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A novel sulfonamide agent, MPSP-001, exhibits potent activity against human cancer cells in vitro through disruption of microtubule
Alternative TitleA novel sulfonamide agent, MPSP-001, exhibits potent activity against human cancer cells in vitro through disruption of microtubule
Liu Zulong1; Tian Wei2; Wang Yong1; Kuang Shan1; Luo Xiaomin1; Yu Qiang1
2012
Source PublicationACTA PHARMACOLOGICA SINICA
ISSN1671-4083
Volume33Issue:2Pages:261-270
AbstractAim: To evaluate the anti-cancer effects of a new sulfonamide derivative, 2-(N-(3-chlorophenyl)-4-methoxyphenylsulfonamido)-N-hydroxypropanamide (MPSP-001).
Other AbstractAim: To evaluate the anti-cancer effects of a new sulfonamide derivative, 2-(N-(3-chlorophenyl)-4-methoxyphenylsulfonamido)-N-hydroxypropanamide (MPSP-001). Methods: Human cancer cell lines (HepG2, THP-1, K562, HGC-27, SKOV3, PANC-1, SW480, Kba, HeLa, A549, MDA-MB-453, and MCF-7) were examined. The cytotoxicity of MPSP-001 was evaluated using the WST-8 assay. Cell cycle distribution was examined with flow cytometry. Mitotic spindle formation was detected using immunofluorescence microscopy. Apoptosis-related proteins were examined with Western blot using specific phosphorylated protein antibodies. Competitive tubulin-binding assay was performed to test whether the compound competitively bound to the colchicine site. Molecular docking was performed to explore the possible binding conformation. Results: MPSP-001 potently inhibited the growth of the 12 different types of human cancer cells with the IC 50 values ranging from 1.9 to 15.7μmol 2 in vitro , and directly bound to the colchicine-site of β-tubulin. Molecular docking predicted that the compound may form two hydrogen bonds to the binding pocket. The compound showed synergistic effects with colchicine and taxol in blocking mitosis of HeLa cells. Conclusion: MPSP-001 shows a broad-spectrum of anti-tumor efficacy in vitro and represents a novel structure with anti-microtubule activity.
KeywordPHASE-I ANTITUMOR-ACTIVITY ANTICANCER AGENT BINDING APOPTOSIS E7070 COLCHICINE DISCOVERY HMN-214 CAMPTOTHECIN MPSP-001 sulfonamide anticancer drug microtubules tubulin mitotic spindle drug resistance drug synergism
Indexed ByCSCD
Language英语
Funding Project[National Natural Science Foundation of China] ; [Shanghai Science and Technology Research] ; [China Ministry of Science and Technology] ; [National Science & Technology Major Project "Key New Drug Creation and Manufacturing Program", China]
CSCD IDCSCD:4437497
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Document Type期刊论文
Identifierhttp://ir.imr.ac.cn/handle/321006/144913
Collection中国科学院金属研究所
Affiliation1.中国科学院
2.中国科学院金属研究所
Recommended Citation
GB/T 7714
Liu Zulong,Tian Wei,Wang Yong,et al. A novel sulfonamide agent, MPSP-001, exhibits potent activity against human cancer cells in vitro through disruption of microtubule[J]. ACTA PHARMACOLOGICA SINICA,2012,33(2):261-270.
APA Liu Zulong,Tian Wei,Wang Yong,Kuang Shan,Luo Xiaomin,&Yu Qiang.(2012).A novel sulfonamide agent, MPSP-001, exhibits potent activity against human cancer cells in vitro through disruption of microtubule.ACTA PHARMACOLOGICA SINICA,33(2),261-270.
MLA Liu Zulong,et al."A novel sulfonamide agent, MPSP-001, exhibits potent activity against human cancer cells in vitro through disruption of microtubule".ACTA PHARMACOLOGICA SINICA 33.2(2012):261-270.
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