Synthesis and anti-tumor activity of novel combretastatins: Combretocyclopentenones and related analogues

Nguyen Hai Nam; Yong Kim; Young Jae You; Dong Ho Hong; Hwan Mook Kim; Byung Zun Ahn

doi:10.1016/S0960-894X(02)00321-9

Synthesis and anti-tumor activity of novel combretastatins: Combretocyclopentenones and related analogues

Nguyen Hai Nam
, Yong Kim
, Young Jae You
, Dong Ho Hong
, Hwan Mook Kim
, Byung Zun Ahn

Pharmaceutical Sciences

Chungnam National University
Korea Research Institute of Bioscience and Biotechnology

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

61 Scopus citations

Abstract

A series of 2-(3,4,5-trimethoxyphenyl)-3-arylcyclopent-2-ene-1-ones (8a-8e) and their related analogues, including pentenone 9a, pentenol 10a, pentene 12a, and furane 15, were synthesized and evaluated for cytotoxicity against murine and human tumor cell lines. Compounds 8a-c, 8e and 9a showed strong cytotoxicity with IC₅₀ values in the range of 8-34 ng/mL. Compound 8e exhibited significant anti-tumor activity in BDF1 mice bearing Lewis lung carcinoma cells with an inhibition ratio of 59%.

Original language	English
Pages (from-to)	1955-1958
Number of pages	4
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	12
Issue number	15
DOIs	https://doi.org/10.1016/S0960-894X(02)00321-9
State	Published - Aug 5 2002

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title = "Synthesis and anti-tumor activity of novel combretastatins: Combretocyclopentenones and related analogues",

abstract = "A series of 2-(3,4,5-trimethoxyphenyl)-3-arylcyclopent-2-ene-1-ones (8a-8e) and their related analogues, including pentenone 9a, pentenol 10a, pentene 12a, and furane 15, were synthesized and evaluated for cytotoxicity against murine and human tumor cell lines. Compounds 8a-c, 8e and 9a showed strong cytotoxicity with IC50 values in the range of 8-34 ng/mL. Compound 8e exhibited significant anti-tumor activity in BDF1 mice bearing Lewis lung carcinoma cells with an inhibition ratio of 59\%.",

author = "Nam, \{Nguyen Hai\} and Yong Kim and You, \{Young Jae\} and Hong, \{Dong Ho\} and Kim, \{Hwan Mook\} and Ahn, \{Byung Zun\}",

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doi = "10.1016/S0960-894X(02)00321-9",

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T1 - Synthesis and anti-tumor activity of novel combretastatins

T2 - Combretocyclopentenones and related analogues

AU - Nam, Nguyen Hai

AU - Kim, Yong

AU - You, Young Jae

AU - Hong, Dong Ho

AU - Kim, Hwan Mook

AU - Ahn, Byung Zun

PY - 2002/8/5

Y1 - 2002/8/5

N2 - A series of 2-(3,4,5-trimethoxyphenyl)-3-arylcyclopent-2-ene-1-ones (8a-8e) and their related analogues, including pentenone 9a, pentenol 10a, pentene 12a, and furane 15, were synthesized and evaluated for cytotoxicity against murine and human tumor cell lines. Compounds 8a-c, 8e and 9a showed strong cytotoxicity with IC50 values in the range of 8-34 ng/mL. Compound 8e exhibited significant anti-tumor activity in BDF1 mice bearing Lewis lung carcinoma cells with an inhibition ratio of 59%.

AB - A series of 2-(3,4,5-trimethoxyphenyl)-3-arylcyclopent-2-ene-1-ones (8a-8e) and their related analogues, including pentenone 9a, pentenol 10a, pentene 12a, and furane 15, were synthesized and evaluated for cytotoxicity against murine and human tumor cell lines. Compounds 8a-c, 8e and 9a showed strong cytotoxicity with IC50 values in the range of 8-34 ng/mL. Compound 8e exhibited significant anti-tumor activity in BDF1 mice bearing Lewis lung carcinoma cells with an inhibition ratio of 59%.

UR - https://www.scopus.com/pages/publications/0037025445

U2 - 10.1016/S0960-894X(02)00321-9

DO - 10.1016/S0960-894X(02)00321-9

M3 - Article

C2 - 12113817

AN - SCOPUS:0037025445

SN - 0960-894X

VL - 12

SP - 1955

EP - 1958

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 15

ER -

Synthesis and anti-tumor activity of novel combretastatins: Combretocyclopentenones and related analogues

Abstract

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