Synthesis and biological evaluation of noscapine analogues as microtubule-interfering agents

Hou Ling Dai; Jian Bin Zheng; Min Lin; Jing Zheng; Fu Sheng Zhou; Xiao Chun Dong; Lei Guo; Jian Wen Liu; Ren Wen

Synthesis and biological evaluation of noscapine analogues as microtubule-interfering agents

Hou Ling Dai, Jian Bin Zheng^*, Min Lin, Jing Zheng, Fu Sheng Zhou, Xiao Chun Dong, Lei Guo, Jian Wen Liu, Ren Wen

^*Corresponding author for this work

Neurology

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

4 Scopus citations

Abstract

A series of noscapine analogues have been synthesized via 13-step reaction starting from 2-hydroxy-3-methoxybenzaldehyde. Anti-tumor activities of these compounds were evaluated against HL-60 cell lines in vitro by the standard MTT assay. It was found that most of these derivatives showed appreciable inhibitory activity against HL-60 and tubulin polymerization. The results also indicated that the potency of compound 31 is about three times more than that of noscapine against HL-60 cell line and tubulin polymerization. Moreover, it induced a massive accumulation of cells in G₂/M phase. These results showed noscapine and its derivatives were worth to be intensively studied further.

Original language	English (US)
Pages (from-to)	1347-1357
Number of pages	11
Journal	Yaoxue Xuebao
Volume	47
Issue number	10
State	Published - Oct 12 2012

Keywords

Cytotoxic activity
Microtubule-interfering agent
Noscapine
Tubulin

ASJC Scopus subject areas

Molecular Medicine
Pharmacology, Toxicology and Pharmaceutics(all)

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title = "Synthesis and biological evaluation of noscapine analogues as microtubule-interfering agents",

abstract = "A series of noscapine analogues have been synthesized via 13-step reaction starting from 2-hydroxy-3-methoxybenzaldehyde. Anti-tumor activities of these compounds were evaluated against HL-60 cell lines in vitro by the standard MTT assay. It was found that most of these derivatives showed appreciable inhibitory activity against HL-60 and tubulin polymerization. The results also indicated that the potency of compound 31 is about three times more than that of noscapine against HL-60 cell line and tubulin polymerization. Moreover, it induced a massive accumulation of cells in G2/M phase. These results showed noscapine and its derivatives were worth to be intensively studied further.",

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author = "Dai, {Hou Ling} and Zheng, {Jian Bin} and Min Lin and Jing Zheng and Zhou, {Fu Sheng} and Dong, {Xiao Chun} and Lei Guo and Liu, {Jian Wen} and Ren Wen",

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TY - JOUR

T1 - Synthesis and biological evaluation of noscapine analogues as microtubule-interfering agents

AU - Dai, Hou Ling

AU - Zheng, Jian Bin

AU - Lin, Min

AU - Zheng, Jing

AU - Zhou, Fu Sheng

AU - Dong, Xiao Chun

AU - Guo, Lei

AU - Liu, Jian Wen

AU - Wen, Ren

PY - 2012/10/12

Y1 - 2012/10/12

N2 - A series of noscapine analogues have been synthesized via 13-step reaction starting from 2-hydroxy-3-methoxybenzaldehyde. Anti-tumor activities of these compounds were evaluated against HL-60 cell lines in vitro by the standard MTT assay. It was found that most of these derivatives showed appreciable inhibitory activity against HL-60 and tubulin polymerization. The results also indicated that the potency of compound 31 is about three times more than that of noscapine against HL-60 cell line and tubulin polymerization. Moreover, it induced a massive accumulation of cells in G2/M phase. These results showed noscapine and its derivatives were worth to be intensively studied further.

AB - A series of noscapine analogues have been synthesized via 13-step reaction starting from 2-hydroxy-3-methoxybenzaldehyde. Anti-tumor activities of these compounds were evaluated against HL-60 cell lines in vitro by the standard MTT assay. It was found that most of these derivatives showed appreciable inhibitory activity against HL-60 and tubulin polymerization. The results also indicated that the potency of compound 31 is about three times more than that of noscapine against HL-60 cell line and tubulin polymerization. Moreover, it induced a massive accumulation of cells in G2/M phase. These results showed noscapine and its derivatives were worth to be intensively studied further.

KW - Cytotoxic activity

KW - Microtubule-interfering agent

KW - Noscapine

KW - Tubulin

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JO - Yao xue xue bao = Acta pharmaceutica Sinica

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SN - 0513-4870

IS - 10

ER -

Synthesis and biological evaluation of noscapine analogues as microtubule-interfering agents

Abstract

Keywords

ASJC Scopus subject areas

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