Journal: Bioorganic chemistry

Article Title: New quinoline/chalcone hybrids as anti-cancer agents: Design, synthesis, and evaluations of cytotoxicity and PI3K inhibitory activity

doi: 10.1016/j.bioorg.2018.10.064

Figure Lengend Snippet: GI 50 of compounds 9i and 9j against 59 cell lines in 9 different cancer panels tested using NCI’s in vitro five dose anticancer assay.

Article Snippet: The presence of such geometry might also be responsible for the absence of the 2-pyrazoline cyclization usually observed in hydrazide-chalcone reactions. fig ft0 fig mode=article f1 fig/graphic|fig/alternatives/graphic mode="anchored" m1 Open in a separate window Fig. 2. caption a7 Possible stacking interaction for compound 9i . fig ft0 fig mode=article f1 fig/graphic|fig/alternatives/graphic mode="anchored" m1 Open in a separate window Scheme 1. caption a7 Synthesis of ( E )- N’ -(( Z )-1-(4-aminophenyl)-3-phenylallylidene)-2-(phenyl)quinoline-4-carbohydrazide derivatives 9a-t . table ft1 table-wrap mode="anchored" t5 caption a7 Panel/cell line GI 50 Compound Panel/cell line GI 50 Compound 9i 9j 9i 9j Leukemia Melanoma CCRF-CEM 5.84 4.53 LOX IMVI 1.56 4.00 HL-60(TB) 2.54 3.49 MALME-3M > 100 > 100 K-562 1.05 3.09 M14 1.16 2.54 MOLT-4 3.30 3.23 MDA-MB-435 0.305 1.00 RPMI-8226 3.86 4.10 SK-MEL-2 2.03 3.81 SR 0.595 3.29 SK-MEL-28 3.78 6.23 Non-small cell lung cancer SK-MEL-5 0.701 2.50 A549/ATCC 2.33 4.79 UACC-257 > 100 33.7 EKVX 3.78 3.99 UACC-62 0.556 2.06 HOP-62 3.21 4.62 Ovarian cancer HOP-92 1.92 4.10 IGROV1 4.98 6.48 NCI-H226 7.54 6.47 OVCAR-3 0.462 2.98 NCI-H23 3.14 5.02 OVCAR-4 1.82 4.71 NCI-H322M 6.00 4.73 OVCAR-5 5.51 8.43 NCI-H460 1.89 3.51 OVCAR-8 4.16 5.25 NCI-H522 0.307 0.622 NCI/ADR-RES 0.519 2.54 Colon cancer SK-OV-3 3.32 4.94 COLO 205 1.99 2.80 Renal cancer HCC-2998 3.40 4.28 786–0 1.84 4.22 HCT-116 1.41 3.18 A498 0.375 1.64 HCT-15 1.03 3.33 ACHN 1.47 4.19 HT29 1.13 3.35 RXF 393 0.698 1.63 KM12 1.15 3.46 SN12C 4.27 6.84 SW-620 1.24 4.24 TK-10 52.30 8.51 CNS cancer UO-31 1.55 2.20 SF-268 2.19 4.09 SF-295 0.540 3.13 Breast cancer SF-539 1.41 2.43 MCF7 0.442 2.53 SNB-19 5.54 6.51 MDA-MB231/ATCC 3.28 3.94 SNB-75 0.371 1.41 HS 578T 1.05 4.68 U251 2.18 4.51 BT-549 2.04 3.92 Prostate cancer T-47D 2.70 2.73 PC-3 2.03 3.40 MDA-MB-468 2.95 4.91 DU-145 3.16 3.68 Open in a separate window GI 50 of compounds 9i and 9j against 59 cell lines in 9 different cancer panels tested using NCI’s in vitro five dose anticancer assay.

Techniques: In Vitro

Journal: ChemMedChem

Article Title: A Structure-Activity Relationship Study of the Antimalarial and Antileishmanial Activities of Nonpeptide Macrocyclic Histone Deacetylase Inhibitors

doi: 10.1002/cmdc.201000087

Figure Lengend Snippet: In vitro inhibition of pfHDAC-1 by selected lead HDACi. [a]

Article Snippet: This may be partly due to differences in the cell penetration abilities of these compounds. table ft1 table-wrap mode="anchored" t5 caption a7 Lead IC 50 [nm] 1 134±4.5 2 93±3.6 4 62±5.3 5 30±2.7 7 29±0.9 15 401±19.7 16 182±13.6 SAHA 98±2.8 Open in a separate window [a] Data obtained through contract arrangement with BPS Bioscience (San Diego, USA; www.bpsbioscience.com ).

Techniques: In Vitro, Inhibition

Journal: International Journal of Molecular Sciences

Article Title: The Role of Irisin/FNDC5 Expression and Its Serum Level in Breast Cancer

doi: 10.3390/ijms24108628

Figure Lengend Snippet: Comparison of FNDC5/Ir (( A )—IRS score 8) expression with E-cadherin (( B )—IRS score 12), N-cadherin (( C )—IRS score 8), SNAIL (( D )—IRS score 3 and % of nuclear expression 4, ( E )—IRS score 12 and % of nuclear expression 4), SLUG (( F )—IRS score 8 and % of nuclear expression 3) and TWIST (( G )—IRS score 4 and % of nuclear expression 2, ( H )—IRS score 4 and % of nuclear expression 2) using immunohistochemistry (IHC) (positive reactions—brown cell cytoplasm) in breast cancer (BC), magnification ×200.

Article Snippet: The expression of proteins was detected by specific primary antibodies, i.e., polyclonal rabbit: anti-irisin/FNDC5 (dilution 1:50; code no. NBP2-14024; Novus Biologicals, Littleton, CO, USA) and anti-SNAIL (1:400, Clone, code 13099-1-AP, Proteintech, Rosemont, IL, USA), monoclonal mouse: anti-E-cadherin antibody (ready to use, Clone NCH-38, code IR059; Dako, Glostrup, Denmark), anti-N-cadherin (1:50, Clone 6G11, code M3613; Dako), anti-SLUG (1:50, clone A-7, sc-166476, Santa Cruz Biotechnology, Santa Cruz, CA, USA), and monoclonal mouse anti-TWIST (dilution 1:50, clone Twist2C1a, code ab-50887, Abcam, Cambridge, UK).

Techniques: Expressing, Immunohistochemistry

Journal: International Journal of Molecular Sciences

Article Title: The Role of Irisin/FNDC5 Expression and Its Serum Level in Breast Cancer

doi: 10.3390/ijms24108628

Figure Lengend Snippet: Correlation of FNDC5/Ir expression level with E-cadherin ( A ) and N-cadherin ( B ), cytoplasmic ( C ) and nuclear ( D ) SNAIL expression levels, cytoplasmic ( E ) and nuclear ( F ) SLUG expression levels, cytoplasmic ( G ) and nuclear ( H ) TWIST expression levels in breast cancer (BC) (sample size n = 541).

Article Snippet: The expression of proteins was detected by specific primary antibodies, i.e., polyclonal rabbit: anti-irisin/FNDC5 (dilution 1:50; code no. NBP2-14024; Novus Biologicals, Littleton, CO, USA) and anti-SNAIL (1:400, Clone, code 13099-1-AP, Proteintech, Rosemont, IL, USA), monoclonal mouse: anti-E-cadherin antibody (ready to use, Clone NCH-38, code IR059; Dako, Glostrup, Denmark), anti-N-cadherin (1:50, Clone 6G11, code M3613; Dako), anti-SLUG (1:50, clone A-7, sc-166476, Santa Cruz Biotechnology, Santa Cruz, CA, USA), and monoclonal mouse anti-TWIST (dilution 1:50, clone Twist2C1a, code ab-50887, Abcam, Cambridge, UK).

Techniques: Expressing