title: Fluorocyclopentenyl-cytosine with broad spectrum and potent antitumor activity.
abstract: 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.
authors.affiliation: Department of Bioinspired Science and College of Pharmacy, Ewha Womans University, Seoul 120-750, Korea.
authors.forename: Won Jun
authors.initials: WJ
authors.lastname: Choi
authors.forename: Hwa-Jin
authors.initials: HJ
authors.lastname: Chung
authors.forename: Girish
authors.initials: G
authors.lastname: Chandra
authors.forename: Varughese
authors.initials: V
authors.lastname: Alexander
authors.forename: Long Xuan
authors.initials: LX
authors.lastname: Zhao
authors.forename: Hyuk Woo
authors.initials: HW
authors.lastname: Lee
authors.forename: Akshata
authors.initials: A
authors.lastname: Nayak
authors.forename: Mahesh S
authors.initials: MS
authors.lastname: Majik
authors.forename: Hea Ok
authors.initials: HO
authors.lastname: Kim
authors.forename: Jin-Hee
authors.initials: JH
authors.lastname: Kim
authors.forename: Young B
authors.initials: YB
authors.lastname: Lee
authors.forename: Chang H
authors.initials: CH
authors.lastname: Ahn
authors.forename: Sang Kook
authors.initials: SK
authors.lastname: Lee
authors.forename: Lak Shin
authors.initials: LS
authors.lastname: Jeong
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D003517:Cyclopentanes / Q000138:chemical synthesis* / Q000494:pharmacology; D003596:Cytosine / Q000031:analogs & derivatives* / Q000494:pharmacology; D006801:Humans; D008175:Lung Neoplasms / Q000188:drug therapy* / Q000473:pathology; D008297:Male; D051379:Mice; D008819:Mice, Nude; D023041:Xenograft Model Antitumor Assays
chemical_list: D000970:Antineoplastic Agents; D003517:Cyclopentanes; D003596:Cytosine