Fluorocyclopentenyl-cytosine with broad spectrum and potent antitumor activity.
Choi WJ, Chung HJ, Chandra G, Alexander V, Zhao LX, Lee HW, Nayak A, Majik MS, Kim HO, Kim JH, Lee YB, Ahn CH, Lee SK, Jeong LS.
On the basis of the potent biological activity of cyclopentenyl-pyrimidines, fluorocyclopentenyl-pyrimidines were designed and synthesized from D-ribose. Among these, the cytosine derivative 5a showed highly potent antigrowth effects in a broad range of tumor cell lines and very potent antitumor activity in a nude mouse tumor xenograft model implanted with A549 human lung cancer cells. However, its 2'-deoxycytidine derivative 5b did not show any antigrowth effects, indicating that 2'-hydroxyl group is essential for the biological activity.