The invention discloses a
cytarabine analogue and a preparation method and application thereof. The
cytarabine structural analogues P1-P4 are synthesized for the first time and can inhibit proliferation of
leukemia cells HL60, and particularly, compared with Ara-C, the
cytarabine structural analogues P4 are higher in
leukemia cell proliferation inhibition capacity and
cell penetration capacity, the concentration of the
drug entering the cells and the concentration of the
active metabolite cytarabine triphosphate generated in the cells are higher, and the
bioavailability is higher; the cytosinearabinoside can be converted into a parent
drug cytosine arabinoside in cells, so that the
blood concentration of target cells
in vivo is remarkably improved, and toxic and side effects and
drug resistance caused by large-
dose medication can be avoided; and the half-life period of cytarabine is remarkably prolonged, the effective
blood concentration is maintained for a long time,
oral administration can be achieved, and inconvenience caused by injection medication can be avoided. The preparation method is simple, easy to operate and suitable for industrial production.