N-(4-{[4-(1H-Benzoimidazol-2-yl)-arylamino]-methyl}-phenyl)-benzamide derivatives as small molecule heparanase inhibitors

Bioorganic and Medicinal Chemistry Letters

Volumn 16, Issue 2, 2006, Pages 404-408

  Xu, Yong Jiang ^a   Miao, Hua Quan ^a   Pan, Weitao ^a   Navarro, Elizabeth C ^a   Tonra, James R ^a   Mitelman, Stan ^a   Camara, M Margarita ^a   Deevi, Dhanvanthri S ^a   Kiselyov, Alexander S ^a   Kussie, Paul ^a   Wong, Wai C ^a   Liu, Hu ^a  

^a ELI LILLY AND COMPANY   (United States)

Author keywords

Benzimidazole; Heparanase inhibitor

Indexed keywords

BENZAMIDE DERIVATIVE; HEPARANASE; LYASE INHIBITOR; N [4 [[4 (1H BENZOIMIDAZOL 2 YL)PHENYLAMINO]METHYL]PHENYL] 3 BROMO 4 METHOXYBENZAMIDE; N [4 [[5 (1H BENZOIMIDAZOL 2 YL)PYRIDIN 2 YLAMINO]METHYL]PHENYL] 3 BROMO 4 METHOXYBENZAMIDE; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ARTICLE; CONTROLLED STUDY; DRUG ACTIVITY; DRUG BLOOD LEVEL; DRUG SYNTHESIS; ENZYME INHIBITION; IC 50; MOUSE; NONHUMAN;

ADMINISTRATION, ORAL; ANIMALS; BENZAMIDES; BENZIMIDAZOLES; CARBOHYDRATE CONFORMATION; CARBOHYDRATE SEQUENCE; DRUG DESIGN; DRUG EVALUATION, PRECLINICAL; ENZYME INHIBITORS; GLUCURONIDASE; MICE; MODELS, ANIMAL; MOLECULAR SEQUENCE DATA; MOLECULAR STRUCTURE; MOLECULAR WEIGHT; STRUCTURE-ACTIVITY RELATIONSHIP;

ANIMALIA;

EID: 27944476660     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2005.09.070     Document Type: Article

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21. 1H NMR and LCMS.
22. 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).