Table 1.
Selectivity Index (SI) and IC50 Values (μM; µg/mL) of in vitro DPPH-radical and RAW264.7 Cell Line NO- radical scavenging properties of the tested compounds of new 3 FQs series vs. respective reference agents
| Treatment | DPPH radical scavenging IC50 value µM (μg/mL)+ | NOS- IC50 value μM (µg/mL)++ |
IC50 PDL Fibro µM (µg/mL) | SI |
|---|---|---|---|---|
| Nitrous FQs series | ||||
| 3a | NI | 121.33±2.02**** | 368.83±23.08**** | 10.35 (K562) |
| (52.1± 0.87) | (158.37±9.91) | |||
| 3b | 4086.1±405.59**** | 351.39± 39.95*** | 153.10±17.13*** | 11.14 (K562) |
| (1754.73±174.18) | (150.9± 17.15) | (65.75±7.36) | ||
| 3c | 71.59±14.22** | 98.74± 9.96** | 407.61±11.38**** | 21.61 (MCF7) |
| (30.74±6.10) | (42.4± 4.28) | (175.03±4.89) | ||
| 3e | 640.82±28.50**** | 71.39± 5.28** | 81.96±9.84*** | 1.24 (A549) |
| (313.45±13.94) | (32.8± 2.4248711) | (37.66±4.52) | ||
| 3d | 440.16±39.85**** | 27.67± 3.37*** | 10.62±1.15*** | 1.83 (T47D) |
| (202.22±18.31) | (13.53± 1.65) | (5.19±0.56) | ||
| 3f | NI | 181.55± 18.05*** | NI | NI |
| (77.97± 7.75) | ||||
| Reduced FQ series | ||||
| 4a | 37.67±3.03*** | 84.21± 9.83** | 51.45±7.11*** | 8.68 (K562) |
| (15.05±1.21) | (33.63± 3.93) | (20.55±2.84) | ||
| 4b | 3.61±0.31NS | 25.54± 2.62*** | 38.05±2.97**** | 3.03 (MCF7) |
| (1.55±0.13) | (10.97± 1.12) | (16.34±1.27) | ||
| 4c | 276.81±28.69**** | 76.78± 5.38** | 95.31±2.55**** | 27.15 (K562) |
| (110.56±11.46) | (30.67± 2.15) | (38.07±1.02) | ||
| 4d | 251.32±28.81*** | 63.49± 6.08ns | 95.29±12.28*** | 10.19 (K562) |
| (107.93±12.37) | (27.27± 2.61) | (40.92±5.27) | ||
| 4e | 229.45±19.08**** | 17.63± 3.07**** | 7.52±0.14**** | 0.36 (K562) |
| (105.42±8.77) | (8.1± 1.41) | (52.49±3.45) | ||
| 4f | 80.17±15.92** | 38.51± 2.90** | 6.07±1.14** | 0.36 (MCF7) |
| (30.74±6.10) | (14.77± 1.12) | (2.33±0.44) | ||
| TriazoloFQ series | ||||
| 5a | 7891.68±886.16*** | 82.73± 9.94** | 9.31±1.45*** | 0.42 (T47D) |
| (3238.67±363.67) | (33.95± 4.08) | (3.82±0.59) | ||
| 5b | 1716.52±237.77*** | 130.09± 2.81**** | 240.05±11.87**** | 3.40 (K562) |
| (737.14±102.11) | (55.87± 1.21) | (103.09±5.10) | ||
| 5c | 193.48±21.20*** | 46.13± 3.79NS | 350.70±23.26**** | 3.65 (A375.s2) |
| (79.4±8.7) | (18.93± 1.55) | (143.92±9.54) | ||
| 5f | 1743.04±191.73**** | 103.42± 10.19** | 96.75±3.23**** | 8.14 (K562) |
| (609±66.99) | (36.13± 3.55) | (33.80±1.13) | ||
| Reference Drug | Ascorbic 3.37±0.29 | Indomethacin | Cisplatin | 1.01 (A375.s2) |
| (1.55±0.13) | 55.06± 2.25 | 0.71 ± 0.13 | ||
| (26.93± 1.10) | (0.21 ± 0.04) | |||
Results are mean ± SD (n = 3 independent replicates). + IC50 values (concentration at which 50% inhibition of DPPH in comparison to non-induced basal 30 minutes incubations or cell proliferation in comparison to non-induced basal incubations) were calculated within testing dose range. ++ The IC50 value is the concentration at which 50% inhibition of Nitric oxide synthase took place in comparison to non-induced basal 24h incubations. P-value is calculated by unpaired t-test between test compound IC50 values μM and ascorbic acid IC50 values μM (DPPH) or Indomethacin IC50 values μM (NOS) using GraphPad Prism software version 8.0.1 * When P<0.05 and ** when P<0.01 or 0.001, *** when P< 0.001or 0.0001 , **** when P<0.0001, NS: not significantly different from reference agent. Bolded numerals stand out as the least IC50 values (most active) among others enlisted in the same tested cell line. NI, Non-Inhibitory.