Anti-cancer activity of 2,4-disubstituted thiophene derivatives: dual inhibitors of lipoxygenase and cyclooxygenase

Sathya, Rakesh K. and Swamy, Jagadish and Swaroop, T. R. and Mohan, C. D. and Ashwini, N. and Bhadraiah, Harsha K. and Zameer, Farhan and Girish, K. S. and Rangappa, K. S. (2015) Anti-cancer activity of 2,4-disubstituted thiophene derivatives: dual inhibitors of lipoxygenase and cyclooxygenase. Medicinal Chemistry, 11 (5). pp. 462-472. ISSN 1573-4064

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Official URL: http://dx.doi.org/10.2174/157340641166614121014191...

Abstract

2,4-Disubstituted thiophene derivatives were synthesized and assessed for anti-inflammatory and anti-cancer activities by targeting at two important enzymes of the arachidonic acid metabolism. Both lipoxygenase and cyclooxygenase enzymes play vital role in chronic inflammation and carcinogenesis. Previous studies have proved that COX-2 and 5-LOX are highly activated in various types of cancers; hence inhibition of these clinically important enzymes constitutes the essential criterion for the suppression of tumor progression and metastasis. Among the tested derivatives, 2d and 2g compounds emerged as potent inhibitors of lipoxygenase and cyclooxygenase enzymes. The potent inhibitor of cyclooxygenase was further tested for in vitro cytotoxicity on cervical cancer (HeLa) cells and in vivo tumor model studies using EAT bearing mice where 2-(3,4,5-trimethoxyphenyl)-4-(N-methylindol-3-yl) thiophene (2g) showed eloquent activity. Further, in silico modeling results confirmed the active catalytic ligand binding pockets which is evident from higher atomic contact energy values of 2d and 2g than compared to standard drug. Thus, 2g may find better application in management of inflammation and in pro-apoptotic therapeutic engineering.

Item Type: Article
Additional Information: Unmapped bibliographic data: DA - 2014/12// [EPrints field already has value set] LA - eng [Field not mapped to EPrints] DB - PubMed [Field not mapped to EPrints] J2 - Med Chem [Field not mapped to EPrints] AN - 25494807 [Field not mapped to EPrints] JO - Medicinal chemistry (Shariqah (United Arab Emirates)) [Field not mapped to EPrints]
Subjects: Physical Sciences > Chemistry
Divisions: PG Campuses > Manasagangotri, Mysore > Chemistry
Depositing User: Praveen Kumari B.L
Date Deposited: 18 May 2015 07:01
Last Modified: 05 May 2016 09:25
URI: http://eprints.uni-mysore.ac.in/id/eprint/17882

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