Design, synthesis, and biological evaluation of novel 4-hydro-quinoline-3- carboxamide derivatives as an immunomodulator

Bioorganic and Medicinal Chemistry Letters

Volumn 15, Issue 12, 2005, Pages 2980-2985

  He, Jun Feng ^a   Yun, Liu Hong ^a   Yang, Ri Fang ^a   Xiao, Zhi Yong ^a   Cheng, Jun Ping ^a   Zhou, Wen Xia ^a   Zhang, Yong Xiang ^a  

^a BEIJING INSTITUTE OF PHARMACOLOGY AND TOXICOLOGY   (China)

Author keywords

Immunomodulator; Linomide; Quinoline 3 carboxamide; SAR

Indexed keywords

AMIDE; FR 137316; IMMUNOMODULATING AGENT; QUINOLINE DERIVATIVE; ROQUINIMEX; TUMOR NECROSIS FACTOR ALPHA; UNCLASSIFIED DRUG;

ANIMAL CELL; ARTICLE; CONTROLLED STUDY; CYTOKINE PRODUCTION; DRUG DESIGN; DRUG POTENCY; DRUG SCREENING; DRUG SYNTHESIS; IMMUNOMODULATION; IN VITRO STUDY; LYMPHOCYTE PROLIFERATION; MACROPHAGE; MOUSE; NONHUMAN; SPLEEN LYMPHOCYTE;

ANIMALS; CELL PROLIFERATION; CELLS, CULTURED; DRUG DESIGN; DRUG SCREENING ASSAYS, ANTITUMOR; HYDROXYQUINOLINES; IMMUNOLOGIC FACTORS; LYMPHOCYTES; MACROPHAGES; QUINOLINES; RATS; SPLEEN; TUMOR NECROSIS FACTOR-ALPHA;

EID: 19844382770     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2005.04.040     Document Type: Article

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16. 2 and 95% humidity. The experiments were started when the cells were growing confluently (after approx. 3 days).To stimulate the macrophages, lipopolysaccharide (LPS; Sigma-Aldrich) was added at 10 μg/mL. The final concentration of drug was 1, 10, and 100 μg/mL, respectively. After 24 h incubation, supernatants were collected to measure the TNF-α level. The level of TNF-α in the supernatants was measured with commercial ELISA kits according to the instructions of the producer and the results were expressed as mean ± SD pg/mL. The activity was expressed as a %inhibition of TNF-α production. The %inhibition = (the mean of control well - the mean of administered drug well)/the mean of control well
17. 6, δ): 11.07 (s, 1H), 7.79 (d, 1H, J = 6.2 Hz), 7.62 (s, 1H), 7.18-7.29 (m, 5H), 7.08-7.11 (m, 1H), 3.79 (q, 2H, J = 7.0 Hz), 2.38 (s, 3H), 2.31 (s, 3H), 1.07 (t, 3H, J = 7.0 Hz)