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Structure Activity Studies on the Crinane Alkaloid Apoptosis-inducing Pharmacophore
被引:0
|作者:
McNulty, James
[1
]
Nair, Jerald J.
[1
]
Bastida, Jaume
[2
]
Pandey, Siyaram
[3
]
Griffin, Carly
[3
]
机构:
[1] McMaster Univ, Dept Chem, Hamilton, ON L8S 4M1, Canada
[2] Univ Barcelona, Fac Farm, Dept Nat Prod, E-08028 Barcelona, Spain
[3] Univ Windsor, Dept Chem & Biochem, Windsor, ON N9B 3P4, Canada
基金:
加拿大自然科学与工程研究理事会;
关键词:
Alkaloid;
Amaryllidaceae;
Crinane;
Apoptosis;
Cytotoxicity;
SOUTH-AFRICAN AMARYLLIDACEAE;
PANCRATISTATIN;
HYMENOCALLIS;
REFINEMENT;
INHIBITORS;
PLANTS;
BULBS;
CELLS;
D O I:
暂无
中图分类号:
R914 [药物化学];
学科分类号:
100701 ;
摘要:
The apoptosis-inducing ability of alpha-ethano bridged crinane alkaloids was investigated using natural and semi-synthetic derivatives uncovering novel structural requirements of this cytotoxic pharmacophore. An alpha-ethano bridge is required; an alpha- or beta-methoxy or hydroxyl H-bond acceptor are all tolerated at C-3; a small substituent (H, or OH) alone is tolerated at C-11; and a C-1 to C-2 double bond is shown to modulate, but is not a requirement for, apoptosis-inducing activity.
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页码:483 / 488
页数:6
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