Synthesis and biological evaluation of novel 1,6-diaryl pyridin-2(1H)-one analogs

Taijie Chen; Yu Luo; Youhong Hu; Bo Yang; Wei Lu

doi:10.1016/j.ejmech.2013.04.008

Synthesis and biological evaluation of novel 1,6-diaryl pyridin-2(1H)-one analogs

Taijie Chen
, Yu Luo^*
, Youhong Hu
, Bo Yang
, Wei Lu

^*此作品的通讯作者

化学与分子工程学院

East China Normal University
CAS - Shanghai Institute of Materia Medica
Institute of Pharmacology and Toxicology Zhejiang University

科研成果: 期刊稿件 › 文章 › 同行评审

16 引用（Scopus）

摘要

A series of 1,6-diaryl pyridin-2(1H)-one analogs were designed and synthesized via consecutive Chan-Lam coupling and Suzuki coupling. These novel compounds were evaluated for their antiproliferative activity against two tumor cell lines (SKOV-3 and HepG2). Compounds 1b, 1c, 1e and 1f displayed comparable in vitro cytotoxicity with taxol, while their in vivo antitumor activity was less effective than taxol. In addition, cell cycle assay indicated that these 1,6-diaryl pyridin-2(1H)-one compounds induced cell cycle arrest in the G1/M phase in the HepG2 cell line.

源语言	英语
页（从-至）	613-620
页数	8
期刊	European Journal of Medicinal Chemistry
卷	64
DOI	https://doi.org/10.1016/j.ejmech.2013.04.008
出版状态	已出版 - 2013

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10.1016/j.ejmech.2013.04.008

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title = "Synthesis and biological evaluation of novel 1,6-diaryl pyridin-2(1H)-one analogs",

abstract = "A series of 1,6-diaryl pyridin-2(1H)-one analogs were designed and synthesized via consecutive Chan-Lam coupling and Suzuki coupling. These novel compounds were evaluated for their antiproliferative activity against two tumor cell lines (SKOV-3 and HepG2). Compounds 1b, 1c, 1e and 1f displayed comparable in vitro cytotoxicity with taxol, while their in vivo antitumor activity was less effective than taxol. In addition, cell cycle assay indicated that these 1,6-diaryl pyridin-2(1H)-one compounds induced cell cycle arrest in the G1/M phase in the HepG2 cell line.",

keywords = "Antitumor activity, Cell cycle, Chan-Lam coupling reaction, Cytotoxicity, Pyridin-2(1H)-one",

author = "Taijie Chen and Yu Luo and Youhong Hu and Bo Yang and Wei Lu",

year = "2013",

doi = "10.1016/j.ejmech.2013.04.008",

language = "英语",

volume = "64",

pages = "613--620",

journal = "European Journal of Medicinal Chemistry",

issn = "0223-5234",

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TY - JOUR

T1 - Synthesis and biological evaluation of novel 1,6-diaryl pyridin-2(1H)-one analogs

AU - Chen, Taijie

AU - Luo, Yu

AU - Hu, Youhong

AU - Yang, Bo

AU - Lu, Wei

PY - 2013

Y1 - 2013

N2 - A series of 1,6-diaryl pyridin-2(1H)-one analogs were designed and synthesized via consecutive Chan-Lam coupling and Suzuki coupling. These novel compounds were evaluated for their antiproliferative activity against two tumor cell lines (SKOV-3 and HepG2). Compounds 1b, 1c, 1e and 1f displayed comparable in vitro cytotoxicity with taxol, while their in vivo antitumor activity was less effective than taxol. In addition, cell cycle assay indicated that these 1,6-diaryl pyridin-2(1H)-one compounds induced cell cycle arrest in the G1/M phase in the HepG2 cell line.

AB - A series of 1,6-diaryl pyridin-2(1H)-one analogs were designed and synthesized via consecutive Chan-Lam coupling and Suzuki coupling. These novel compounds were evaluated for their antiproliferative activity against two tumor cell lines (SKOV-3 and HepG2). Compounds 1b, 1c, 1e and 1f displayed comparable in vitro cytotoxicity with taxol, while their in vivo antitumor activity was less effective than taxol. In addition, cell cycle assay indicated that these 1,6-diaryl pyridin-2(1H)-one compounds induced cell cycle arrest in the G1/M phase in the HepG2 cell line.

KW - Antitumor activity

KW - Cell cycle

KW - Chan-Lam coupling reaction

KW - Cytotoxicity

KW - Pyridin-2(1H)-one

UR - https://www.scopus.com/pages/publications/84878134534

U2 - 10.1016/j.ejmech.2013.04.008

DO - 10.1016/j.ejmech.2013.04.008

M3 - 文章

C2 - 23708235

AN - SCOPUS:84878134534

SN - 0223-5234

VL - 64

SP - 613

EP - 620

JO - European Journal of Medicinal Chemistry

JF - European Journal of Medicinal Chemistry

ER -

Synthesis and biological evaluation of novel 1,6-diaryl pyridin-2(1H)-one analogs

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