Literature DB >> 20392646

Synthesis, topoisomerase I and II inhibitory activity, cytotoxicity, and structure-activity relationship study of hydroxylated 2,4-diphenyl-6-aryl pyridines.

Radha Karki1, Pritam Thapa, Mi Jeong Kang, Tae Cheon Jeong, Jung Min Nam, Hye-Lin Kim, Younghwa Na, Won-Jea Cho, Youngjoo Kwon, Eung-Seok Lee.   

Abstract

A new series of 2,4-diphenyl-6-aryl pyridines containing hydroxyl group(s) at the ortho, meta, or para position of the phenyl ring were synthesized, and evaluated for topoisomerase I and II inhibitory activity and cytotoxicity against several human cancer cell lines for the development of novel anticancer agents. Structure-activity relationship study revealed that the substitution of hydroxyl group(s) increased topoisomerase I and II inhibitory activity in the order of meta > para > ortho position. Substitution of hydroxyl group on the para position showed better cytotoxicity. (c) 2010 Elsevier Ltd. All rights reserved.

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Year:  2010        PMID： 20392646     DOI： 10.1016/j.bmc.2010.03.051

Source DB:  PubMed          Journal:  Bioorg Med Chem        ISSN： 0968-0896            Impact factor:   3.641


  8 in total

1.  Discovery of indeno[1, 2 - c] quinoline derivatives as dual topoisomerases I/II inhibitors: part 3.

Authors:  Chih-Hua Tseng; Cherng-Chyi Tzeng; Chiao-Li Yang; Pei-Jung Lu; Yu-Peng Liu; Hui-Ling Chen; Chien-Yu Chen; Chia-Ning Yang; Yeh-Long Chen
Journal:  Mol Divers       Date:  2013-11       Impact factor: 2.943

2.  Design and development of topoisomerase inhibitors using molecular modelling studies.

Authors:  Muthu K Kathiravan; Madhavi M Khilare; Aparna S Chothe; Madhuri A Nagras
Journal:  J Chem Biol       Date:  2012-09-29

3.  Hydroxylated chalcones with dual properties: Xanthine oxidase inhibitors and radical scavengers.

Authors:  Emily Hofmann; Jonathan Webster; Thuy Do; Reid Kline; Lindsey Snider; Quintin Hauser; Grace Higginbottom; Austin Campbell; Lili Ma; Stefan Paula
Journal:  Bioorg Med Chem       Date:  2015-12-17       Impact factor: 3.641

4.  Dapson in heterocyclic chemistry, part VIII: synthesis, molecular docking and anticancer activity of some novel sulfonylbiscompounds carrying biologically active 1,3-dihydropyridine, chromene and chromenopyridine moieties.

Authors:  Mansour S Al-Said; Mostafa M Ghorab; Yassin M Nissan
Journal:  Chem Cent J       Date:  2012-07-02       Impact factor: 4.215

5.  TI-I-174, a Synthetic Chalcone Derivative, Suppresses Nitric Oxide Production in Murine Macrophages via Heme Oxygenase-1 Induction and Inhibition of AP-1.

Authors:  Mi Jin Kim; Taraman Kadayat; Da Eun Kim; Eung-Seok Lee; Pil-Hoon Park
Journal:  Biomol Ther (Seoul)       Date:  2014-09-30       Impact factor: 4.634

6.  Toxicity assessments of chalcone and some synthetic chalcone analogues in a zebrafish model.

Authors:  Ya-Ting Lee; Tsorng-Harn Fong; Hui-Min Chen; Chao-Yuan Chang; Yun-Hsin Wang; Ching-Yuh Chern; Yau-Hung Chen
Journal:  Molecules       Date:  2014-01-07       Impact factor: 4.411

7.  Chalcone Derivatives Enhance ATP-Binding Cassette Transporters A1 in Human THP-1 Macrophages.

Authors:  I-Jou Teng; Min-Chien Tsai; Shao-Fu Shih; Bi-Feng Tsuei; Hsin Chang; Yi-Ping Chuang; Chin-Sheng Lin; Ching-Yuh Chern; Sy-Jou Chen
Journal:  Molecules       Date:  2018-07-03       Impact factor: 4.411

8.  Pro-Angiogenic Effects of Chalcone Derivatives in Zebrafish Embryos in Vivo.

Authors:  Yau-Hung Chen; Chao-Yuan Chang; Chiung-Fang Chang; Po-Chih Chen; Ya-Ting Lee; Ching-Yuh Chern; Jen-Ning Tsai
Journal:  Molecules       Date:  2015-07-09       Impact factor: 4.411
  8 in total

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