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Life Sci. 2013 Nov 26;93(23):904-11. doi: 10.1016/j.lfs.2013.10.001. Epub 2013 Oct 15.

Synthesis, angiopreventive activity, and in vivo tumor inhibition of novel benzophenone-benzimidazole analogs.

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  • 1Department of Chemistry, Yuvaraj's College (Autonomous), University of Mysore, Mysore 570 005, Karnataka, India.

Abstract

AIM:

The development of anticancer drugs with specific targets is of prime importance in modern biology. This study investigates the angiopreventive and in vivo tumor inhibition activities of novel synthetic benzophenone-benzimidazole analogs.

MAIN METHODS:

The multistep synthesis of novel benzophenone-benzimidazole analogs (8a-n) allowing substitution with methoxy, methyl and halogen groups at different positions on the identical chemical backbone and the variations in the number of substituents were synthesized and characterized. The newly synthesized compounds were further evaluated for cytotoxic and antiproliferative effects against Ehrlich ascites carcinoma (EAC) cells. The potent lead compounds were further assessed for antiangiogenic effects in a CAM model and a tumor-induced vasculature in vivo model. The effect of angioprevention on tumor growth was verified in a mouse model.

KEY FINDINGS:

The cytotoxicity studies revealed that compounds 8f and 8n are strongly cytotoxic. Analyzing the structure-activity relationship, we found that an increase in the number of methyl groups in addition to methoxy substitution at the para position of the benzoyl ring in compound 8n resulted in higher potency compared to 8f. Furthermore, neovessel formation in in vivo systems, such as the chorioallantoic membrane (CAM) and tumor-induced mice peritoneum models, was significantly suppressed and reflected the tumor inhibition observed in mice.

SIGNIFICANCE:

These results suggest the potential clinical application of compound 8n as an antiangiogenic drug for cancer therapy.

© 2013 Elsevier Inc. All rights reserved.

KEYWORDS:

Angioprevention; Benzophenone–benzimidazoles; Cytotoxicity; Methoxy group

PMID:
24135459
[PubMed - indexed for MEDLINE]
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