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: Antimicrobial Agents and Chemotherapy

Article Title: Activity of Sanguinarine against Candida albicans Biofilms

doi: 10.1128/AAC.02259-16

Figure Lengend Snippet: MICs of SAN and fluconazole against C. albicans strains a

Article Snippet: In contrast, as much as 1,024 μg/ml of fluconazole could inhibit biofilm formation only by about 60% ( ) or destroy mature biofilms by 29.9% ( ). table ft1 table-wrap mode="anchored" t5 TABLE 1 caption a7 Strains SAN Fluconazole MIC 80 MIC 50 MIC 80 MIC 50 SC5314 3.2 3.2 0.25 0.125 ATCC 14053 3.2 1.6 0.5 0.25 {"type":"entrez-protein","attrs":{"text":"SCZ60053","term_id":"1081663679","term_text":"SCZ60053"}} SCZ60053 3.2 1.6 >64 0.25 {"type":"entrez-protein","attrs":{"text":"SCZ60054","term_id":"1081601568","term_text":"SCZ60054"}} SCZ60054 3.2 1.6 >64 0.125 Open in a separate window a Values are in micrograms per milliliter.

Techniques:

Journal: Antimicrobial Agents and Chemotherapy

Article Title: Activity of Sanguinarine against Candida albicans Biofilms

doi: 10.1128/AAC.02259-16

Figure Lengend Snippet: SAN inhibits C. albicans biofilm formation in vitro. Biofilm formation was evaluated using an XTT reduction assay, and the results are presented as the percent SAN- or fluconazole-treated biofilm relative to control biofilm formed without treatment. The results represent means ± standard deviations for three independent experiments. *, P < 0.05; **, P < 0.01; ***, P < 0.001; ****, P < 0.0001 (one-way analysis of variance [ANOVA]). (A) Effects of different concentrations of SAN or fluconazole on biofilm formation. (B) Effects of different concentrations of SAN or fluconazole on mature biofilms. (C) Effects of different concentrations of SAN on biofilm formation, shown in SEM images. Images in the dotted boxes are enlarged in the rightmost column.

Article Snippet: In contrast, as much as 1,024 μg/ml of fluconazole could inhibit biofilm formation only by about 60% ( ) or destroy mature biofilms by 29.9% ( ). table ft1 table-wrap mode="anchored" t5 TABLE 1 caption a7 Strains SAN Fluconazole MIC 80 MIC 50 MIC 80 MIC 50 SC5314 3.2 3.2 0.25 0.125 ATCC 14053 3.2 1.6 0.5 0.25 {"type":"entrez-protein","attrs":{"text":"SCZ60053","term_id":"1081663679","term_text":"SCZ60053"}} SCZ60053 3.2 1.6 >64 0.25 {"type":"entrez-protein","attrs":{"text":"SCZ60054","term_id":"1081601568","term_text":"SCZ60054"}} SCZ60054 3.2 1.6 >64 0.125 Open in a separate window a Values are in micrograms per milliliter.

Techniques: In Vitro, Control

Journal: Antimicrobial Agents and Chemotherapy

Article Title: Activity of Sanguinarine against Candida albicans Biofilms

doi: 10.1128/AAC.02259-16

Figure Lengend Snippet: Effects of different concentrations of SAN on hypha formation. Exponentially growing C. albicans SC5314 cells were transferred to hypha-inducing liquid media. The cellular morphology was photographed after incubation at 37°C for 3.5 h. Bars, 100 μm.

Article Snippet: In contrast, as much as 1,024 μg/ml of fluconazole could inhibit biofilm formation only by about 60% ( ) or destroy mature biofilms by 29.9% ( ). table ft1 table-wrap mode="anchored" t5 TABLE 1 caption a7 Strains SAN Fluconazole MIC 80 MIC 50 MIC 80 MIC 50 SC5314 3.2 3.2 0.25 0.125 ATCC 14053 3.2 1.6 0.5 0.25 {"type":"entrez-protein","attrs":{"text":"SCZ60053","term_id":"1081663679","term_text":"SCZ60053"}} SCZ60053 3.2 1.6 >64 0.25 {"type":"entrez-protein","attrs":{"text":"SCZ60054","term_id":"1081601568","term_text":"SCZ60054"}} SCZ60054 3.2 1.6 >64 0.125 Open in a separate window a Values are in micrograms per milliliter.

Techniques: Incubation

Journal: Antimicrobial Agents and Chemotherapy

Article Title: Activity of Sanguinarine against Candida albicans Biofilms

doi: 10.1128/AAC.02259-16

Figure Lengend Snippet: The effect of SAN is associated with suppression of the cAMP pathway. (A) Real-time RT-PCR results for some important adhesion/filamentation-related genes. Gene expression fold changes are relative to results of the control group (C. albicans SC5314 without SAN treatment). 18S rRNA was used to normalize the expression data. Data are means ± standard deviations from three independent experiments. *, P < 0.05; **, P < 0.01; ***, P < 0.001 (unpaired t test). (B) Endogenous cAMP levels of C. albicans. Intracellular cAMP levels of C. albicans in the group treated with 1.6 μg/ml of SAN and the control group were determined. The results represent means ± standard deviations from three independent experiments. *, P < 0.05 (unpaired t test). (C) Exogenous cAMP reverted the morphological transition defect of C. albicans caused by SAN. The cellular morphology was photographed after incubation in RPMI 1640 medium at 37°C for 3.5 h. Bars, 100 μm.

Article Snippet: In contrast, as much as 1,024 μg/ml of fluconazole could inhibit biofilm formation only by about 60% ( ) or destroy mature biofilms by 29.9% ( ). table ft1 table-wrap mode="anchored" t5 TABLE 1 caption a7 Strains SAN Fluconazole MIC 80 MIC 50 MIC 80 MIC 50 SC5314 3.2 3.2 0.25 0.125 ATCC 14053 3.2 1.6 0.5 0.25 {"type":"entrez-protein","attrs":{"text":"SCZ60053","term_id":"1081663679","term_text":"SCZ60053"}} SCZ60053 3.2 1.6 >64 0.25 {"type":"entrez-protein","attrs":{"text":"SCZ60054","term_id":"1081601568","term_text":"SCZ60054"}} SCZ60054 3.2 1.6 >64 0.125 Open in a separate window a Values are in micrograms per milliliter.

Techniques: Quantitative RT-PCR, Gene Expression, Control, Expressing, Incubation

Journal: Bioorganic chemistry

Article Title: Design, synthesis and biological evaluation of fused naphthofuro[3,2- c ] quinoline-6,7,12-triones and pyrano[3,2- c ]quinoline-6,7,8,13-tetraones derivatives as ERK inhibitors with efficacy in BRAF-mutant melanoma

doi: 10.1016/j.bioorg.2018.10.044

Figure Lengend Snippet: The main cytotoxic parameters (GI 50 , TGI and LC 50 ) of compound 3b in μM.

Article Snippet: Accordingly, we decided to go further and test this hypothesis. table ft1 table-wrap mode="anchored" t5 caption a7 Tumor cell lines GI 50 TGI LC 50 Leukemia CCRF-CEM 0.41 4.86 > 100 HL-60 (TB) 1.70 5.25 34.76 K-562 0.37 2.00 50.12 MOLT-4 0.44 3.16 > 100 RPMI-8226 0.39 2.63 > 100 SR 0.50 3.98 > 100 Non-small cell lung cancer A549/ATCC 1.02 2.88 8.32 EKVX 0.25 2.45 26.30 HOP-62 0.20 0.65 3.24 HOP-92 0.15 0.39 1.00 NCI-H226 0.14 0.35 0.87 NCI-H23 0.35 1.82 7.08 NCI-H322M 0.32 1.45 7.24 NCI-H460 0.22 0.49 1.48 NCI-H522 0.32 1.38 8.13 Colon cancer COLO 205 10.47 27.54 72.44 HCC-2998 063 2.57 9.12 HCT-116 0.31 1.10 4.57 HCT-15 0.21 0.51 2.00 HT29 3.72 12.88 39.81 KM 12 0.45 3.02 27.54 SW-620 0.33 1.00 7.59 CNS cancer SF-268 0.46 3.98 48.98 SF-295 0.63 2.29 6.61 SF-539 0.23 0.56 2.09 SNB-19 0.31 1.10 6.17 SNB-75 0.16 0.42 1.29 U251 0.27 0.76 2.82 Melanoma LOX IMVI 0.32 1.32 3.98 MALME-3M 0.23 044 0.85 M14 0.40 1.51 4.57 MDA-MB-435 0.30 1.20 4.07 SK-MEL-2 1.74 5.13 19.95 SK-MEL-28 0.34 1.23 4.68 SK-MEL-5 1.30 1.20 3.72 UACC-257 1.32 3.39 8.51 UACC-62 0.28 1.15 3.98 Ovarian cancer IGROV1 0.22 0.74 3.47 OVCAR-3 0.24 0.56 1.82 OVCAR-4 0.17 0.45 1.51 OVCAR-5 3.47 14.79 40.74 OVCAR-8 0.39 2.29 30.20 NCI/ADR-RES 0.35 1.78 34.67 SK-OV-3 0.35 1.78 5.62 Renal cancer 786–0 0.22 0.54 2.45 A498 0.21 0.95 3.55 ACHN 0.20 0.58 2.63 RXF 393 0.21 0.58 2.51 SN12C 0.20 0.47 1.35 TK-10 0.38 1.10 6.03 UO-31 0.19 0.60 2.51 Prostate cancer PC-3 0.18 0.46 1.58 DU-145 0.28 0.78 12.30 Breast cancer MCF7 0.23 1.05 18.62 MDA-MB-231/ATCC 0.17 0.51 2.82 HS 578 T 0.26 1.38 > 100 BT-549 0.30 1.32 6.76 T-47D 0.26 0.98 5.13 MDA-MB-468 0.25 0.87 4.57 Open in a separate window The main cytotoxic parameters (GI 50 , TGI and LC 50 ) of compound 3b in μM.

Techniques: