Abstract
Objective: Synthesis of N-1 Substituted Indolylchalcone Hybrids and evaluation of anti-angiogenic activity using Chorioallantoic Membrane (CAM) Assay.
 Methods: Claisen-schmidt reaction is used for the synthesis of 30 Indolylchalcone hybrids, it involves condensation of N-1 substituted indole-3-carboxaldehyde and N1 substituted 2-acetyl-benzimidazole. The phase transfer catalyst, a green catalyst such as anhydrous potassium carbonate (K2CO3) and PEG-400 are used in the alkylation and arylation. All synthesized indolylchalcone hybrids were evaluated for their antiangiogenic activity by in vivo-chorioallantoic membrane (CAM) assay method.
 Results: The synthesized indolylchalcone compounds are evaluated. The morphometric study was carried out as described by Melkonian et al. (2002). The Compounds with code C-2, I-1, I-2 are showing the more potent effect on the dose-dependent assay of CAM. The compounds with code C-1, C-3, E-1 to E-3, M-1 and M-5 shows the significant activity, however, though the compounds with code B-1, B-2, CL-1 and A-5 were showing antiangiogenic effect at 0.1 µM, but does not show any significant activity on dose-dependent assay of CAM.
 Conclusion: The synthesized Indolylchalcones as shown in the graph possess very good dose-dependent anti-angiogenic activities. The potency of anti-angiogenetic activity shows that methyl>Ethyl>Cl-benzyl>Benzyl>Isobutyl. 2-acetyl benzimidazole analogs have possible future scope to develop as potent angiogenesis inhibitors.
Highlights
Angiogenesis or neovascularization is a combination of two Greek words, “angio” and “genesis” means vase and birth, respectively
More than 30 y ago, the scientist Folkman proposed that the role of these blood vessel to supply food, oxygen and nutrious to malignant tumor because of that growth was dependent on the development of tumor-associated blood vessels, a process called angiogenesis [2]
We found during our Chorioallantoic Membrane (CAM) Assay Study that there was noticeable decrease in number of blood vessels as compared with the negative control group, as shown in fig. 1A
Summary
Angiogenesis or neovascularization is a combination of two Greek words, “angio” and “genesis” means vase and birth, respectively. The well-known marketed anti-angiogenic inhibitors drug, bevacizumab (Avastin) [6], and sorafenib (Nexavar, BAY 43-9006) and sunitinib malate (Sutent, SU11248) [7] have been approved by the United States Food and Drug Administration for the treatment of cancer patients. These marketed drugs has serious side effects, such as hypertension, bleeding and gastrointestinal perforation; they have been associated with currently available antiVEGF agents, limiting their chronic use [8]. There is an urgent need to find a chalcone hybrid molecule that can be more potent towards cancerous cell and less toxic to normal cell and may overcome the problem of multidrug-resistant strains
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