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)

Cite this

@article{d7a3b27f2e4345b19f4554e3642f5c4b,

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.",

keywords = "Cytotoxic activity, Microtubule-interfering agent, Noscapine, Tubulin",

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",

year = "2012",

month = oct,

day = "12",

language = "English (US)",

volume = "47",

pages = "1347--1357",

journal = "Yao xue xue bao = Acta pharmaceutica Sinica",

issn = "0513-4870",

publisher = "Zhonghua Yixuehui Zazhishe",

number = "10",

}

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

UR - http://www.scopus.com/inward/record.url?scp=84871229045&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=84871229045&partnerID=8YFLogxK

M3 - Article

C2 - 23289148

AN - SCOPUS:84871229045

VL - 47

SP - 1347

EP - 1357

JO - Yao xue xue bao = Acta pharmaceutica Sinica

JF - Yao xue xue bao = Acta pharmaceutica Sinica

SN - 0513-4870

IS - 10

ER -

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

Abstract

Keywords

ASJC Scopus subject areas

Other files and links

Fingerprint

Cite this