Synthesis, topoisomerase I inhibition and antitumor cytotoxicity of 2,2′:6′,2″-, 2,2′:6′,3″- and 2,2′:6′,4″-terpyridine derivatives

Long Xuan Zhao; Tae Sung Kim; Soo Hyun Ahn; Tae Hyung Kim; Eun kyung Kim; Won Jea Cho; Heesung Choi; Chong Soon Lee; Jung Ae Kim; Tae Cheon Jeong; Ching jer Chang; Eung Seok Lee

doi:10.1016/S0960-894X(01)00531-5

Synthesis, topoisomerase I inhibition and antitumor cytotoxicity of 2,2′:6′,2″-, 2,2′:6′,3″- and 2,2′:6′,4″-terpyridine derivatives

Long Xuan Zhao, Tae Sung Kim, Soo Hyun Ahn, Tae Hyung Kim, Eun kyung Kim, Won Jea Cho, Heesung Choi, Chong Soon Lee, Jung Ae Kim, Tae Cheon Jeong, Ching jer Chang, Eung Seok Lee

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

99 Citations (Scopus)

Abstract

For the development of new anticancer agents, 2,2′:6′,2″-, 2,2′:6′,3″- and 2,2′:6′,4″-terpyridine derivatives were designed and evaluated for their topoisomerase I inhibitory activity and antitumor cytotoxicity. Structure-activity relationship studies indicated that 2,2′:6′,2″-terpyridine derivatives were highly cytotoxic toward several human tumor cell lines, whereas 2,2′:6′,3″- and 2,2′:6′,4″-terpyridine derivatives were potent topoisomerase I inhibitors.

Original language	English
Pages (from-to)	2659-2662
Number of pages	4
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	11
Issue number	19
DOIs	https://doi.org/10.1016/S0960-894X(01)00531-5
Publication status	Published - 2001 Oct 8
Externally published	Yes

ASJC Scopus subject areas

Biochemistry
Molecular Medicine
Molecular Biology
Pharmaceutical Science
Drug Discovery
Clinical Biochemistry
Organic Chemistry

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10.1016/S0960-894X(01)00531-5

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Zhao, L. X., Kim, T. S., Ahn, S. H., Kim, T. H., Kim, E. K., Cho, W. J., Choi, H., Lee, C. S., Kim, J. A., Jeong, T. C., Chang, C. J., & Lee, E. S. (2001). Synthesis, topoisomerase I inhibition and antitumor cytotoxicity of 2,2′:6′,2″-, 2,2′:6′,3″- and 2,2′:6′,4″-terpyridine derivatives. Bioorganic and Medicinal Chemistry Letters, 11(19), 2659-2662. https://doi.org/10.1016/S0960-894X(01)00531-5

Synthesis, topoisomerase I inhibition and antitumor cytotoxicity of 2,2′:6′,2″-, 2,2′:6′,3″- and 2,2′:6′,4″-terpyridine derivatives. / Zhao, Long Xuan; Kim, Tae Sung; Ahn, Soo Hyun; Kim, Tae Hyung; Kim, Eun kyung; Cho, Won Jea; Choi, Heesung; Lee, Chong Soon; Kim, Jung Ae; Jeong, Tae Cheon; Chang, Ching jer; Lee, Eung Seok.

In: Bioorganic and Medicinal Chemistry Letters, Vol. 11, No. 19, 08.10.2001, p. 2659-2662.

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

Zhao, LX, Kim, TS, Ahn, SH, Kim, TH, Kim, EK, Cho, WJ, Choi, H, Lee, CS, Kim, JA, Jeong, TC, Chang, CJ & Lee, ES 2001, 'Synthesis, topoisomerase I inhibition and antitumor cytotoxicity of 2,2′:6′,2″-, 2,2′:6′,3″- and 2,2′:6′,4″-terpyridine derivatives', Bioorganic and Medicinal Chemistry Letters, vol. 11, no. 19, pp. 2659-2662. https://doi.org/10.1016/S0960-894X(01)00531-5

Zhao, Long Xuan ; Kim, Tae Sung ; Ahn, Soo Hyun ; Kim, Tae Hyung ; Kim, Eun kyung ; Cho, Won Jea ; Choi, Heesung ; Lee, Chong Soon ; Kim, Jung Ae ; Jeong, Tae Cheon ; Chang, Ching jer ; Lee, Eung Seok. / Synthesis, topoisomerase I inhibition and antitumor cytotoxicity of 2,2′:6′,2″-, 2,2′:6′,3″- and 2,2′:6′,4″-terpyridine derivatives. In: Bioorganic and Medicinal Chemistry Letters. 2001 ; Vol. 11, No. 19. pp. 2659-2662.

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title = "Synthesis, topoisomerase I inhibition and antitumor cytotoxicity of 2,2′:6′,2″-, 2,2′:6′,3″- and 2,2′:6′,4″-terpyridine derivatives",

abstract = "For the development of new anticancer agents, 2,2′:6′,2″-, 2,2′:6′,3″- and 2,2′:6′,4″-terpyridine derivatives were designed and evaluated for their topoisomerase I inhibitory activity and antitumor cytotoxicity. Structure-activity relationship studies indicated that 2,2′:6′,2″-terpyridine derivatives were highly cytotoxic toward several human tumor cell lines, whereas 2,2′:6′,3″- and 2,2′:6′,4″-terpyridine derivatives were potent topoisomerase I inhibitors.",

author = "Zhao, {Long Xuan} and Kim, {Tae Sung} and Ahn, {Soo Hyun} and Kim, {Tae Hyung} and Kim, {Eun kyung} and Cho, {Won Jea} and Heesung Choi and Lee, {Chong Soon} and Kim, {Jung Ae} and Jeong, {Tae Cheon} and Chang, {Ching jer} and Lee, {Eung Seok}",

note = "Funding Information: This work was supported by a grant (HMP-00-B-21500-0110) from the Ministry of Health and Welfare, R.O.K. ",

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doi = "10.1016/S0960-894X(01)00531-5",

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AU - Zhao, Long Xuan

AU - Kim, Tae Sung

AU - Ahn, Soo Hyun

AU - Kim, Tae Hyung

AU - Kim, Eun kyung

AU - Cho, Won Jea

AU - Choi, Heesung

AU - Lee, Chong Soon

AU - Kim, Jung Ae

AU - Jeong, Tae Cheon

AU - Chang, Ching jer

AU - Lee, Eung Seok

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PY - 2001/10/8

Y1 - 2001/10/8

N2 - For the development of new anticancer agents, 2,2′:6′,2″-, 2,2′:6′,3″- and 2,2′:6′,4″-terpyridine derivatives were designed and evaluated for their topoisomerase I inhibitory activity and antitumor cytotoxicity. Structure-activity relationship studies indicated that 2,2′:6′,2″-terpyridine derivatives were highly cytotoxic toward several human tumor cell lines, whereas 2,2′:6′,3″- and 2,2′:6′,4″-terpyridine derivatives were potent topoisomerase I inhibitors.

AB - For the development of new anticancer agents, 2,2′:6′,2″-, 2,2′:6′,3″- and 2,2′:6′,4″-terpyridine derivatives were designed and evaluated for their topoisomerase I inhibitory activity and antitumor cytotoxicity. Structure-activity relationship studies indicated that 2,2′:6′,2″-terpyridine derivatives were highly cytotoxic toward several human tumor cell lines, whereas 2,2′:6′,3″- and 2,2′:6′,4″-terpyridine derivatives were potent topoisomerase I inhibitors.

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Synthesis, topoisomerase I inhibition and antitumor cytotoxicity of 2,2′:6′,2″-, 2,2′:6′,3″- and 2,2′:6′,4″-terpyridine derivatives

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