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Literature DB >> 15893928

Synthesis and biological evaluation of chalcones and their derived pyrazoles as potential cytotoxic agents.

B A Bhat¹, K L Dhar, S C Puri, A K Saxena, M Shanmugavel, G N Qazi.

Abstract

A series of substituted chalcones and their corresponding pyrazoles were synthesized and evaluated for in vitro cytotoxic activity against a panel of human cancer cell lines. Out of 93 compounds screened, 8 compounds, 1s, 3i,j,n, 4i,j,n and 4s, showed marked activity. Compounds 4j,n and 4s were found to be the most promising in this study. SAR is also discussed.

Entities: Chemical Disease Gene Species

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Year: 2005 PMID： 15893928 DOI： 10.1016/j.bmcl.2005.03.121

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

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Cited

37 in total

1. Crystal structure of (E)-1-(1-hy-droxy-naphthalen-2-yl)-3-(2,3,4-tri-meth-oxy-phen-yl)prop-2-en-1-one.

Authors: J Srividya; D Reuben Jonathan; B K Revathi; G Anbalagan
Journal: Acta Crystallogr E Crystallogr Commun Date: 2015-07-29

2. New bichalcone analogs as NF-κB inhibitors and as cytotoxic agents inducing Fas/CD95-dependent apoptosis.

Authors: M Vijaya Bhaskar Reddy; Yuh-Chiang Shen; Jai-Sing Yang; Tsong-Long Hwang; Kenneth F Bastow; Keduo Qian; Kuo-Hsiung Lee; Tian-Shung Wu
Journal: Bioorg Med Chem Date: 2011-03-04 Impact factor: 3.641

3. One-pot diastreoselective synthesis of highly functionalized cyclohexenones: 2-oxo-N,4,6-triarylcyclohex-3-enecarboxamides.

Authors: Mir Rasul Mousavi; Malek Taher Maghsoodlou; Sayyed Mostafa Habibi-Khorassani
Journal: Mol Divers Date: 2014-08-06 Impact factor: 2.943

4. Cytotoxic 3,4,5-trimethoxychalcones as mitotic arresters and cell migration inhibitors.

Authors: Lívia B Salum; Wanessa F Altei; Louise D Chiaradia; Marlon N S Cordeiro; Rafael R Canevarolo; Carolina P S Melo; Evelyn Winter; Bruno Mattei; Hikmat N Daghestani; Maria Cláudia Santos-Silva; Tânia B Creczynski-Pasa; Rosendo A Yunes; José A Yunes; Adriano D Andricopulo; Billy W Day; Ricardo J Nunes; Andreas Vogt
Journal: Eur J Med Chem Date: 2013-03-06 Impact factor: 6.514

Synthesis and biological evaluation of chalcones and their derived pyrazoles as potential cytotoxic agents.

1. Crystal structure of (E)-1-(1-hy-droxy-naphthalen-2-yl)-3-(2,3,4-tri-meth-oxy-phen-yl)prop-2-en-1-one.

2. New bichalcone analogs as NF-κB inhibitors and as cytotoxic agents inducing Fas/CD95-dependent apoptosis.

3. One-pot diastreoselective synthesis of highly functionalized cyclohexenones: 2-oxo-N,4,6-triarylcyclohex-3-enecarboxamides.

4. Cytotoxic 3,4,5-trimethoxychalcones as mitotic arresters and cell migration inhibitors.

5. (E)-3-[4-(Dodec-yloxy)phen-yl]-1-(2-hydroxy-phen-yl)prop-2-en-1-one.

6. (E)-3-[4-(Dec-yloxy)phen-yl]-1-(4-hydroxy-phen-yl)prop-2-en-1-one.

7. (E)-3-[4-(Hex-yloxy)phen-yl]-1-(2-hydroxy-phen-yl)prop-2-en-1-one.

8. (2E,4E)-1-(6-Chloro-2-methyl-4-phenyl-3-quinol-yl)-5-phenyl-penta-2,4-dien-1-one.

9. (E)-3-[4-(Hex-yloxy)phen-yl]-1-(4-hydroxy-phen-yl)prop-2-en-1-one.

10. (E)-3-(4-Decyl-oxyphen-yl)-1-(2-hydroxy-phen-yl)prop-2-en-1-one.