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Literature DB >> 16246560

1-[4-(1H-Benzoimidazol-2-yl)-phenyl]-3-[4-(1H-benzoimidazol-2-yl)-phenyl]-urea derivatives as small molecule heparanase inhibitors.

Weitao Pan¹, Hua-Quan Miao, Yong-Jiang Xu, Elizabeth C Navarro, James R Tonra, Erik Corcoran, Armin Lahiji, Paul Kussie, Alexander S Kiselyov, Wai C Wong, Hu Liu.

Abstract

A novel class of 1-[4-(1H-benzoimidazol-2-yl)-phenyl]-3-[4-(1H-benzoimidazol-2-yl)-phenyl]-ureas are described as potent inhibitors of heparanase. Among them are 1,3-bis-[4-(1H-benzoimidazol-2-yl)-phenyl]-urea (7a) and 1,3-bis-[4-(5,6-dimethyl-1H-benzoimidazol-2-yl)-phenyl]-urea (7d), which displayed good heparanase inhibitory activity (IC(50) 0.075-0.27 microM). Compound 7a showed good efficacy in a B16 metastasis model.

Entities: Chemical

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Year: 2005 PMID： 16246560 DOI： 10.1016/j.bmcl.2005.09.069

Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823

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Cited

16 in total

1. Novel 1, 3-N, O-Spiroheterocyclic compounds inhibit heparanase activity and enhance nedaplatin-induced cytotoxicity in cervical cancer cells.

Authors: Yanan Song; Bin Hu; Hongjie Qu; Lu Wang; Yunxiao Zhang; Jinchao Tao; Jinquan Cui
Journal: Oncotarget Date: 2016-06-14

Review 2. Versatile role of heparanase in inflammation.

Authors: Rachel Goldberg; Amichay Meirovitz; Nir Hirshoren; Raanan Bulvik; Adi Binder; Ariel M Rubinstein; Michael Elkin
Journal: Matrix Biol Date: 2013-03-13 Impact factor: 11.583

3. Primary anti-proliferative activity evaluation of 1-(quinolizidin-1'-yl)methyl- and 1-(ω-tert-amino)alkyl-substituted 2-phenyl-, 2-benzyl- and 2-[(benzotriazol-1/2-yl)methyl]benzimidazoles on human cancer cell lines.

Authors: Michele Tonelli; Bruno Tasso; Lorenzo Mina; Giuseppe Paglietti; Vito Boido; Fabio Sparatore
Journal: Mol Divers Date: 2013-04-13 Impact factor: 2.943

Review 10. The Role of Heparanase and Sulfatases in the Modification of Heparan Sulfate Proteoglycans within the Tumor Microenvironment and Opportunities for Novel Cancer Therapeutics.

Authors: Edward Hammond; Ashwani Khurana; Viji Shridhar; Keith Dredge
Journal: Front Oncol Date: 2014-07-24 Impact factor: 6.244

1-[4-(1H-Benzoimidazol-2-yl)-phenyl]-3-[4-(1H-benzoimidazol-2-yl)-phenyl]-urea derivatives as small molecule heparanase inhibitors.

1. Novel 1, 3-N, O-Spiroheterocyclic compounds inhibit heparanase activity and enhance nedaplatin-induced cytotoxicity in cervical cancer cells.

Review 2. Versatile role of heparanase in inflammation.

3. Primary anti-proliferative activity evaluation of 1-(quinolizidin-1'-yl)methyl- and 1-(ω-tert-amino)alkyl-substituted 2-phenyl-, 2-benzyl- and 2-[(benzotriazol-1/2-yl)methyl]benzimidazoles on human cancer cell lines.

Review 4. Heparanase in inflammation and inflammation-associated cancer.

Review 5. Heparanase enzyme in chronic inflammatory bowel disease and colon cancer.

Review 6. Heparanase: a target for drug discovery in cancer and inflammation.

7. Heparanase Inhibitors Facilitate the Assembly of the Basement Membrane in Artificial Skin.

8. Decrease of laminin-511 in the basement membrane due to photoaging reduces epidermal stem/progenitor cells.

9. Computational Investigation Identified Potential Chemical Scaffolds for Heparanase as Anticancer Therapeutics.

Review 10. The Role of Heparanase and Sulfatases in the Modification of Heparan Sulfate Proteoglycans within the Tumor Microenvironment and Opportunities for Novel Cancer Therapeutics.