Discovery of the first non-ATP competitive IGF-1R kinase inhibitors: Advantages in comparison with competitive inhibitors

Lesuisse, Dominique; Mauger, Jacques; Nemecek, Conception; Maignan, S.; Boiziau, Janine; Harlow, Greg R.; Hittinger, Augustin; Ruf, Swen; Strobel, Hartmut; Nair, Anil C.; Ritter, Kurt; Malleron, Jean-Luc; Dagallier, Anne; El-Ahmad, Youssef; Guilloteau, J.P.; Guizani, Houlfa; Bouchard, Hervé; Venot, Corinne

doi:10.1016/j.bmcl.2011.03.003

Cited by 23 publications

(18 citation statements)

References 16 publications

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“…Imidazolone 87 showed potent IGF‐1R inhibitory potency in HTRF (IC 50 = 98 nM) and ELISA (IC 50 = 7 nM) assay and displayed remarkable anticancer efficacy (IC 50 = 8 nM) in IGF‐1‐dependant cell assay. The good activity of compound 87 might be attributed to the free NH group, which was not only beneficial for the solubility but also helpful for the pronounced bioactivity . Additionally, imidazolone 88 was also able to strongly suppress the migration of prostate cancer (PC‐3) (IC 50 = 8.1 μM) without obvious toxicity up to 200 μM in MTT assay .…”

Section: Imidazoles As Anticancer Agentsmentioning

confidence: 99%

Comprehensive Review in Current Developments of Imidazole-Based Medicinal Chemistry

et al. 2013

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Imidazole ring is an important five-membered aromatic heterocycle widely present in natural products and synthetic molecules. The unique structural feature of imidazole ring with desirable electron-rich characteristic is beneficial for imidazole derivatives to readily bind with a variety of enzymes and receptors in biological systems through diverse weak interactions, thereby exhibiting broad bioactivities. The related research and developments of imidazole-based medicinal chemistry have become a rapidly developing and increasingly active topic. Particularly, numerous imidazole-based compounds as clinical drugs have been extensively used in the clinic to treat various types of diseases with high therapeutic potency, which have shown the enormous development value. This work systematically gives a comprehensive review in current developments of imidazole-based compounds in the whole range of medicinal chemistry as anticancer, antifungal, antibacterial, antitubercular, anti-inflammatory, antineuropathic, antihypertensive, antihistaminic, antiparasitic, antiobesity, antiviral, and other medicinal agents, together with their potential applications in diagnostics and pathology. It is hoped that this review will be helpful for new thoughts in the quest for rational designs of more active and less toxic imidazole-based medicinal drugs, as well as more effective diagnostic agents and pathologic probes.

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Section: Imidazoles As Anticancer Agentsmentioning

confidence: 99%

Comprehensive Review in Current Developments of Imidazole-Based Medicinal Chemistry

et al. 2013

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“…In particular, several reports present interest in cancer research. 10,11 Cancer is one of the most devastating diseases of today. It is manifested as uncontrolled growth of cells and invasion or intrusion into and the destruction of adjacent tissues.…”

Section: Introductionmentioning

confidence: 99%

Structure-activity relationships of 3-substituted-5,5- diphenylhydantoins as potential antiproliferative and antimicrobial agents

Trišović¹,

Božić²,

Obradović

et al. 2011

JSCS

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A series of twelve 3-substituted-5,5-diphenylhydantoins was synthesized, including some whose anticonvulsant activities have already been reported in the literature. Their antiproliferative activities against HCT-116 human colon carcinoma cells were evaluated to determine structure-activity relationships. Almost all of the compounds exhibited statistically significant antiproliferative effects at a concentration of 100 μM, while the derivative bearing a benzyl group was active even at lower concentrations. Moreover, their in vitro antibacterial activities against Escherichia coli ATCC 25922, Staphylococcus aureus ATCC 25923 and clinical isolates of Escherichia coli, Proteus mirabilis, Pseudomonas aeruginosa, Enterococcus faecalis and Staphylococcus aureus were evaluated. Only the 3-iso-propyl and 3-benzyl derivatives showed weak antibacterial activities against the Gram-positive bacterium E. faecalis and the Gram-negative bacteria E. coli ATCC 25922 and E. coli

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“…A dataset of 164 IGF-1R inhibitors with their IC 50 values were collected from a Binding-DB database [8,12,13]. The biological activity values (IC 50 ) were converted into the negative logarithmic pIC (-logIC 50 +6).…”

Section: Dataset Collection and Fragmentationmentioning

confidence: 99%

Application of Group-Based QSAR and Molecular Docking in the Design of Insulin-Like Growth Factor Antagonists

Abdullahi¹,

Abdualkader²,

Abdulsamat³

et al. 2015

Trop. J. Pharm Res

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Purpose: To identify the structural requirements for designing a lead key for insulin-like growth factor (IGF-1R) inhibition using group-based quantitative structure activity relationship (GQSAR Met 1126, Arg, 1128, Met 1052, GLU 1050, Met 1112, Leu 1051, Met 1049, Val 1033 at ATP binding sites of IGF-1R kinase domain. Conclusion:The generated models provide a site-specific insight into the structural requirements for IGF-1R inhibition which can be used to design and develop potent inhibitors.

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Discovery of the first non-ATP competitive IGF-1R kinase inhibitors: Advantages in comparison with competitive inhibitors

Cited by 23 publications

References 16 publications

Comprehensive Review in Current Developments of Imidazole-Based Medicinal Chemistry

Comprehensive Review in Current Developments of Imidazole-Based Medicinal Chemistry

Structure-activity relationships of 3-substituted-5,5- diphenylhydantoins as potential antiproliferative and antimicrobial agents

Application of Group-Based QSAR and Molecular Docking in the Design of Insulin-Like Growth Factor Antagonists

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