Literature DB >> 22071256

1,2,3-Triazole tethered β-lactam-chalcone bifunctional hybrids: synthesis and anticancer evaluation.

Pardeep Singh1, Raghu Raj, Vipan Kumar, Mohinder P Mahajan, P M S Bedi, Tandeep Kaur, A K Saxena.   

Abstract

The manuscript describes the synthesis of novel 1,2,3-triazole tethered β-lactam-chalcone bifunctional hybrids via click chemistry approach utilizing azide-alkyne cycloaddition reactions and their evaluation as anticancer agents against four human cancer cell lines. The presence of a cyclohexyl substituent at N-1 of β-lactam ring and methoxy substituents, preferably ortho on ring A and para on ring B on chalcones markedly improved the anticancer profiles of the synthesized scaffolds with the most potent of the test compound exhibiting an IC(50) value of <1, 67.1, <1 and 6.37 μM against A-549(lung), PC-3(prostate), THP-1(leukemia), and Caco-2(colon) cell lines, respectively.
Copyright © 2011 Elsevier Masson SAS. All rights reserved.

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Year:  2011        PMID: 22071256     DOI: 10.1016/j.ejmech.2011.10.033

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


  15 in total

Review 1.  Chalcone: A Privileged Structure in Medicinal Chemistry.

Authors:  Chunlin Zhuang; Wen Zhang; Chunquan Sheng; Wannian Zhang; Chengguo Xing; Zhenyuan Miao
Journal:  Chem Rev       Date:  2017-05-10       Impact factor: 60.622

2.  Synthesis of novel perillyl-dihydropyrimidinone hybrids designed for antiproliferative activity.

Authors:  Vinicius Vendrusculo; Vanessa P de Souza; Luiz Antônio M Fontoura; Marcelo G M D'Oca; Thais P Banzato; Paula A Monteiro; Ronaldo A Pilli; João Ernesto de Carvalho; Dennis Russowsky
Journal:  Medchemcomm       Date:  2018-07-31       Impact factor: 3.597

3.  Design, synthesis and antiproliferative evaluation of novel sulfanilamide-1,2,3-triazole derivatives as tubulin polymerization inhibitors.

Authors:  Shewei Guo; Yingwei Zhen; Mengguo Guo; Longzhou Zhang; Guosheng Zhou
Journal:  Invest New Drugs       Date:  2018-07-18       Impact factor: 3.850

4.  (E)-N-(4-{[1-(Prop-2-en-1-yl)-1H-1,2,3-triazol-4-yl]meth-oxy}benzyl-idene)morpholin-4-amine.

Authors:  Mehmet Akkurt; Aliasghar Jarrahpour; Mehdi Mohammadi Chermahini; Pezhman Shiri; Namık Ozdemir
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2014-02-12

5.  Synthetic chalcones with potent antioxidant ability on H₂O₂-induced apoptosis in PC12 cells.

Authors:  Jian-Zhang Wu; Chan-Chan Cheng; Lai-Lai Shen; Zhan-Kun Wang; Shou-Biao Wu; Wu-Lan Li; Su-Hua Chen; Rong-Ping Zhou; Pei-Hong Qiu
Journal:  Int J Mol Sci       Date:  2014-10-14       Impact factor: 5.923

6.  Anti-tubercular activity and molecular docking studies of indolizine derivatives targeting mycobacterial InhA enzyme.

Authors:  Katharigatta N Venugopala; Sandeep Chandrashekharappa; Pran Kishore Deb; Christophe Tratrat; Melendhran Pillay; Deepak Chopra; Nizar A Al-Shar'i; Wafa Hourani; Lina A Dahabiyeh; Pobitra Borah; Rahul D Nagdeve; Susanta K Nayak; Basavaraj Padmashali; Mohamed A Morsy; Bandar E Aldhubiab; Mahesh Attimarad; Anroop B Nair; Nagaraja Sreeharsha; Michelyne Haroun; Sheena Shashikanth; Viresh Mohanlall; Raghuprasad Mailavaram
Journal:  J Enzyme Inhib Med Chem       Date:  2021-12       Impact factor: 5.051

7.  4-(1-Methyl-eth-yl)-N-((E)-4-{[1-(prop-2-en-1-yl)-1H-1,2,3-triazol-4-yl]meth-oxy}benzyl-idene)aniline.

Authors:  Mehmet Akkurt; Aliasghar Jarrahpour; Mehdi Mohammadi Chermahini; Pezhman Shiri; Muhammad Nawaz Tahir
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2013-01-19

8.  (E)-3-(3,5-Dimeth-oxy-phen-yl)-1-(1-hy-droxy-naphthalen-2-yl)prop-2-en-1-one.

Authors:  Ha-Jin Lee; Yoongho Lim; Dongsoo Koh
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2012-11-24

9.  (2E)-3-(4-Fluoro-phen-yl)-1-[5-methyl-1-(4-methyl-phen-yl)-1H-1,2,3-triazol-4-yl]prop-2-en-1-one.

Authors:  Bakr F Abdel-Wahab; Hanan A Mohamed; Seik Weng Ng; Edward R T Tiekink
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2013-04-05

10.  (E)-N-(1,3-Benzodioxol-5-yl)-1-(4-{[1-(prop-2-en-1-yl)-1H-1,2,3-triazol-4-yl]meth-oxy}phen-yl)methanimine.

Authors:  Mehmet Akkurt; Aliasghar Jarrahpour; Mehdi Mohammadi Chermahini; Pezhman Shiri; Orhan Büyükgüngör
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2013-09-21
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