Synthesis and evaluation of Novel Benzimidazole derivative [Bz-Im] and its radio/biological studies

Tiwari, Anjani K.; Mishra, Anil K.; Bajpai, Aruna; Mishra, Pushpa; Singh, Sweta; Sinha, Deepa; Singh, Vinay Kumar

doi:10.1016/j.bmcl.2007.02.071

Cited by 23 publications

(14 citation statements)

References 17 publications

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“…Some of these compounds showed promising antiproliferative effect against tumor cell lines, as a continuation of our previous efforts (9)(10)(11)(12). Some of these compounds showed promising antiproliferative effect against tumor cell lines, as a continuation of our previous efforts (9)(10)(11)(12).…”

supporting

confidence: 52%

“…The present study aimed to synthesize and evaluate the biological activity of some quinazoline's cytotoxicity in vitro against different cell lines. Some of these compounds showed promising antiproliferative effect against tumor cell lines, as a continuation of our previous efforts (9)(10)(11)(12). A new series of quinazoline compounds are designed, in such a way to accommodate a substituted benzimidazole ring at position 3.…”

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confidence: 94%

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Disubstituted 4(3H) Quinazolones: A Novel Class of Antitumor Agents

Srivastava

Tiwari

et al. 2009

Chem Biol Drug Des

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A series of disubstituted 4(3H) quinazolines were designed for potential application in tumors. Firstly, N-benzoyl anthranilic acid is formed, which undergoes cyclization in the presence of pyridine. Subsequently, nucleophilic attack by semicarbazide on the carbonyl carbon gives 2-substituted 3-carbamido 4(3H) quinazolones, which gives final compound with appropriate substitution. The final as well as intermediate products were confirmed by NMR, FT-IR, and mass spectrometry. In vitro toxicity was performed with different cell lines and showed that the connection of hydrophilic styryl to quinazoline moiety increases its efficacy.

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confidence: 52%

mentioning

confidence: 94%

Disubstituted 4(3H) Quinazolones: A Novel Class of Antitumor Agents

Srivastava

Tiwari

et al. 2009

Chem Biol Drug Des

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“…Radiolabeling of the compounds was carried out by following the procedure described in the literature (18,19). New Zealand Rabbits 2-3 Kg and BALB ⁄ c 22-28 g were used for blood clearance and imaging and biodistribution studies.…”

Section: Kinetic Measurementsmentioning

confidence: 99%

Retracted: Kinetics of Formation for Lanthanide (III) Complexes of DTPA‐(Me‐Trp)₂ used as Imaging Agent

et al. 2011

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Diethlenetriamine-N,N,N'N''N''-pentaacetic acid (DTPA)-bis (amide) analogs have been synthesized and evaluated as a potential biomedical imaging agents. Imaging and biodistribution studies were performed in mice that showed a significant accumulation of DTPA analogs in brain. The stability and protonation constants of the complexes formed between the ligand [DTPA-(Me-Trp)(2)] and Gd(3+), Eu(3+), and Cu(2+) have been determined by pH potentiometry (Gd(3+), Eu(3+)) and spectrophotometry (Cu(2+)) at 25 °C and at constant ionic strength maintained by 0.10 M KCl. The kinetic inertness of Gd [DTPA-(Me-Trp)(2)] was characterized by the rates of exchange reactions with Zn(2+) and Eu(3+). In the Eu(3+) exchange, a second-order [H(+)] dependence was found for the pseudo-first-order rate constant [k(0) = (4.5 ± 1.2) × 10(-6)/s; k(1) = 0.58 ± 0.1 /M/s, k(2) = (6.6 ± 0.2) × 10(4) /M(2)/s, k(3) = (4.8 ± 0.8) × 10(-4) /M/s]. In the Eu(3+) exchange, at pH <5.0, the rate decreases with increasing concentration of the exchanging ion. At physiological pH, the kinetic inertness of [DTPA-(Me-Trp)(2)] is more inert than GdDTPA(2-), the most commonly used MRI contrast agent (t(1/2) = 127 h). High kinetic stability is an important requirement for the Gd complexes used as contrast enhancement agents in magnetic resonance imaging.

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“…In the fused heterocyclic moieties benzimidazole nucleus plays an important pharmacophore with unique chemical and biological properties. [5][6][7][8] They have been found to possess various biological activities like analgesic, antihistaminic, anti-inflammatory, antispasmodic, analgesic, antimicrobial, antitumor, antiproliferative, anti-HIV-RT, antiulcer, antitubercular, anti-cancer and anti-fungal [9][10][11][12] antiinflammatory 13 , proton pump inhibitors 14,15 and cycloxygenase inhibitor activities. [16][17][18][19][20] Some of the benzimidazole derivatives are involved in medicinal treatment such as infertility, epilepsy and diabetic deseases.…”

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confidence: 99%

Untitled

2016

IJPSR

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ABSTRACT:In this study, homology modeling and molecular docking studies were performed to explore structural features and binding mechanism of synthesized benzimidazole derivatives as ubiquitin inhibitors. A homology modeling procedure was employed to construct a 3D model of ubiquitin protein by using MODELLER9.15. For this procedure, the X-ray crystal structure of Gumby / fam105b in Complex with linear Di-ubiquitin (PDB ID: 4KSL) at 2.83 Å resolution was used as template. The predicted model was analyzed by PROCHECK. The 3D structure of predicted model shows 93.9% of amino acids in most favored region. The predicted model was used for molecular docking studies by using Autodock4.2. All the synthesized benzimidazole derivatives show good binding energy and interactions with the model. Compound one shows three interactions with Asp348, Leu297 and Tyr351.

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Synthesis and evaluation of Novel Benzimidazole derivative [Bz-Im] and its radio/biological studies

Cited by 23 publications

References 17 publications

Disubstituted 4(3H) Quinazolones: A Novel Class of Antitumor Agents

Disubstituted 4(3H) Quinazolones: A Novel Class of Antitumor Agents

Retracted: Kinetics of Formation for Lanthanide (III) Complexes of DTPA‐(Me‐Trp)₂ used as Imaging Agent

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Synthesis and evaluation of Novel Benzimidazole derivative [Bz-Im] and its radio/biological studies

Cited by 23 publications

References 17 publications

Disubstituted 4(3H) Quinazolones: A Novel Class of Antitumor Agents

Disubstituted 4(3H) Quinazolones: A Novel Class of Antitumor Agents

Retracted: Kinetics of Formation for Lanthanide (III) Complexes of DTPA‐(Me‐Trp)2 used as Imaging Agent

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Retracted: Kinetics of Formation for Lanthanide (III) Complexes of DTPA‐(Me‐Trp)₂ used as Imaging Agent