Fluorocyclopentenyl-cytosine with broad spectrum and potent antitumor activity

Won Jun Choi; Hwa Jin Chung; Girish Chandra; Varughese Alexander; Long Xuan Zhao; Hyuk Woo Lee; Akshata Nayak; Mahesh S. Majik; Hea Ok Kim; Jin Hee Kim; Young B. Lee; Chang H. Ahn; Sang Kook Lee; Lak Shin Jeong

doi:10.1021/jm3004009

Fluorocyclopentenyl-cytosine with broad spectrum and potent antitumor activity

Won Jun Choi
, Hwa Jin Chung
, Girish Chandra
, Varughese Alexander
, Long Xuan Zhao
, Hyuk Woo Lee
, Akshata Nayak
, Mahesh S. Majik
, Hea Ok Kim
, Jin Hee Kim
, Young B. Lee
, Chang H. Ahn
, Sang Kook Lee
, Lak Shin Jeong

Department of Pharmacy

Research output: Contribution to journal › Article › peer-review

69 Scopus citations

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.

Original language	English
Pages (from-to)	4521-4525
Number of pages	5
Journal	Journal of Medicinal Chemistry
Volume	55
Issue number	9
DOIs	https://doi.org/10.1021/jm3004009
State	Published - 10 May 2012

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10.1021/jm3004009

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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.",

author = "Choi, \{Won Jun\} and Chung, \{Hwa Jin\} and Girish Chandra and Varughese Alexander and Zhao, \{Long Xuan\} and Lee, \{Hyuk Woo\} and Akshata Nayak and Majik, \{Mahesh S.\} and Kim, \{Hea Ok\} and Kim, \{Jin Hee\} and Lee, \{Young B.\} and Ahn, \{Chang H.\} and Lee, \{Sang Kook\} and Jeong, \{Lak Shin\}",

year = "2012",

month = may,

day = "10",

doi = "10.1021/jm3004009",

language = "English",

volume = "55",

pages = "4521--4525",

journal = "Journal of Medicinal Chemistry",

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TY - JOUR

T1 - Fluorocyclopentenyl-cytosine with broad spectrum and potent antitumor activity

AU - Choi, Won Jun

AU - Chung, Hwa Jin

AU - Chandra, Girish

AU - Alexander, Varughese

AU - Zhao, Long Xuan

AU - Lee, Hyuk Woo

AU - Nayak, Akshata

AU - Majik, Mahesh S.

AU - Kim, Hea Ok

AU - Kim, Jin Hee

AU - Lee, Young B.

AU - Ahn, Chang H.

AU - Lee, Sang Kook

AU - Jeong, Lak Shin

PY - 2012/5/10

Y1 - 2012/5/10

N2 - 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.

AB - 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.

UR - https://www.scopus.com/pages/publications/84861028393

U2 - 10.1021/jm3004009

DO - 10.1021/jm3004009

M3 - Article

C2 - 22524616

AN - SCOPUS:84861028393

SN - 0022-2623

VL - 55

SP - 4521

EP - 4525

JO - Journal of Medicinal Chemistry

JF - Journal of Medicinal Chemistry

IS - 9

ER -

Fluorocyclopentenyl-cytosine with broad spectrum and potent antitumor activity

Abstract

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