Table 2.
Cytotoxicity (as of %Control) IC50 Values in µM (µg/mL) of the Tested Compounds of New 3 FQs Series vs. Cisplatin
| Treatment | A549 | A375.s2 | MCF7 | PANC-1 | PC-3 | K562 | T47D |
|---|---|---|---|---|---|---|---|
| Nitrous FQs series | |||||||
| 3a | 1003.52± 140.23*** | 173.69± 21.29*** | 70.91 2.14* | 1935.38± 211.18**** | 526.55 ±37.51* | 35.63 ±6.12 | 309.67 ±6.19**** |
| (430.9± 60.21) | (74.58± 9.14) | (30.45± 0.92) | (831.03 ±90.68) | (226.10 ±16.11) | (15.30 ±2.63) | (132.97 ±2.66) | |
| 3b | 79.96± 12.26*** | 405.76± 60.03*** | 122.88± 7.80* | 2541.43± 51.14**** | 303.12 ±30.58** | 13.74 ±1.32** | 302.47 ±10.75**** |
| (34.34± 5.26) | (174.25± 25.78) | (52.77± 3.35) | (1091.39± 21.96) | (130.17 ±13.13) | (5.90±0.57) | (129.89 ±4.61) | |
| 3c | 149.15± 22.13*** | 393.83± 10.13**** | 18.86± 2.31*** | NI | 1065.26±140.57** | 588.82 ±32.51**** | 710.82± 90.34** |
| (64.04± 9.50) | (169.11± 4.35) | (8.10 ±0.99) | (457.41± 60.36) | (252.83± 13.96) | (305.22 v3.79) | ||
| 1310.5± 194.14*** | 285.14±38.54** (131.00±17.71) | 182.48± 12.20**** | 148.74 ±8.84**** | 211.64 ±24.11*** | 606.45 ±25.20**** | ||
| 3d | 66.05±9.60*** | (602.07± 89.19) | (83.83 ±5.61) | (68.33 ±4.06) | (97.23 ±11.08) | (278.61 ±11.58) | |
| (30.34±4.41) | |||||||
| 3e | 45.14± 6.64** | 56.25± 6.90*** | 79.87± 10.43 | 99.28± 5.86**** | 49.61± 5.30**** | 54.90 ±1.39* | 5.80 ±0.22**** |
| (22.08± 3.24) | (27.52± 3.37) | (39.07± 5.10) | (48.56 ±2.87) | (24.27± 2.59) | (22.53 ±0.57) | (2.84 ±0.11) | |
| 3f | NI | 1323.73±120.05*** | 162.62± 3.378*** | NI | NI | 38.54 ±0.49* | NI |
| (553.51± 50.20) | (68.00± 1.41) | (16.55 ±0.21) | |||||
| Reduced FQs series | |||||||
| 4a | 83.60± 7.36**** | 151.55± 19.98*** | 62.77± 5.31* | 172.53± 15.0**** | 255.17 ±45.32*** | 8.68 ±1.67** | 327.96± 26.79**** |
| (33.39±2.94) | 60.53 ±7.98 | 25.07± 2.12 | (68.91± 5.99) | 101.92 ±18.10 | 3.47 ±0.67 | (130.99 ±10.70) | |
| 4b | 75.42± 8.78*** | 50.99± 6.26*** | 12.57 ±0.66*** | 308.62 ±38.38*** | 131.79± 17.67**** | 37.96 ±6.47 | 44.04 ±3.41 |
| (32.39± 3.77) | 21.9 ±2.69 | (5.40 ±0.28 ) | (132.54 ±21.05) | (56.60 ±7.59) | (16.30 ±2.78) | (18.91± 1.47) | |
| 4c | 12.29± 2.17 | 75.81± 10.89*** | 16.14± 2.26*** | 30.41± 4.77** | 13.14± 2.55**** | 3.51 ±0.66*** | 6.73 ±1.16*** |
| (4.908± 0.87) | (30.28± 4.35) | (6.45± 0.90) | (12.15± 1.90) | (5.25± 1.02) | (1.40± 0.26) | (2.69 ±0.46) | |
| 4d | 72.43±6.79*** | 373.87± 11.31**** | 348.59± 29.31*** | 2509.19± 44.84**** | 1192.24± 83.72*** | 9.35 ±1.80** | 533.6±40.00**** |
| (31.10±2.92) | (160.55± 4.85) | (149.70± 12.59) | (1077.55± 19.26) | (512.0 ±35.95) | (4.01 ±0.77) | (229.15±17.18) | |
| 4e | 137.40± 16.05** | 90.38 ±12.62*** | 158.67± 7.56** | 159.98 ±21.17*** | 179.30± 21.03**** | 21.13± 1.49*** | 102.07± 16.87*** |
| (63.13± 7.38) | (41.53± 5.79) | (72.90 ±3.47) | (73.51 ±9.73) | (82.38 ±9.66) | (8.67± 0.61) | (46.9 ±7.75) | |
| 4f | 26.37± 5.09* | 109.41± 15.17*** | 16.95 ±2.65*** | 93.42± 2.97**** | 256.13± 12.05**** | 36.95 ±4.54 | 213.74 ±22.46*** |
| (10.11± 1.95) | (41.95± 5.81) | (6.5± 1.01) | (35.82± 1.14) | (98.20 ±4.62) | (14.17 ±1.74) | (81.95 ±8.61) | |
| TriazoloFQs series | |||||||
| 5a | 132.54± 23.17*** | 30.57± 3.08**** | 77.57± 13.77ns | 840.61± 146.74*** | 1525.28±140.75*** | 277.05± 24.93**** | 22.32 ±1.41**** |
| (54.39± 9.51) | (12.54± 1.26) | (31.83 ±6.65) | (344.98± 60.22) | (625.96± 73.50) | (113.70 ±10.23) | (9.16 ±0.58) | |
| 5b | 164.06± 12.29**** | 923.39± 62.70**** | 656.20± 11.86**** | 788.13 ±49.02**** | 494.84 ±40.46 | 70.44 ±11.36** | 142.52± 14.45*** |
| (70.45± 5.28) | (396.54± 26.93) | (281.80 ±5.09) | (338.45 ±21.05) | (212.50 ±17.38) | (30.25 ±4.88 ) | (61.20 ±6.21) | |
| 5c | 125.17± 8.37**** | 96.07± 18.05*** | 431.30 ±58.58*** | 1745.17± 287.74*** | 548.37± 95.89 | 2017.35±27.22**** | 133.92± 4.05** |
| (51.37± 3.43) | (39.42± 7.40) | (177.0 ±24.04) | (716.2 ±118.09) | (225.05± 39.35) | (827.90 ±11.17) | (54.96 ±1.66) | |
| 5f | 138.88± 16.86*** | 86.66± 12.45*** | 131.9 ±19.52* | 519.06 5.94**** | 490.65 ±55.33 | 11.88 ±0.61** | 527.59 ±13.35*** |
| (48.53± 5.89) | (30.28± 4.35) | (46.08 ±6.82) | (181.35±2.08) | (171.43± 19.33) | (4.15 ±0.21) | (184.33 ±4.66) | |
| 12.27 ± 2.05 | 0.7 ± 0.1 | 92.58±12.54 | 7.01 ± 1.17 | 454.37±10.65 | 29.3 ± 5 | 45.15 ± 7.84 | |
| (3.68 ± 0.62) | (0.22 ± 0.03) | (42.54 5.76) | (2.10 ± 0.35) | 208.77±4.89 | (8.8 ± 1.5) | (13.55 ± 2.35) | |
Results are mean ± SD (n = 3-4 independent replicates). IC50 values (concentration at which 50% inhibition of cell proliferation took place in comparison to non-induced basal 72 h incubations) were calculated within 0.1-200 μg/mL range. NI is a lack of cytotoxicity within the tested 0.1-200 μg/mL concentration range. P-value calculated by unpaired t-test between test compound IC50 values and cisplatin's (μM) using Graph Pad 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.