Journal: Bioorganic & medicinal chemistry letters

Article Title: Synthesis and in vitro screening of novel N -benzyl aplysinopsin analogs as potential anticancer agents

doi: 10.1016/j.bmcl.2011.01.020

Figure Lengend Snippet: Antitumor activity (GI 50 / μM) a and toxicity (LC 50 / μM) b data of compounds selected for 5 dose studies for the NCI 60-cell lines screen

Article Snippet: The results are presented in . table ft1 table-wrap mode="anchored" t5 caption a7 Panel/cell line Compound 3a Compound 3i GI 50 LC 50 GI 50 LC 50 Leukemia Cancer CCRF-CEM 3.06 >100 >100 >100 HL-60(TB) 2.54 >100 >100 >100 K-562 0.97 >100 77.6 >100 MOLT-4 1.38 >100 >100 >100 RPMI-8226 3.61 >100 >100 >100 Non-Small Cell Lung Cancer A549/ATCC 4.44 >100 0.77 >100 EKVX 4.22 >100 >100 >100 HOP-62 3.58 73.0 >100 >100 HOP-92 na na >100 NCI-H226 5.94 >100 80.7 >100 NCI-H23 4.07 >100 60.1 >100 NCI-H322M 0.72 >100 71.0 >100 NCI-H460 2.91 >100 >100 >100 NCI-H522 na na 11.0 >100 Colon Cancer COLO 205 3.16 >100 >100 >100 HCC-2998 2.43 85.0 >100 >100 HCT-116 1.21 >100 5.41 >100 HCT-15 na na >100 >100 HT29 5.99 >100 20.8 >100 KM12 3.73 >100 7.49 >100 SW-620 2.27 >100 38.3 >100 CNS Cancer SF-268 4.22 >100 32.0 >100 SF-295 3.09 >100 >100 >100 SF-539 2.39 >100 4.40 >100 SNB-19 3.77 >100 >100 >100 SNB-75 4.60 >100 2.47 >100 U-251 2.03 59.1 2.94 >100 Melanoma Cancer LOX IMVI 1.43 >100 2.32 >100 MALME-3M 2.01 >100 23.5 >100 M14 1.43 >100 57.2 >100 MDA-MB-435 2.76 >100 32.4 >100 SK-MEL-2 0.30 30.6 >100 >100 SK-MEL-28 3.79 >100 >100 >100 SK-MEL-5 3.25 >100 >100 >100 UACC-257 4.20 >100 0.013 0.30 UACC62 1.27 51.0 >100 >100 Ovarian Cancer IGR-OV1 0.66 >100 3.02 >100 OVCAR-3 2.05 >100 >100 30.1 OVCAR-4 4.13 >100 2.49 >100 OVCAR-5 5.51 >100 >100 >100 OVCAR-8 3.75 >100 0.019 >100 NCI/ADR-RES >100 >100 >100 >100 SK-OV-3 0.86 79.8 >100 >100 Renal Cancer 786-0 2.36 >100 37.4 >100 A498 0.55 >100 31.5 >100 ACHN 2.08 >100 >100 >100 CAKI-1 2.74 >100 >100 >100 RXF 393 0.58 >100 1.62 >100 SN12C 2.80 >100 >100 >100 TK-10 3.87 >100 5.64 >100 UO-31 2.70 >100 >100 >100 Prostate Cancer PC-3 2.44 >100 23.6 >100 DU-145 na na 5.24 >100 Breast Cancer MCF7 3.55 >100 >100 >100 MDA-MB-231/ATCC 3.32 >100 6.45 >100 HS 578T 0.97 >100 3.67 >100 BT-549 1.24 >100 98.8 >100 T-47D 1.50 >100 >100 >100 MDA-MB-468 4.14 >100 >100 >100 Open in a separate window NA: Not analyzed a GI 50 : 50% Growth inhibition, concentration of drug resulting in a 50% reduction in net protein increase compared with control cells. b LC 50 : Lethal concentration, concentration of drug lethal to 50% of cells.

Techniques: Activity Assay