Inhibition of angiogenesis by THAM-derived cotelomers endowed with thalidomide moieties

Périno, Sandrine; Contino‐Pépin, Christiane; Satchi‐Fainaro, Ronit; Butterfield, Catherine; Pucci, Bernard

doi:10.1016/j.bmcl.2003.10.045

Cited by 12 publications

(4 citation statements)

References 33 publications

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“…Previously, we demonstrated the therapeutic potency of thalidomide derivatives in angiogenesis inhibition [26] and EAE. [27] Although we cannot yet provide details on the precise mechanism of action of thalidomide and its derivatives, herein we have shown enhanced activity from molecular modifications of thalidomide and proposed new therapeutic applications for this "re-discovered" old drug.…”

Section: Discussionmentioning

confidence: 98%

“…These compounds exhibited a significant ability to inhibit angiogenesis in a mouse model of corneal neovascularization when compared to thalidomide. [26] We recently described a novel class of thalidomide analogues substituted on the phthalimide ring system. Among the several structural modifications on the phthalimide ring, the introduction of either a carboxylic function or an N-(aminopropyl)amino group at the C4 position led to a reduction of clinical signs of EAE.…”

Section: Introductionmentioning

confidence: 99%

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Thalidomide Derivatives for the Treatment of Neuroinflammation

Contino‐Pépin¹,

Parat²,

Patinote³

et al. 2010

ChemMedChem

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The precise mechanism-of-action of thalidomide remains uncertain and might differ between diseases and under different clinical condition. With implications in the treatment of a variety of inflammatory and autoimmune diseases, as well as for use as an anticancer agent, alone or in combination with established therapeutics, it is clear that thalidomide and its derivatives deserve further scrutiny. In particular, thalidomide was shown to be effective in a mouse model of multiple sclerosis (MS), an autoimmune inflammatory disorder, called experimental autoimmune encephalomyelitis (EAE). Herein, we describe the synthesis and preliminary biological evaluation of new macromolecular prodrugs of thalidomide bearing an aminoalkyl group on the phthalimide ring. The effectiveness of these compounds to limit EAE was investigated, and it was shown that, at 100 mg kg⁻¹ thalidomide-equivalent dose, they abrogated the clinical and pathological features of EAE.

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Section: Discussionmentioning

confidence: 98%

Section: Introductionmentioning

confidence: 99%

Thalidomide Derivatives for the Treatment of Neuroinflammation

Contino‐Pépin¹,

Parat²,

Patinote³

et al. 2010

ChemMedChem

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“…Moreover, telomer A showed a significant inhibition in the area of neovascularization while 4-carboxy thalidomide resulted in significant changes in the architecture of vessels [180]. Abbas and colleagues have shown that the oral application of thalidomide prevented neovascularization in a rabbit alkali burn model of corneal angiogenesis.…”

Section: Thalidomidementioning

confidence: 97%

Antineovascular Agents in the Treatment of Eye Diseases

Eichler¹,

Yafai²,

Wiedemann³

et al. 2006

CPD

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Neovascularization is a common and potentially visually threatening complication of eye diseases such as diabetic retinopathy (DR) and age-related macular degeneration (AMD). An antiangiogenic therapy is aimed at inhibiting the growth of new blood vessels and should prevent onset or progression of neovascularization. Accumulated evidence indicates that growth factors, endothelial cell surface receptors, and extracellular matrix (ECM) proteins are major mediators of neovascularization and appealing targets for pharmacotherapeutical intervention. Vascular endothelial growth factor (VEGF) plays a critical role in the pathogenesis of retinal neovascularization (in linking tissue ischemia to angiogenesis), and is likely to contribute also significantly to choroidal neovascularization (CNV). Several antineovascular agents antagonize the function of VEGF, by blocking its proangiogenic activity. Indeed, VEGF targeting or disruption of VEGF signalling is the most effective strategy known so far in the pharmacological treatment of ocular neovascularization. Other compounds such as pigment epithelium-derived factor (PEDF) either aim at balancing the levels of pro-angiogenic and angiostatic molecules, target inflammation (cyclooxygenase inhibitors, steroids) or comprise modifiers of the ECM such as inhibitors of matrix metalloproteinases (MMPs) and agents that block the action of integrins. Vascular targeting agents (combretastatin) promote removal of newly formed vessels. This review provides an update on recent investigations directed at the pharmacotherapeutical management of ocular neovascular diseases, placing special emphasis on the underlying target molecules and relevant intracellular signalling pathways.

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“…Briefly, thalidomide carboxylic acid 9 was prepared from 1,2,4-tribenzene-carboxylic anhydride 8 by following reported procedures. 25 …”

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confidence: 99%

Design and biological characterization of hybrid compounds of curcumin and thalidomide for multiple myeloma

Zhang²,

Chojnacki

et al. 2013

Org. Biomol. Chem.

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In our efforts to develop effective treatment agents for human multiple myeloma (MM), a series of hybrid molecules based on the structures of thalidomide (1) and curcumin (2) were designed, synthesized, and biologically characterized in human multiple myeloma MM1S, RPMI8226, U266 cells, and human lung cancer A549 cells. The biological results showed that two hybrid compounds, 5 and 7, exhibited significantly improved lethal effects towards all three human MM cell models compared to 1 or 2 alone, as well as the combination of 1 and 2. Furthermore, mechanistic studies in U266 cells demonstrated that 5 and 7 can induce the production of reactive oxygen species (ROS) and cause G1/S arrest, thus leading to apoptosis and cell death. Additionally, they exhibited inhibitory effects on NFκB activation in A549 cells. Collectively, the results obtained from these hybrid compounds strongly encourage their further optimization as new leads to develop effective treatment agents for human MM.

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Inhibition of angiogenesis by THAM-derived cotelomers endowed with thalidomide moieties

Cited by 12 publications

References 33 publications

Thalidomide Derivatives for the Treatment of Neuroinflammation

Thalidomide Derivatives for the Treatment of Neuroinflammation

Antineovascular Agents in the Treatment of Eye Diseases

Design and biological characterization of hybrid compounds of curcumin and thalidomide for multiple myeloma

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