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

Bioorganic and Medicinal Chemistry Letters

Volumn 16, Issue 2, 2006, Pages 409-412

  Pan, Weitao ^a   Miao, Hua Quan ^a   Xu, Yong Jiang ^a   Navarro, Elizabeth C ^a   Tonra, James R ^a   Corcoran, Erik ^a   Lahiji, Armin ^a   Kussie, Paul ^a   Kiselyov, Alexander S ^a,b   Wong, Wai C ^a   Liu, Hu ^a  

^a ELI LILLY AND COMPANY   (United States)

^b CHEMDIV INC   (United States)

Author keywords

Benzimidazole; Heparanase inhibitor; Urea

Indexed keywords

1,3 BIS[4 (1H BENZOIMIDAZOL 2YL)PHENYL]UREA; 1,3 BIS[4 (5,6 DIMETHYL 1H BENZOIMIDAZOL 2 YL)PHENYL]UREA; CARBANILAMIDE DERIVATIVE; HEPARANASE; LYASE INHIBITOR; UNCLASSIFIED DRUG;

ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL MODEL; ARTICLE; CONTROLLED STUDY; DRUG EFFICACY; DRUG SYNTHESIS; ENZYME INHIBITION; IC 50; METASTASIS; MOUSE; NONHUMAN;

ANIMALS; CARBANILIDES; CELL LINE, TUMOR; DRUG DESIGN; DRUG SCREENING ASSAYS, ANTITUMOR; ENZYME INHIBITORS; GLUCURONIDASE; LUNG NEOPLASMS; MELANOMA, EXPERIMENTAL; MICE; MOLECULAR STRUCTURE; MOLECULAR WEIGHT; NEOPLASM METASTASIS; STRUCTURE-ACTIVITY RELATIONSHIP;

ANIMALIA;

EID: 27944497698     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2005.09.069     Document Type: Article

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18. Unpublished results.
19. 1H NMR and LCMS.
20. 3H-HS-sepharose slurry (25 μl, 4 nM) was then added into the mixture and incubated overnight at 37°C. The reaction buffer was transferred to 96-well Luma plates (Perkin-Elmer). The plates were air-dried and the radioactivity was directly detected in a TopCounter (Perkin-Elmer).