Synthesis and biological evaluation of novel 2-arylamino-3-(arylsulfonyl)quinoxalines as PI3Kα inhibitors

Peng Wu; Yi Su; Xiaowen Liu; Lei Zhang; Yong Ye; Jianchao Xu; Shaoyu Weng; Yani Li; Tao Liu; Shufang Huang; Bo Yang; Qiaojun He; Yongzhou Hu

doi:10.1016/j.ejmech.2011.09.015

Synthesis and biological evaluation of novel 2-arylamino-3-(arylsulfonyl)quinoxalines as PI3Kα inhibitors

Peng Wu
, Yi Su
, Xiaowen Liu
, Lei Zhang
, Yong Ye
, Jianchao Xu
, Shaoyu Weng
, Yani Li
, Tao Liu
, Shufang Huang
, Bo Yang
, Qiaojun He
, Yongzhou Hu

Zhejiang University

Research output: Contribution to journal › Journal article › Research › peer-review

Abstract

A series of novel 2-arylamino-3-(arylsulfonyl)quinoxalines was synthesized through a newly developed approach. All synthesized target compounds were screened for their cytotoxicities against cancer cell lines including PC3, A549, HCT116, HL60 and KB. Representative compounds with favorable cytotoxicities were tested for their PI3Kα inhibitory activities. Among the synthesized target compounds, 17 (PI3Kα IC50: 0.07 μM) displayed the most potent cellular activities (IC50 values of 0.14 μM, 0.07 μM, 0.95 μM and 0.05 μM against PC3, A549, HCT116 and HL 60, respectively).

Original language	English
Journal	European Journal of Medicinal Chemistry
Volume	46
Issue number	11
Pages (from-to)	5540–5548
ISSN	0223-5234
DOIs	https://doi.org/10.1016/j.ejmech.2011.09.015
Publication status	Published - 2011
Externally published	Yes

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This output contributes to the following UN Sustainable Development Goals (SDGs)

SDG 3 Good Health and Well-being

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10.1016/j.ejmech.2011.09.015

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@article{36c267237d6a41b3ae172ed83e6ba330,

title = "Synthesis and biological evaluation of novel 2-arylamino-3-(arylsulfonyl)quinoxalines as PI3Kα inhibitors",

abstract = "A series of novel 2-arylamino-3-(arylsulfonyl)quinoxalines was synthesized through a newly developed approach. All synthesized target compounds were screened for their cytotoxicities against cancer cell lines including PC3, A549, HCT116, HL60 and KB. Representative compounds with favorable cytotoxicities were tested for their PI3Kα inhibitory activities. Among the synthesized target compounds, 17 (PI3Kα IC50: 0.07 μM) displayed the most potent cellular activities (IC50 values of 0.14 μM, 0.07 μM, 0.95 μM and 0.05 μM against PC3, A549, HCT116 and HL 60, respectively).",

author = "Peng Wu and Yi Su and Xiaowen Liu and Lei Zhang and Yong Ye and Jianchao Xu and Shaoyu Weng and Yani Li and Tao Liu and Shufang Huang and Bo Yang and Qiaojun He and Yongzhou Hu",

year = "2011",

doi = "10.1016/j.ejmech.2011.09.015",

language = "English",

volume = "46",

pages = "5540–5548",

journal = "European Journal of Medicinal Chemistry",

issn = "0223-5234",

publisher = "Elsevier Masson s.r.l.",

number = "11",

}

TY - JOUR

T1 - Synthesis and biological evaluation of novel 2-arylamino-3-(arylsulfonyl)quinoxalines as PI3Kα inhibitors

AU - Wu, Peng

AU - Su, Yi

AU - Liu, Xiaowen

AU - Zhang, Lei

AU - Ye, Yong

AU - Xu, Jianchao

AU - Weng, Shaoyu

AU - Li, Yani

AU - Liu, Tao

AU - Huang, Shufang

AU - Yang, Bo

AU - He, Qiaojun

AU - Hu, Yongzhou

PY - 2011

Y1 - 2011

N2 - A series of novel 2-arylamino-3-(arylsulfonyl)quinoxalines was synthesized through a newly developed approach. All synthesized target compounds were screened for their cytotoxicities against cancer cell lines including PC3, A549, HCT116, HL60 and KB. Representative compounds with favorable cytotoxicities were tested for their PI3Kα inhibitory activities. Among the synthesized target compounds, 17 (PI3Kα IC50: 0.07 μM) displayed the most potent cellular activities (IC50 values of 0.14 μM, 0.07 μM, 0.95 μM and 0.05 μM against PC3, A549, HCT116 and HL 60, respectively).

AB - A series of novel 2-arylamino-3-(arylsulfonyl)quinoxalines was synthesized through a newly developed approach. All synthesized target compounds were screened for their cytotoxicities against cancer cell lines including PC3, A549, HCT116, HL60 and KB. Representative compounds with favorable cytotoxicities were tested for their PI3Kα inhibitory activities. Among the synthesized target compounds, 17 (PI3Kα IC50: 0.07 μM) displayed the most potent cellular activities (IC50 values of 0.14 μM, 0.07 μM, 0.95 μM and 0.05 μM against PC3, A549, HCT116 and HL 60, respectively).

U2 - 10.1016/j.ejmech.2011.09.015

DO - 10.1016/j.ejmech.2011.09.015

M3 - Journal article

C2 - 21945250

SN - 0223-5234

VL - 46

SP - 5540

EP - 5548

JO - European Journal of Medicinal Chemistry

JF - European Journal of Medicinal Chemistry

IS - 11

ER -

Synthesis and biological evaluation of novel 2-arylamino-3-(arylsulfonyl)quinoxalines as PI3Kα inhibitors

Abstract

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