Discovery of a novel class of potent and orally bioavailable sphingosine 1-phosphate receptor 1 antagonists

Journal of Medicinal Chemistry

Volumn 55, Issue 3, 2012, Pages 1368-1381

  Ibrahim, Mohamed A ^a   Johnson, Henry W B ^a   Jeong, Joon Won ^a   Lewis, Gary L ^a   Shi, Xian ^a   Noguchi, Robin T ^a   Williams, Matthew ^a   Leahy, James W ^a   Nuss, John M ^a   Woolfrey, John ^a   Banica, Monica ^a   Bentzien, Frauke ^a   Chou, Yu Chien ^a   Gibson, Anna ^a   Heald, Nathan ^a   Lamb, Peter ^a   Mattheakis, Larry ^a   Matthews, David ^a   Shipway, Aaron ^a   Wu, Xiang ^a   Zhang, Wentao ^a   Zhou, Sihong ^a   Shankar, Geetha ^a   more..

^a EXELIXIS INC   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

1 [2 (1H 1,2,3 TRIAZOL 1 YL)ACETYL] 4 (4 FLUOROBENZYL)N[4 (4 FLUOROPHENOXY)PHENYL]PYRROLIDINE 2 CARBOXAMIDE; 1 [2 (1H 1,2,4 TRIAZOL 1 YL)ACETYL] 4 (4 FLUOROBENZYL)N[4 (4 FLUOROPHENOXY)PHENYL]PYRROLIDINE 2 CARBOXAMIDE; 1 [2 (1H 1,2,4 TRIAZOL 1 YL)ACETYL] 4 BENZYL N(4 PHENOXYPHENYL)PYRROLIDINE 2 CARBOXAMIDE; 1 [2 (1H 1,2,4 TRIAZOL 1 YL)ACETYL]N(4 PHENOXY PHENYL) 4 PHENYLPYRROLIDINE 2 CARBOXAMIDE; 1 [2 (1H IMIDAZOL 5 YL)ACETYL] 4 BENZYL N (4 PHENOXYPHENYL)PYRROLIDINE 2 CARBOXAMIDE; 1 [2 (1H IMIDAZOL 5 YL)ACETYL] 4 BENZYL N[4 (4 FLUOROPHENOXY)PHENYL]PIPERAZINE 2 CARBOXAMIDE; 1 [2 (1H IMIDAZOL 5 YL)ACETYL]N(4 PHENOXYPHENYL) 4 PHENYLPYRROLIDINE 2 CARBOXAMIDE; 1 [2 (2H 1,2,3 TRIAZOL 2 YL)ACETYL] 4 (4 FLUOROBENZYL)N[4 (4 FLUOROPHENOXY)PHENYL)PYRROLIDINE 2 CARBOXAMIDE; 1 [2 (2H 1,2,3 TRIAZOL 2 YL)ACETYL] 4 (4 FLUOROBENZYL)N[4 (4 FLUOROPHENOXY)PHENYL]PYRROLIDINE 2 CARBOXAMIDE; 2 [2 (1H IMIDAZOL 5 YL)ACETAMIDO] 3 (BENZYLOXY)(DIBENZO FURAN 2 YL)PROPANAMIDE; 2 [2 (1H IMIDAZOL 5 YL)ACETAMIDO] 3 (BENZYLOXY)N METHYL N (4 PHENOXYPHENYL)PROPANAMIDE; 2 [2 (1H IMIDAZOL 5 YL)ACETAMIDO] 3 (BENZYLOXY)N(3 CHLORO 4 PHENOXYPHENYL)PROPANAMIDE; 2 [2 (1H IMIDAZOL 5 YL)ACETAMIDO] 3 (BENZYLOXY)N(4 BENZYLPHENYL)PROPANAMIDE; 2 [2 (1H IMIDAZOL 5 YL)ACETAMIDO] 3 (BENZYLOXY)N(BIPHENYL 4 YL)PROPANAMIDE; 2 [2 (1H IMIDAZOL 5 YL)ACETAMIDO] 3 (BENZYLOXY)N(DIBENZO FURAN 2 YL)PROPANAMIDE; 2 [2 (1H IMIDAZOL 5 YL)ACETAMIDO] 3 (BENZYLOXY)N[4 (3 CHLOROPHENOXY)PHENYL]PROPANAMIDE; 2 [2 (1H IMIDAZOL 5 YL)ACETAMIDO] 3 (BENZYLOXY)N[4 (4 CHLOROPHENOXY)PHENYL]PROPANAMIDE; 2 [2 (1H IMIDAZOL 5 YL)ACETAMIDO] 3 (BENZYLOXY)N[4 (4 FLUOROPHENOXY)PHENYL]PROPANAMIDE; 2 [2 (1H IMIDAZOL 5 YL)ACETAMIDO] 3 (BENZYLOXY)N[4 (BENZYLOXY)PHENYL]PROPANAMIDE; 2 [2 (1H IMIDAZOL 5 YL)ACETAMIDO] 3 (BENZYLOXY)N[4 (CYCLOHEXYLOXY)PHENYL]PROPANAMIDE; 2 [2 (1H IMIDAZOL 5 YL)ACETAMIDO] 3 (BENZYLOXY)N[4 (PHENYLAMINO)PHENYL]PROPANAMIDE; 2 [2 (1H IMIDAZOL 5 YL)ACETAMIDO] 3 (BENZYLOXY)N[4- 2 CHLOROPHENOXY)PHENYL]PROPANAMIDE; 2 [2 (1H IMIDAZOL 5 YL)ACETAMIDO]N(4 PHENOXYPHENYL) 5 PHENYLPENTANAMIDE; 2 [2 (1H IMIDAZOL 5 YL)N METHYLACETAMIDO] 3 (BENZYLOXY)N(4 PHENOXYPHENYL)PROPANAMIDE; ANTINEOPLASTIC AGENT; RECEPTOR BLOCKING AGENT; UNCLASSIFIED DRUG; XL 541;

ANIMAL EXPERIMENT; ANIMAL MODEL; ANTINEOPLASTIC ACTIVITY; AREA UNDER THE CURVE; ARTICLE; BREAST ADENOCARCINOMA; CANCER INHIBITION; CONTROLLED STUDY; DRUG BIOAVAILABILITY; DRUG EFFICACY; DRUG HALF LIFE; DRUG POTENCY; DRUG SYNTHESIS; EXPERIMENTAL DOG; EXPERIMENTAL MONKEY; HIGH THROUGHPUT SCREENING; IC 50; IN VIVO STUDY; MAXIMUM PLASMA CONCENTRATION; MOUSE; NONHUMAN; RAT;

ADMINISTRATION, ORAL; AMIDES; ANGIOGENESIS INHIBITORS; ANILINE COMPOUNDS; ANIMALS; ANTINEOPLASTIC AGENTS; BIOLOGICAL AVAILABILITY; CELL LINE; CELL PROLIFERATION; DOGS; HAPLORHINI; HIGH-THROUGHPUT SCREENING ASSAYS; MICE; NEOVASCULARIZATION, PATHOLOGIC; PROLINE; RATS; RECEPTORS, LYSOSPHINGOLIPID; SERINE; STEREOISOMERISM; XENOGRAFT MODEL ANTITUMOR ASSAYS;

EID: 84863116381     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm201533b     Document Type: Article

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