Table 5.
Antiproliferative Activities of Dihydropyridopyrazoles 78–110
Compd | ![]() |
% cell viability | % apoptosis Jurkat | ||||
---|---|---|---|---|---|---|---|
HeLa | MCF-7/AZ | Jurkat | |||||
R1 | R2 | R | |||||
1 | 19 ± 5 | 55 ± 3 | 18 ± 5 | 54 ± 2 | |||
2 | 91 ± 2 | 76 ± 2 | 75 ± 5 | 4 ± 3 | |||
76a | 53 ± 5 | 58 ± 4 | 35 ± 6 | 49 ± 4 | |||
76c | 54 ± 6 | 52 ± 3 | 54 ± 1 | 55 ± 4 | |||
78 | Ph | 4-Br-Ph | 3,4,5-tri-OMe-Ph | 73 ± 5 | 90 ± 3 | 99 ± 1 | 2 ± 1 |
79 | 4-Me-Ph | Me | 3,4,5-tri-OMe-Ph | 77 ± 4 | 71 ± 5 | 77 ± 2 | 23 ± 1 |
80 | H | 4-Br-Ph | 3,4,5-tri-OMe-Ph | 67 ± 4 | 98 ± 3 | 78 ± 7 | 5 ± 1 |
81 | iPr | Me | 3,4,5-tri-OMe-Ph | 83 ± 5 | 99 ± 0 | 77 ± 9 | 4 ± 0 |
82 | Me | Me | 3,4,5-tri-OMe-Ph | 55 ± 3 | 98 ± 1 | 79 ± 4 | 5 ± 1 |
83 | H | Me | 3,4,5-tri-OMe-Ph | 50 ± 2 | 58 ± 5 | 47 ± 3 | 55 ± 4 |
84 | H | Me | 3,4-di-OMe-Ph | 73 ± 3 | 95 ± 4 | 88 ± 2 | 5 ± 1 |
85 | H | Me | 4-OMe-Ph | 73 ± 7 | 82 ± 3 | 94 ± 4 | 11 ± 1 |
86 | H | Me | 4-OCF3-Ph | 97 ± 2 | 84 ± 3 | 97 ± 6 | 9 ± 2 |
87 | H | Me | 4-SMe-Ph | 45 ± 2 | 95 ± 4 | 87 ± 4 | 14 ± 6 |
88 | H | Me | Ph | 74 ± 4 | 84 ± 3 | 87 ± 5 | 10 ± 2 |
89 | H | Me | 2-NO2-Ph | 71 ± 4 | 99 ± 2 | 64 ± 1 | 6 ± 1 |
90 | H | Me | 4-OH-3-OMe-5-NO2-Ph | 78 ± 3 | 89 ± 5 | 90 ± 2 | 2 ± 1 |
91 | H | Me | 3-Br-Ph | 51 ± 3 | 63 ± 4 | 68 ± 3 | 58 ± 2 |
92 | H | Me | 3,5-di-Br-4-OH-Ph | 58 ± 7 | 60 ± 4 | 58 ± 3 | 53 ± 0 |
93 | H | Me | 3-Br-4-OEt-5-OMe-Ph | 52 ± 2 | 49 ± 4 | 28 ± 5 | 49 ± 1 |
94 | H | Me | 4-OAc-3-Br-5-OMe-Ph | 47 ± 2 | 46 ± 2 | 36 ± 6 | 58 ± 1 |
95 | H | Me | 3-Br-4-NMe2-Ph | 55 ± 3 | 59 ± 3 | 34 ± 5 | 41 ± 1 |
96 | H | Me | 3-Br-4,5-di-OMe-Ph | 16 ± 3 | 47 ± 1 | 29 ± 3 | 56 ± 1 |
97 | H | Me | 3-Cl-Ph | 43 ± 4 | 54 ± 3 | 76 ± 4 | 28 ± 4 |
98 | H | Me | 3,4-di-Cl-Ph | 88 ± 1 | 56 ± 3 | 71 ± 4 | 33 ± 4 |
99 | H | Me | 3-F-Ph | 99 ± 1 | 76 ± 2 | 84 ± 2 | 28 ± 1 |
100 | H | Me | 2-Br-Ph | 57 ± 4 | 100 ± 3 | 90 ± 1 | 8 ± 2 |
101 | H | Me | 4-Br-Ph | 62 ± 3 | 92 ± 2 | 90 ± 1 | 10 ± 2 |
102 | H | Me | Me | 70 ± 4 | 97 ± 2 | 78 ± 5 | 5 ± 1 |
103 | H | Me |
![]() |
95 ± 5 | 91 ± 4 | 89 ± 6 | 14 ± 2 |
104 | H | Me |
![]() |
58 ± 2 | 100 ± 1 | 94 ± 2 | 6 ± 1 |
105 | H | Me |
![]() |
82 ± 4 | 98 ± 3 | 74 ± 4 | 18 ± 1 |
106 | H | Me |
![]() |
98 ± 2 | 100 ± 2 | 82 ± 5 | 6 ± 4 |
107 | H | Me |
![]() |
94 ± 1 | 100 ± 1 | 92 ± 5 | 4 ± 2 |
108 | H | Me |
![]() |
69 ± 4 | 96 ± 2 | 88 ± 9 | 11 ± 3 |
109 | H | Me |
![]() |
84 ± 4 | 100 ± 3 | 85 ± 6 | 7 ± 2 |
110 | H | Me |
![]() |
72 ± 6 | 100 ± 4 | 97 ± 3 | 11 ± 2 |