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result sql = Seocalcitol (EB 1089): a vitamin D analogue of anti-cancer potential. Background, design, synthesis, pre-clinical and clinical evaluation.
Seocalcitol (EB 1089): a vitamin D analogue of anti-cancer potential. Background, design, synthesis, pre-clinical and clinical evaluation.
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char = i;code = 105
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char = a;code = 97
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char = s;code = 115
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char = i;code = 105
char = s;code = 115
char = ;code = 32
char = S;code = 83
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char = c;code = 99
char = a;code = 97
char = l;code = 108
char = c;code = 99
char = i;code = 105
char = t;code = 116
char = o;code = 111
char = l;code = 108
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char = E;code = 69
char = B;code = 66
char = ;code = 32
char = 1;code = 49
char = 0;code = 48
char = 8;code = 56
char = 9;code = 57
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char = .;code = 46
char = ;code = 32
char = D;code = 68
char = e;code = 101
char = s;code = 115
char = p;code = 112
char = i;code = 105
char = t;code = 116
char = e;code = 101
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char = b;code = 98
char = e;code = 101
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char = n;code = 110
char = g;code = 103
char = ;code = 32
char = 5;code = 53
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char = 2;code = 50
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char = 0;code = 48
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char = t;code = 116
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char = m;code = 109
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char = s;code = 115
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char = m;code = 109
char = o;code = 111
char = r;code = 114
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char = p;code = 112
char = o;code = 111
char = t;code = 116
char = e;code = 101
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char = t;code = 116
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char = t;code = 116
char = h;code = 104
char = a;code = 97
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char = 1;code = 49
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char = l;code = 108
char = p;code = 112
char = h;code = 104
char = a;code = 97
char = ,;code = 44
char = 2;code = 50
char = 5;code = 53
char = (;code = 40
char = O;code = 79
char = H;code = 72
char = );code = 41
char = 2;code = 50
char = D;code = 68
char = 3;code = 51
char = ;code = 32
char = w;code = 119
char = i;code = 105
char = t;code = 116
char = h;code = 104
char = ;code = 32
char = r;code = 114
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char = s;code = 115
char = p;code = 112
char = e;code = 101
char = c;code = 99
char = t;code = 116
char = ;code = 32
char = t;code = 116
char = o;code = 111
char = ;code = 32
char = r;code = 114
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char = g;code = 103
char = u;code = 117
char = l;code = 108
char = a;code = 97
char = t;code = 116
char = i;code = 105
char = o;code = 111
char = n;code = 110
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char = o;code = 111
char = f;code = 102
char = ;code = 32
char = c;code = 99
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char = l;code = 108
char = l;code = 108
char = ;code = 32
char = g;code = 103
char = r;code = 114
char = o;code = 111
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char = t;code = 116
char = h;code = 104
char = ;code = 32
char = a;code = 97
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char = d;code = 100
char = ;code = 32
char = d;code = 100
char = i;code = 105
char = f;code = 102
char = f;code = 102
char = e;code = 101
char = r;code = 114
char = e;code = 101
char = n;code = 110
char = t;code = 116
char = i;code = 105
char = a;code = 97
char = t;code = 116
char = i;code = 105
char = o;code = 111
char = n;code = 110
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char = i;code = 105
char = n;code = 110
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char = v;code = 118
char = i;code = 105
char = t;code = 116
char = r;code = 114
char = o;code = 111
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char = a;code = 97
char = s;code = 115
char = ;code = 32
char = w;code = 119
char = e;code = 101
char = l;code = 108
char = l;code = 108
char = ;code = 32
char = a;code = 97
char = s;code = 115
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char = i;code = 105
char = n;code = 110
char = ;code = 32
char = v;code = 118
char = i;code = 105
char = v;code = 118
char = o;code = 111
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char = ;code = 32
char = E;code = 69
char = B;code = 66
char = ;code = 32
char = 1;code = 49
char = 0;code = 48
char = 8;code = 56
char = 9;code = 57
char = ;code = 32
char = d;code = 100
char = i;code = 105
char = s;code = 115
char = p;code = 112
char = l;code = 108
char = a;code = 97
char = y;code = 121
char = s;code = 115
char = ;code = 32
char = a;code = 97
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char = r;code = 114
char = e;code = 101
char = d;code = 100
char = u;code = 117
char = c;code = 99
char = e;code = 101
char = d;code = 100
char = ;code = 32
char = c;code = 99
char = a;code = 97
char = l;code = 108
char = c;code = 99
char = a;code = 97
char = e;code = 101
char = m;code = 109
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char = c;code = 99
char = ;code = 32
char = a;code = 97
char = c;code = 99
char = t;code = 116
char = i;code = 105
char = v;code = 118
char = i;code = 105
char = t;code = 116
char = y;code = 121
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char = i;code = 105
char = n;code = 110
char = ;code = 32
char = v;code = 118
char = i;code = 105
char = v;code = 118
char = o;code = 111
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char = c;code = 99
char = o;code = 111
char = m;code = 109
char = p;code = 112
char = a;code = 97
char = r;code = 114
char = e;code = 101
char = d;code = 100
char = ;code = 32
char = t;code = 116
char = o;code = 111
char = ;code = 32
char = t;code = 116
char = h;code = 104
char = a;code = 97
char = t;code = 116
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char = o;code = 111
char = f;code = 102
char = ;code = 32
char = 1;code = 49
char = a;code = 97
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char = p;code = 112
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char = a;code = 97
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char = ;code = 32
char = 2;code = 50
char = 5;code = 53
char = (;code = 40
char = O;code = 79
char = H;code = 72
char = );code = 41
char = 2;code = 50
char = D;code = 68
char = 3;code = 51
char = .;code = 46
char = ;code = 32
char = T;code = 84
char = h;code = 104
char = e;code = 101
char = s;code = 115
char = e;code = 101
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char = c;code = 99
char = h;code = 104
char = a;code = 97
char = r;code = 114
char = a;code = 97
char = c;code = 99
char = t;code = 116
char = e;code = 101
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char = i;code = 105
char = s;code = 115
char = t;code = 116
char = i;code = 105
char = c;code = 99
char = s;code = 115
char = ;code = 32
char = m;code = 109
char = a;code = 97
char = k;code = 107
char = e;code = 101
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char = E;code = 69
char = B;code = 66
char = ;code = 32
char = 1;code = 49
char = 0;code = 48
char = 8;code = 56
char = 9;code = 57
char = ;code = 32
char = a;code = 97
char = ;code = 32
char = p;code = 112
char = o;code = 111
char = t;code = 116
char = e;code = 101
char = n;code = 110
char = t;code = 116
char = i;code = 105
char = a;code = 97
char = l;code = 108
char = l;code = 108
char = y;code = 121
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char = u;code = 117
char = s;code = 115
char = e;code = 101
char = f;code = 102
char = u;code = 117
char = l;code = 108
char = ;code = 32
char = c;code = 99
char = o;code = 111
char = m;code = 109
char = p;code = 112
char = o;code = 111
char = u;code = 117
char = n;code = 110
char = d;code = 100
char = ;code = 32
char = f;code = 102
char = o;code = 111
char = r;code = 114
char = ;code = 32
char = t;code = 116
char = h;code = 104
char = e;code = 101
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char = t;code = 116
char = r;code = 114
char = e;code = 101
char = a;code = 97
char = t;code = 116
char = m;code = 109
char = e;code = 101
char = n;code = 110
char = t;code = 116
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char = o;code = 111
char = f;code = 102
char = ;code = 32
char = c;code = 99
char = a;code = 97
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char = c;code = 99
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char = r;code = 114
char = .;code = 46
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char = R;code = 82
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char = c;code = 99
char = e;code = 101
char = n;code = 110
char = t;code = 116
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char = c;code = 99
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char = c;code = 99
char = a;code = 97
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char = a;code = 97
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char = u;code = 117
char = a;code = 97
char = t;code = 116
char = i;code = 105
char = o;code = 111
char = n;code = 110
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char = o;code = 111
char = f;code = 102
char = ;code = 32
char = E;code = 69
char = B;code = 66
char = ;code = 32
char = 1;code = 49
char = 0;code = 48
char = 8;code = 56
char = 9;code = 57
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char = h;code = 104
char = a;code = 97
char = s;code = 115
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char = f;code = 102
char = o;code = 111
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char = u;code = 117
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char = d;code = 100
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char = o;code = 111
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char = e;code = 101
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char = t;code = 116
char = a;code = 97
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char = i;code = 105
char = s;code = 115
char = h;code = 104
char = i;code = 105
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char = ;code = 32
char = a;code = 97
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char = a;code = 97
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char = i;code = 105
char = m;code = 109
char = u;code = 117
char = m;code = 109
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char = t;code = 116
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char = e;code = 101
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char = a;code = 97
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char = e;code = 101
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char = d;code = 100
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char = s;code = 115
char = e;code = 101
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char = c;code = 99
char = a;code = 97
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char = c;code = 99
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char = p;code = 112
char = a;code = 97
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char = i;code = 105
char = e;code = 101
char = n;code = 110
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char = s;code = 115
char = .;code = 46
char = ;code = 32
char = E;code = 69
char = a;code = 97
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char = l;code = 108
char = y;code = 121
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char = r;code = 114
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char = u;code = 117
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char = t;code = 116
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char = c;code = 99
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char = f;code = 102
char = i;code = 105
char = r;code = 114
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char = w;code = 119
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char = c;code = 99
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char = c;code = 99
char = a;code = 97
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char = a;code = 97
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char = i;code = 105
char = v;code = 118
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char = t;code = 116
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char = b;code = 98
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char = e;code = 101
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char = a;code = 97
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char = m;code = 109
char = a;code = 97
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char = s;code = 115
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char = c;code = 99
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char = b;code = 98
char = e;code = 101
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char = p;code = 112
char = r;code = 114
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char = d;code = 100
char = u;code = 117
char = c;code = 99
char = e;code = 101
char = d;code = 100
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char = i;code = 105
char = n;code = 110
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char = t;code = 116
char = h;code = 104
char = e;code = 101
char = ;code = 32
char = c;code = 99
char = l;code = 108
char = i;code = 105
char = n;code = 110
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char = c;code = 99
char = .;code = 46
char = ;code = 32
char = F;code = 70
char = u;code = 117
char = r;code = 114
char = t;code = 116
char = h;code = 104
char = e;code = 101
char = r;code = 114
char = m;code = 109
char = o;code = 111
char = r;code = 114
char = e;code = 101
char = ,;code = 44
char = ;code = 32
char = E;code = 69
char = B;code = 66
char = ;code = 32
char = 1;code = 49
char = 0;code = 48
char = 8;code = 56
char = 9;code = 57
char = ;code = 32
char = h;code = 104
char = a;code = 97
char = s;code = 115
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char = b;code = 98
char = e;code = 101
char = e;code = 101
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char = s;code = 115
char = h;code = 104
char = o;code = 111
char = w;code = 119
char = n;code = 110
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char = t;code = 116
char = o;code = 111
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char = u;code = 117
char = c;code = 99
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char = e;code = 101
char = g;code = 103
char = r;code = 114
char = e;code = 101
char = s;code = 115
char = s;code = 115
char = i;code = 105
char = o;code = 111
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char = ;code = 32
char = t;code = 116
char = u;code = 117
char = m;code = 109
char = o;code = 111
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char = s;code = 115
char = ,;code = 44
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char = e;code = 101
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char = a;code = 97
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char = e;code = 101
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char = e;code = 101
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char = d;code = 100
char = .;code = 46
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char = e;code = 101
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char = o;code = 111
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char = m;code = 109
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char = n;code = 110
char = t;code = 116
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char = o;code = 111
char = f;code = 102
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char = E;code = 69
char = B;code = 66
char = ;code = 32
char = 1;code = 49
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char = 8;code = 56
char = 9;code = 57
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char = a;code = 97
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char = m;code = 109
char = i;code = 105
char = s;code = 115
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char = .;code = 46
char = ;code = 32
char = H;code = 72
char = o;code = 111
char = w;code = 119
char = e;code = 101
char = v;code = 118
char = e;code = 101
char = r;code = 114
char = ,;code = 44
char = ;code = 32
char = i;code = 105
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char = s;code = 115
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char = f;code = 102
char = i;code = 105
char = n;code = 110
char = a;code = 97
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char = e;code = 101
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char = a;code = 97
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char = a;code = 97
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char = i;code = 105
char = o;code = 111
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char = s;code = 115
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char = a;code = 97
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char = a;code = 97
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char = t;code = 116
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char = t;code = 116
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char = e;code = 101
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char = c;code = 99
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char = m;code = 109
char = p;code = 112
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char = t;code = 116
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char = o;code = 111
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char = f;code = 102
char = ;code = 32
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char = r;code = 114
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char = l;code = 108
char = e;code = 101
char = d;code = 100
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char = i;code = 105
char = c;code = 99
char = a;code = 97
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char = ;code = 32
char = t;code = 116
char = r;code = 114
char = i;code = 105
char = a;code = 97
char = l;code = 108
char = s;code = 115
char = .;code = 46
char = <;code = 60
char = b;code = 98
char = r;code = 114
char = /;code = 47
char = >;code = 62
result sql = It is well established that the metabolically active form of vitamin D, 1alpha,25-dihydroxyvitamin D3 (1alpha,25(OH)2D3) plays a key role in the establishment and maintenance of the calcium metabolism in the body. In addition to this classic effect of 1alpha,25(OH)2D3, substantial evidence has emerged demonstrating that 1alpha,25(OH)2D3 is able to regulate cell growth and differentiation in a number of different cell types, including cancer cells. However, the clinical usefulness of 1alpha,25(OH)2D3 is limited by its tendency to cause hypercalcaemia. Much effort has therefore been directed to identifying new vitamin D analogues with potent cell regulatory effects, but with weaker effects on the calcium metabolism than those of 1alpha,25(OH)2D3. One of these new synthetic analogues is Seocalcitol (EB 1089). Despite being 50-200 times more potent than 1alpha,25(OH)2D3 with respect to regulation of cell growth and differentiation in vitro as well as in vivo, EB 1089 displays a reduced calcaemic activity in vivo compared to that of 1alpha, 25(OH)2D3. These characteristics make EB 1089 a potentially useful compound for the treatment of cancer. Recent clinical evaluation of EB 1089 has focused mainly on establishing a maximum tolerated dose in cancer patients. Early results confirm that the low calcaemic activity observed in animals can be reproduced in the clinic. Furthermore, EB 1089 has been shown to induce regression of tumours, especially in hepatocellular carcinoma where complete remission has been obtained. In conclusion, the development of EB 1089 as an anti-cancer drug holds promise. However, its final evaluation must await the completion of ongoing controlled clinical trials.

Publication: Curr. Pharm. Des. 2000 May ;6(7)::803-28.
Publication Date: 2000 May
Study Author(s): Hansen, C M;Hamberg, K J;Binderup, E;Binderup, L;
Institution: Department of Chemistry, Leo Pharmaceutical Products, 55, Industriparken, Ballerup, DK-2750, Denmark. [email protected]
Shortcut link to this study:
It is well established that the metabolically active form of vitamin D, 1alpha,25-dihydroxyvitamin D3 (1alpha,25(OH)2D3) plays a key role in the establishment and maintenance of the calcium metabolism in the body. In addition to this classic effect of 1alpha,25(OH)2D3, substantial evidence has emerged demonstrating that 1alpha,25(OH)2D3 is able to regulate cell growth and differentiation in a number of different cell types, including cancer cells. However, the clinical usefulness of 1alpha,25(OH)2D3 is limited by its tendency to cause hypercalcaemia. Much effort has therefore been directed to identifying new vitamin D analogues with potent cell regulatory effects, but with weaker effects on the calcium metabolism than those of 1alpha,25(OH)2D3. One of these new synthetic analogues is Seocalcitol (EB 1089). Despite being 50-200 times more potent than 1alpha,25(OH)2D3 with respect to regulation of cell growth and differentiation in vitro as well as in vivo, EB 1089 displays a reduced calcaemic activity in vivo compared to that of 1alpha, 25(OH)2D3. These characteristics make EB 1089 a potentially useful compound for the treatment of cancer. Recent clinical evaluation of EB 1089 has focused mainly on establishing a maximum tolerated dose in cancer patients. Early results confirm that the low calcaemic activity observed in animals can be reproduced in the clinic. Furthermore, EB 1089 has been shown to induce regression of tumours, especially in hepatocellular carcinoma where complete remission has been obtained. In conclusion, the development of EB 1089 as an anti-cancer drug holds promise. However, its final evaluation must await the completion of ongoing controlled clinical trials.
PMID: 10828309

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