Antitumor agents 270. Novel substituted 6-phenyl-4H-furo[3,2-c]pyran-4-one derivatives as potent and highly selective anti-breast cancer agents

Yizhou Dong; Qian Shi; Kyoko Nakagawa-Goto; Pei Chi Wu; Susan L. Morris-Natschke; Arnold Brossi; Kenneth F. Bastow; Jing Yu Lang; Mien Chie Hung; Kuo Hsiung Lee

doi:10.1016/j.bmc.2009.11.049

Antitumor agents 270. Novel substituted 6-phenyl-4H-furo[3,2-c]pyran-4-one derivatives as potent and highly selective anti-breast cancer agents

Yizhou Dong
, Qian Shi
, Kyoko Nakagawa-Goto
, Pei Chi Wu
, Susan L. Morris-Natschke
, Arnold Brossi
, Kenneth F. Bastow
, Jing Yu Lang
, Mien Chie Hung
, Kuo Hsiung Lee

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

39 Scopus citations

Abstract

6-Phenyl-4H-furo[3,2-c]pyran-4-one derivatives based on neo-tashinlactone (1) were synthesized and evaluated as novel anti-breast cancer agents. Compounds 10-13, 23, 25, and 27 showed potent inhibition against the SK-BR-3 breast cancer cell line. Importantly, 25 and 27 showed the highest cancer cell line selectivity, being approximately 100-250-fold more potent against SK-BR-3 (ED₅₀ 0.28 and 0.44 μM, respectively) compared with other cancer cell lines tested. In addition, 25 displayed low cytotoxicity against normal breast cell lines 184A1 and MCF10A. Compounds 25 and 27 merit further investigation in our continuing program to generate and develop selective anti-breast cancer agents.

Original language	English
Pages (from-to)	803-808
Number of pages	6
Journal	Bioorganic and Medicinal Chemistry
Volume	18
Issue number	2
DOIs	https://doi.org/10.1016/j.bmc.2009.11.049
State	Published - 15 Jan 2010
Externally published	Yes

Keywords

6-Phenyl-4H-furo[3,2-c]pyran-4-ones
Breast cancer
Neo-tanshinlactone

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10.1016/j.bmc.2009.11.049

Cite this

Dong, Y., Shi, Q., Nakagawa-Goto, K., Wu, P. C., Morris-Natschke, S. L., Brossi, A., Bastow, K. F., Lang, J. Y., Hung, M. C., & Lee, K. H. (2010). Antitumor agents 270. Novel substituted 6-phenyl-4H-furo[3,2-c]pyran-4-one derivatives as potent and highly selective anti-breast cancer agents. Bioorganic and Medicinal Chemistry, 18(2), 803-808. https://doi.org/10.1016/j.bmc.2009.11.049

@article{66b5759d05f14ef6bbff13a4fb0f4e3a,

title = "Antitumor agents 270. Novel substituted 6-phenyl-4H-furo[3,2-c]pyran-4-one derivatives as potent and highly selective anti-breast cancer agents",

abstract = "6-Phenyl-4H-furo[3,2-c]pyran-4-one derivatives based on neo-tashinlactone (1) were synthesized and evaluated as novel anti-breast cancer agents. Compounds 10-13, 23, 25, and 27 showed potent inhibition against the SK-BR-3 breast cancer cell line. Importantly, 25 and 27 showed the highest cancer cell line selectivity, being approximately 100-250-fold more potent against SK-BR-3 (ED50 0.28 and 0.44 μM, respectively) compared with other cancer cell lines tested. In addition, 25 displayed low cytotoxicity against normal breast cell lines 184A1 and MCF10A. Compounds 25 and 27 merit further investigation in our continuing program to generate and develop selective anti-breast cancer agents.",

keywords = "6-Phenyl-4H-furo[3,2-c]pyran-4-ones, Breast cancer, Neo-tanshinlactone",

author = "Yizhou Dong and Qian Shi and Kyoko Nakagawa-Goto and Wu, \{Pei Chi\} and Morris-Natschke, \{Susan L.\} and Arnold Brossi and Bastow, \{Kenneth F.\} and Lang, \{Jing Yu\} and Hung, \{Mien Chie\} and Lee, \{Kuo Hsiung\}",

year = "2010",

month = jan,

day = "15",

doi = "10.1016/j.bmc.2009.11.049",

language = "English",

volume = "18",

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journal = "Bioorganic and Medicinal Chemistry",

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publisher = "Elsevier Ltd.",

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Dong, Y, Shi, Q, Nakagawa-Goto, K, Wu, PC, Morris-Natschke, SL, Brossi, A, Bastow, KF, Lang, JY, Hung, MC & Lee, KH 2010, 'Antitumor agents 270. Novel substituted 6-phenyl-4H-furo[3,2-c]pyran-4-one derivatives as potent and highly selective anti-breast cancer agents', Bioorganic and Medicinal Chemistry, vol. 18, no. 2, pp. 803-808. https://doi.org/10.1016/j.bmc.2009.11.049

TY - JOUR

T1 - Antitumor agents 270. Novel substituted 6-phenyl-4H-furo[3,2-c]pyran-4-one derivatives as potent and highly selective anti-breast cancer agents

AU - Dong, Yizhou

AU - Shi, Qian

AU - Nakagawa-Goto, Kyoko

AU - Wu, Pei Chi

AU - Morris-Natschke, Susan L.

AU - Brossi, Arnold

AU - Bastow, Kenneth F.

AU - Lang, Jing Yu

AU - Hung, Mien Chie

AU - Lee, Kuo Hsiung

PY - 2010/1/15

Y1 - 2010/1/15

N2 - 6-Phenyl-4H-furo[3,2-c]pyran-4-one derivatives based on neo-tashinlactone (1) were synthesized and evaluated as novel anti-breast cancer agents. Compounds 10-13, 23, 25, and 27 showed potent inhibition against the SK-BR-3 breast cancer cell line. Importantly, 25 and 27 showed the highest cancer cell line selectivity, being approximately 100-250-fold more potent against SK-BR-3 (ED50 0.28 and 0.44 μM, respectively) compared with other cancer cell lines tested. In addition, 25 displayed low cytotoxicity against normal breast cell lines 184A1 and MCF10A. Compounds 25 and 27 merit further investigation in our continuing program to generate and develop selective anti-breast cancer agents.

AB - 6-Phenyl-4H-furo[3,2-c]pyran-4-one derivatives based on neo-tashinlactone (1) were synthesized and evaluated as novel anti-breast cancer agents. Compounds 10-13, 23, 25, and 27 showed potent inhibition against the SK-BR-3 breast cancer cell line. Importantly, 25 and 27 showed the highest cancer cell line selectivity, being approximately 100-250-fold more potent against SK-BR-3 (ED50 0.28 and 0.44 μM, respectively) compared with other cancer cell lines tested. In addition, 25 displayed low cytotoxicity against normal breast cell lines 184A1 and MCF10A. Compounds 25 and 27 merit further investigation in our continuing program to generate and develop selective anti-breast cancer agents.

KW - 6-Phenyl-4H-furo[3,2-c]pyran-4-ones

KW - Breast cancer

KW - Neo-tanshinlactone

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ER -

Antitumor agents 270. Novel substituted 6-phenyl-4H-furo[3,2-c]pyran-4-one derivatives as potent and highly selective anti-breast cancer agents

Abstract

Keywords

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