section: Biological Activitymentioning

confidence: 99%

Benzimidazole‐based protein kinase inhibitors: Current perspectives in targeted cancer therapy

et al. 2022

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Targeted therapy has emerged to be the cornerstone of advanced cancer treatment, allowing for more selectivity and avoiding the common drug toxicity and resistance. Identification of potential targets having vital role in growth and survival of cancer cells got much easier with the aid of the recent advances in high throughput screening approaches. Various protein kinases came into focus as valuable targets in cancer therapy. Meanwhile, benzimidazole‐based scaffolds have gained significant attention as promising protein kinase inhibitors with high potency and varied selectivity. Great diversity of these scaffolds has inspired the medicinal chemists to inspect the effect of structural changes upon inhibitory activity on the molecular level through modeling studies. The present review gathers all the considerable attempts to develop benzimidazole‐based compounds; designed as protein kinase inhibitors with anticancer activity since 2015; that target aurora kinase, CDK, CK2, EGFR, FGFR, and VEGFR‐2; to allow further development and progression regarding benzimidazoles.

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“…Considering the biological importance of the benzimidazole heterocycle, Luxami et al have designed hybrid analogues having the structural features of benzimidazole and 4-aminoquinazoline (important scaffold with anti-cancer potential). 73 Amongst the synthesized analogues, compounds 44 and 45 have shown arora kinase inhibition with IC 50 values of 7.50 and 0.53 mM, respectively (Scheme 19). Along with aurora kinase inhibition, these hybrids were also found to be useful as ratiometric chemosensors for the estimation of lead and cyanide concentration EGFR inhibitors containing 4-aminoquinazoline such as getinib and erlotinib are benecial for anti-cancer activity but they lack clinical efficiency due to the point mutation of the EGFR enzyme.…”

Section: Anti-cancer Hybridsmentioning

confidence: 99%

Recent advances in the pharmacological diversification of quinazoline/quinazolinone hybrids

2020

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Quinazoline–benzimidazole hybrid as dual optical sensor for cyanide and Pb2+ ions and Aurora kinase inhibitor

Cited by 24 publications

References 48 publications

Study of the binding and energy transfer of erbium ion with rhaponticin and its pharmacokinetics application

Study of the binding and energy transfer of erbium ion with rhaponticin and its pharmacokinetics application

Benzimidazole‐based protein kinase inhibitors: Current perspectives in targeted cancer therapy

Recent advances in the pharmacological diversification of quinazoline/quinazolinone hybrids

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