Synthesis and antitumor activity evaluation of PI3K inhibitors containing 3-substituted quinazolin-4(3H)-one moiety

Hao Zhang; Min Hang Xin; Xiao Xiao Xie; Shuai Mao; Sai Jie Zuo; She Min Lu; San Qi Zhang

doi:10.1016/j.bmc.2015.11.027

Synthesis and antitumor activity evaluation of PI3K inhibitors containing 3-substituted quinazolin-4(3H)-one moiety

Hao Zhang
, Min Hang Xin
, Xiao Xiao Xie
, Shuai Mao
, Sai Jie Zuo
, She Min Lu
, San Qi Zhang

Health Science Center

Xi'an Jiaotong University

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

23 Scopus citations

Abstract

In present study, a series of N-(2-methoxy-5-(3-substituted quinazolin-4(3H)-one-6-yl)-pyridin-3-yl)phenylsulfonamide were synthesized. Their antiproliferative activities in vitro were evaluated via MTT assay against HCT116 and MCF-7 cancer cell lines. The SAR of title compounds was discussed. The compounds (S)-C5 and (S)-C8 displayed potent inhibitory activity against PI3Ks and mTOR, especially against PI3Kα. In addition, compound (S)-C5 can efficaciously inhibit tumor growth in a mice S-180 model. These findings suggest that our designed compounds can serve as potent PI3K inhibitors and effective anticancer agents.

Original language	English
Pages (from-to)	7765-7776
Number of pages	12
Journal	Bioorganic and Medicinal Chemistry
Volume	23
Issue number	24
DOIs	https://doi.org/10.1016/j.bmc.2015.11.027
State	Published - 15 Dec 2015

UN SDGs

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

SDG 3 Good Health and Well-being

Keywords

Antitumor activity
PI3K inhibitor
Quinazolin-4(3H)-ones
Synthesis

Access to Document

10.1016/j.bmc.2015.11.027

Cite this

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title = "Synthesis and antitumor activity evaluation of PI3K inhibitors containing 3-substituted quinazolin-4(3H)-one moiety",

abstract = "In present study, a series of N-(2-methoxy-5-(3-substituted quinazolin-4(3H)-one-6-yl)-pyridin-3-yl)phenylsulfonamide were synthesized. Their antiproliferative activities in vitro were evaluated via MTT assay against HCT116 and MCF-7 cancer cell lines. The SAR of title compounds was discussed. The compounds (S)-C5 and (S)-C8 displayed potent inhibitory activity against PI3Ks and mTOR, especially against PI3Kα. In addition, compound (S)-C5 can efficaciously inhibit tumor growth in a mice S-180 model. These findings suggest that our designed compounds can serve as potent PI3K inhibitors and effective anticancer agents.",

keywords = "Antitumor activity, PI3K inhibitor, Quinazolin-4(3H)-ones, Synthesis",

author = "Hao Zhang and Xin, \{Min Hang\} and Xie, \{Xiao Xiao\} and Shuai Mao and Zuo, \{Sai Jie\} and Lu, \{She Min\} and Zhang, \{San Qi\}",

note = "Publisher Copyright: {\textcopyright} 2015 Published by Elsevier Ltd.",

year = "2015",

month = dec,

day = "15",

doi = "10.1016/j.bmc.2015.11.027",

language = "英语",

volume = "23",

pages = "7765--7776",

journal = "Bioorganic and Medicinal Chemistry",

issn = "0968-0896",

publisher = "Elsevier Ltd",

number = "24",

}

TY - JOUR

T1 - Synthesis and antitumor activity evaluation of PI3K inhibitors containing 3-substituted quinazolin-4(3H)-one moiety

AU - Zhang, Hao

AU - Xin, Min Hang

AU - Xie, Xiao Xiao

AU - Mao, Shuai

AU - Zuo, Sai Jie

AU - Lu, She Min

AU - Zhang, San Qi

PY - 2015/12/15

Y1 - 2015/12/15

N2 - In present study, a series of N-(2-methoxy-5-(3-substituted quinazolin-4(3H)-one-6-yl)-pyridin-3-yl)phenylsulfonamide were synthesized. Their antiproliferative activities in vitro were evaluated via MTT assay against HCT116 and MCF-7 cancer cell lines. The SAR of title compounds was discussed. The compounds (S)-C5 and (S)-C8 displayed potent inhibitory activity against PI3Ks and mTOR, especially against PI3Kα. In addition, compound (S)-C5 can efficaciously inhibit tumor growth in a mice S-180 model. These findings suggest that our designed compounds can serve as potent PI3K inhibitors and effective anticancer agents.

AB - In present study, a series of N-(2-methoxy-5-(3-substituted quinazolin-4(3H)-one-6-yl)-pyridin-3-yl)phenylsulfonamide were synthesized. Their antiproliferative activities in vitro were evaluated via MTT assay against HCT116 and MCF-7 cancer cell lines. The SAR of title compounds was discussed. The compounds (S)-C5 and (S)-C8 displayed potent inhibitory activity against PI3Ks and mTOR, especially against PI3Kα. In addition, compound (S)-C5 can efficaciously inhibit tumor growth in a mice S-180 model. These findings suggest that our designed compounds can serve as potent PI3K inhibitors and effective anticancer agents.

KW - Antitumor activity

KW - PI3K inhibitor

KW - Quinazolin-4(3H)-ones

KW - Synthesis

UR - https://www.scopus.com/pages/publications/84949503611

U2 - 10.1016/j.bmc.2015.11.027

DO - 10.1016/j.bmc.2015.11.027

M3 - 文章

C2 - 26652969

AN - SCOPUS:84949503611

SN - 0968-0896

VL - 23

SP - 7765

EP - 7776

JO - Bioorganic and Medicinal Chemistry

JF - Bioorganic and Medicinal Chemistry

IS - 24

ER -

Synthesis and antitumor activity evaluation of PI3K inhibitors containing 3-substituted quinazolin-4(3H)-one moiety

Abstract

UN SDGs

Keywords

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