Synthesis of Bis‐acridine Derivatives Exhibiting Anticancer and Anti‐inflammatory Activity. (7th March 2013)

• Record Type: Journal Article
• Authors: Sondhi, Sham M.; Kumar, Sandeep; Rani, Reshma; Chakraborty, Ajanta; Roy, Partha
• Is Part Of: Journal of heterocyclic chemistry. Volume 50:Number 2(2013:Mar.)
• Page Start: 252
• Page End: 260
• Publication Date: 2013-03-07
• Subjects: Heterocyclic compounds -- Periodicals; 547.59
• DOI: 10.1002/jhet.985
• Languages: English
• ISSNs: 0022-152X

Abstract

<abstract abstract-type="main" xml:lang="en" id="jhet985-abs-0001"> <title> <x xml:space="preserve">Abstract</x> </title> <p id="jhet985-para-0002">A series of bis‐acridine derivatives <bold>3a</bold>–<bold>j</bold> and <bold>5a</bold>–<bold>j</bold> have been synthesized by condensation of 9‐chloro‐2, 4‐(un)substituted acridines <bold>(1a</bold>–<bold>e)</bold> and 9‐isothiocyanato‐2, 4‐(un)substituted acridines <bold>(4a</bold>–<bold>e)</bold> with diamine <bold>2a</bold> and <bold>2b</bold>, respectively. These bis‐acridines were evaluated <italic>in vitro</italic> for activity against a panel of human cancer cell lines of lung (NCI H‐522), ovary (PA1), breast (T47D), colon (HCT‐15), and liver (HepG2). Several bis‐acridines were found to possess good anticancer activity against various cancer cell lines. Of these, compound <bold>3h</bold> exhibited good anticancer activity against all cancer cell lines tested except liver (HepG2) cell line. In addition to this, these compounds were screened for anti‐inflammatory activity at a dose of 50 mg/kg p.o<italic>.</italic> Compound <bold>3g</bold> exhibited 41% anti‐inflammatory activity, which is better than most commonly used standard drug <named-content id="jhet985-info-0001" content-type="drugGenericName" xlink:type="simple" xmlns:xlink="http://www.w3.org/1999/xlink">ibuprofen</named-content>, which showed 39% anti‐inflammatory (at 50 mg/kg <italic>p</italic>. <italic>o</italic>.) activity.</p> </abstract>