The anaphylatoxin C5a is a potent chemotactic factor for neutrophils and other leukocytes, and functions as an important inflammatory mediator. Through a high capacity screening followed by chemical optimization,
2,4-Diaza-4-deox~ypodophyllotoxin 4 and its cis analogue 14 are synthesised stereoselectively from 3,4-methylenedic)xyaniline 5, and show significant activity against vincristine-resistant P-388 leukaemia in vivo.
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