Table 1.
Structures and Activities of Flex-Hets and t-RA in cancer and normal renal cells
| Caki-1 cancer | 786-O cancer | HK-2 normal | RTC91696 normal | |
|---|---|---|---|---|
| SHetC2 | 85.71% ± 4.53% | 78.53% ± 6.11% | 52.67% ± 1.84% | 52.31% ± 7.38% |
| 4.91 ± 0.29 μmol/L | 7.48 ± 0.34 μmol/L | 4.47 ± 0.49 μmol/L | 7.67 ± 0.49 μmol/L | |
| SHetA2 | 84.40% ± 3.86% | 72.00% ± 5.06% | 51.02% ± 7.07% | 36.84% ± 6.80% |
| 4.93 ± 0.22 μmol/L | 7.55 ± 0.38 μmol/L | 4.50 ± 0.28 μmol/L | 4.57 ± 0.49 μmol/L | |
| SHetA4 | 68.92% ± 6.94% | 45.04% ± 4.80% | 26.35% ± 0.80% | 39.67% ± 2.52% |
| 5.07 ± 0.15 μmol/L | 2.56 ± 0.34 μmol/L | 5.19 ± 0.25 μmol/L | 7.55 ± 0.51 μmol/L | |
| SHetA3 | 56.48% ± 14.58% | 54.10% ± 13.66% | 35.34% ± 2.09% | 28.23% ± 3.07% |
| 7.28 ± 0.27 μmol/L | 7.2 ± 0.72 μmol/L | 5.14 ± 0.26 μmol/L | 5.92 ± 1.91 μmol/L | |
| SHetD3 | 56.99% ± 12.12% | 61.52% ± 1.44% | 26.37% ± 0.22% | 46.27% ± 0.95% |
| 7.14 ± 0.22 μmol/L | 7.15 ± 0.81 μmol/L | 6.91 ± 0.66 μmol/L | 9.42 ± 0.43 μmol/L | |
| SHetD4 | 38.67% ± 1.50% | 44.55% ± 17.56% | 43.67% ± 0.44% | 37.74% ± 6.61% |
| 7.56 ± 0.15 μmol/L | 5.08 ± 0.71 μmol/L | 7.42 ± 0.20 μmol/L | 5.36 ± 0.60 μmol/L | |
| SHetD5 | 34.10% ± 1.20% | 41.80% ± 16.91% | 47.97% ± 1.00% | ND |
| 7.22 ± 0.25 μmol/L | 5.14 ± 0.70 μmol/L | 4.96 ± 0.25 μmol/L | ||
| t-RA | 6.46% ± 9.40% | 0.00% ± 1.43% | 15.81% ± 0.47% | ND |
| 4.64 ± 1.14 μmol/L | 23.60 ± 0.0 μmol/L | 6.28 ± 2.19 μmol/L |
NOTE: The top value represents the efficacy (maximum growth inhibition observed) and the bottom value represents the potency (EC50, concentration needed to induce half maximal efficacy). The hydrophilicity of the compounds is increased by the end group with NO2 being the least hydrophobic, CO2Et intermediate, and CO2CH3 being the most hydrophilic.
Abbreviations: ND, not determined; t-RA, trans-retinoic acid.