Literature DB >> 25226228

Thiophene-3-carboxamide analogue of annonaceous acetogenins as antitumor drug lead.

Naoto Kojima1, Tetsuya Fushimi2, Takahiro Tatsukawa2, Tetsuaki Tanaka2, Mutsumi Okamura3, Akinobu Akatsuka3, Takao Yamori3, Shingo Dan3, Hiroki Iwasaki4, Masayuki Yamashita4.   

Abstract

Five novel acetogenin analogues with a furan, thiophene, or thiazole ring were synthesized, and their inhibitory activities toward human cancer cell lines were evaluated. The analogues showed more potent activities than natural acetogenin. One of them, the thiophene-3-carboxamide analogue, strongly inhibited the growth of human lung cancer cell line NCI-H23 in the xenograft mouse assay without critical toxicity.
Copyright © 2014 Elsevier Masson SAS. All rights reserved.

Entities:  

Keywords:  Annonaceous acetogenin; Antitumor activity; Chemical synthesis; Structure–activity relationship

Mesh:

Substances:

Year:  2014        PMID: 25226228     DOI: 10.1016/j.ejmech.2014.09.026

Source DB:  PubMed          Journal:  Eur J Med Chem        ISSN: 0223-5234            Impact factor:   6.514


  4 in total

1.  Structure-antitumor activity relationship of hybrid acetogenins focusing on connecting groups between heterocycles and the linker moiety.

Authors:  Kaito Ohta; Tetsuya Fushimi; Mutsumi Okamura; Akinobu Akatsuka; Shingo Dan; Hiroki Iwasaki; Masayuki Yamashita; Naoto Kojima
Journal:  RSC Adv       Date:  2022-05-25       Impact factor: 4.036

2.  Annonaceous acetogenins mediated up-regulation of Notch2 exerts growth inhibition in human gastric cancer cells in vitro.

Authors:  Yan Li; Jianbin Ye; Zhongbiao Chen; Junjie Wen; Fei Li; Pengpeng Su; Yanqing Lin; Bingxin Hu; Danlin Wu; Lijun Ning; Qi Xue; Hongxiang Gu; Yunshan Ning
Journal:  Oncotarget       Date:  2017-03-28

3.  A novel thiophene-3-carboxamide analog of annonaceous acetogenin exhibits antitumor activity via inhibition of mitochondrial complex I.

Authors:  Akinobu Akatsuka; Naoto Kojima; Mutsumi Okamura; Shingo Dan; Takao Yamori
Journal:  Pharmacol Res Perspect       Date:  2016-07-12

4.  Folate-modified Annonaceous acetogenins nanosuspensions and their improved antitumor efficacy.

Authors:  Jingyi Hong; Zhonghao Sun; Yijing Li; Yifei Guo; Yonghong Liao; Meifeng Liu; Xiangtao Wang
Journal:  Int J Nanomedicine       Date:  2017-07-14
  4 in total

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