Cathearanthus alkaloid
A technology of periwinkle and alkaloids, which can be applied in drug combinations, compounds of group 5/15 elements of the periodic table, organic chemistry, etc., can solve the problems of high neurotoxic side effects and low anti-tumor activity, and achieve good anti-tumor activity , low neurotoxicity
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Embodiment 1
[0024] Obtaining of Compound A1
[0025] 6'-N oxidation-epoxy vinblastine (6'-N b -oxide-leurosine) at the 3-position for semi-synthetic modification, the original -COOCH at the 3-position 3 Replace with -COOCH 2 C 6 h 5 , whose structure is:
[0026]
[0027] Semi-lethal dose (IC 50 ) Experimental results:
[0028] IC 50 Value (μM / L)
[0029] cancer cell line
He La
7.3
16
A549
2.9
3.6
DLD-1
10.7
14
MX-1
1.6
1.8
OVCAR-3
1.5
2.0
[0030] Mouse animal experiment results (the number of mice with abnormal conditions):
[0031]
[0032] Activity experiments showed that the semi-lethal dose (IC 50 ) values are all less than vinblastine, indicating that it has better antitumor activity than vinblastine; meanwhile, the mouse animal experiment results show that the number of mice with abnormal conditions is significantly lowe...
Embodiment 2
[0034] Obtaining of compound B1
[0035] 6'-N oxidation-epoxy vinblastine (6'-N b -oxide-leurosine) at the 3-position for semi-synthetic modification, the original -COOCH at the 3-position 3 Replace with -COOCH 2 C 6 h 5 , while the original -OCOCH at the 4-position 3 Substituted by -OH, its structure is:
[0036]
[0037] Semi-lethal dose (IC 50 ) Experimental results:
[0038] IC 50 Value (μM / L)
[0039] cancer cell line
Compound B1
He La
8.3
16
A549
3.0
3.6
DLD-1
11.6
14
MX-1
1.6
1.8
OVCAR-3
1.8
2.0
[0040] Mouse animal experiment results (the number of mice with abnormal conditions):
[0041]
[0042] Activity experiments showed that the semi-lethal dose (IC 50 ) values are all less than vinblastine, indicating that it has better anti-tumor activity than vinblastine; meanwhile, the mouse animal experiment results show that t...
Embodiment 3
[0044] Obtaining of compound A2
[0045] 6'-N oxidation-epoxy vinblastine (6'-N b -oxide-leurosine) at the 3-position for semi-synthetic modification, the original -COOCH at the 3-position 3 Replaced with -COOC 6 h 5 , whose structure is:
[0046]
[0047] Semi-lethal dose (IC 50 ) Experimental results:
[0048] IC 50 Value (μM / L)
[0049] cancer cell line
He La
14.6
16
A549
3.5
3.6
DLD-1
12.8
14
MX-1
1.8
1.8
OVCAR-3
1.8
2.0
[0050] Mouse animal experiment results (the number of mice with abnormal conditions):
[0051]
[0052]
[0053] Activity experiments showed that the semi-lethal dose (IC 50 ) and slightly vinblastine, indicating that its anti-tumor activity is equivalent to that of vinblastine; meanwhile, the mouse animal experiment results show that the amount of abnormal situation mice is not significantly d...
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