Literature DB >> 25442306

Synthesis and identification of α-cyano bis(indolyl)chalcones as novel anticancer agents.

Dalip Kumar1, N Maruthi Kumar2, Mukund P Tantak2, Maiko Ogura3, Eriko Kusaka3, Takeo Ito4.   

Abstract

Microwave-assisted synthesis of 23 α-cyano bis(indolyl)chalcones (6a-w) and their in vitro anticancer activity against three human cancer cell lines have been discussed. Among the synthesized chalcones, compound 6n was found to be the most potent and selective against A549 lung cancer cell line (IC50 = 0.8 μM). In a preliminary mechanism of action studies some α-cyano bis(indolyl)chalcones were found to enhance tubulin polymerization suggesting these compounds could act as microtubule stabilizing agents.
Copyright © 2014 Elsevier Ltd. All rights reserved.

Entities:  

Keywords:  Anticancer agents; Bis(indole); Chalcones; Microwave-assisted synthesis; Tubulin inhibitors

Mesh：

Substances：

Year:  2014        PMID： 25442306     DOI： 10.1016/j.bmcl.2014.09.085

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  7 in total

1.  2-(3'-Indolyl)-N-arylthiazole-4-carboxamides: Synthesis and evaluation of antibacterial and anticancer activities.

Authors:  Mukund P Tantak; Jing Wang; Rajnish Prakash Singh; Anil Kumar; Kavita Shah; Dalip Kumar
Journal:  Bioorg Med Chem Lett       Date:  2015-08-06       Impact factor: 2.823

Review 2.  Target-based anticancer indole derivatives and insight into structure‒activity relationship: A mechanistic review update (2018-2021).

Authors:  Ashima Dhiman; Rupam Sharma; Rajesh K Singh
Journal:  Acta Pharm Sin B       Date:  2022-04-01       Impact factor: 14.903

3.  The crystal structures of two chalcones: (2E)-1-(5-chloro-thio-phen-2-yl)-3-(2-methyl-phen-yl)prop-2-en-1-one and (2E)-1-(anthracen-9-yl)-3-[4-(propan-2-yl)phen-yl]prop-2-en-1-one.

Authors:  Marisiddaiah Girisha; Hemmige S Yathirajan; Jerry P Jasinski; Christopher Glidewell
Journal:  Acta Crystallogr E Crystallogr Commun       Date:  2016-07-19

4.  Novel indolyl-chalcone derivatives inhibit A549 lung cancer cell growth through activating Nrf-2/HO-1 and inducing apoptosis in vitro and in vivo.

Authors:  Xuan Zhao; WenLiang Dong; YuanDi Gao; Dong-Shoo Shin; Qing Ye; Le Su; Fan Jiang; BaoXiang Zhao; JunYing Miao
Journal:  Sci Rep       Date:  2017-06-20       Impact factor: 4.379

5.  Novel 3-(3, 5-difluoro-4-hydroxyphenyl)-1-(naphthalen-2-yl) prop-2-en-1-one as a potent inhibitor of MAP-kinase in HeLa cell lines and anti-angiogenic activity is mediated by HIF-1α in EAC animal model.

Authors:  Dileep Kumar M Guruswamy; Kyathegowdana Doddi Srivinavasa Balaji; Kattepura Krishnappa Dharmappa; Shankar Jayarama
Journal:  Oncotarget       Date:  2020-12-15

6.  Synthesis and photobiological applications of naphthalimide-benzothiazole conjugates: cytotoxicity and topoisomerase IIα inhibition.

Authors:  Iqubal Singh; Vijay Luxami; Diptiman Choudhury; Kamaldeep Paul
Journal:  RSC Adv       Date:  2021-12-22       Impact factor: 3.361

Review 7.  Chalcone Scaffold in Anticancer Armamentarium: A Molecular Insight.

Authors:  Manik Das; Kuntal Manna
Journal:  J Toxicol       Date:  2016-01-03
  7 in total

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