Synthesis of newer piperidinyl chalcones and their anticancer activity in human cancer cell lines

B. S. Jayashree, Harshkumar H. Patel, Neethu Susan Mathew, Yogendra Nayak

Research output: Contribution to journalArticle

8 Citations (Scopus)

Abstract

Newer tetrahydropyridine chalcones were synthesized and tested for their antioxidant and anticancer activity. These molecules showed significant anticancer activity at IC50 < 50 μM in human cancer cell lines such as A549 (lung adenocarcinoma), HepG2 (hepatocellular liver carcinoma), HeLa (cervical cancer), HCT-116 (colon carcinoma cells), MCF-7 (breast cancer cell line), and MDA MB 231 (breast cancer cells) cancer cells. The test compounds significantly inhibited cancer cell migrations in scratch wound assay for angiogenesis. Further, the test compounds bearing naphthalene substituents on the main ring showed in vitro antioxidant activity at <100 μM by 2,2′-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) radical cation, superoxide radical scavenging, O-phenonthroline, and lipid peroxidation assays. In conclusion, two test compounds bearing naphthalene substitutions exhibited potent anticancer activity that could be attributed to their ability to induce apoptosis, inhibit cancer cell migrations, provide anti-angiogenic properties, and also partly by reducing oxidative stress by scavenging free radicals.

Original languageEnglish
Pages (from-to)3673-3688
Number of pages16
JournalResearch on Chemical Intermediates
Volume42
Issue number4
DOIs
Publication statusPublished - 01-04-2016

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Chalcones
Cells
Bearings (structural)
Scavenging
Assays
Antioxidants
Oxidative stress
Sulfonic Acids
Superoxides
Liver
Free Radicals
Cations
Substitution reactions
Apoptosis
Lipids
Molecules

All Science Journal Classification (ASJC) codes

  • Chemistry(all)

Cite this

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abstract = "Newer tetrahydropyridine chalcones were synthesized and tested for their antioxidant and anticancer activity. These molecules showed significant anticancer activity at IC50 < 50 μM in human cancer cell lines such as A549 (lung adenocarcinoma), HepG2 (hepatocellular liver carcinoma), HeLa (cervical cancer), HCT-116 (colon carcinoma cells), MCF-7 (breast cancer cell line), and MDA MB 231 (breast cancer cells) cancer cells. The test compounds significantly inhibited cancer cell migrations in scratch wound assay for angiogenesis. Further, the test compounds bearing naphthalene substituents on the main ring showed in vitro antioxidant activity at <100 μM by 2,2′-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) radical cation, superoxide radical scavenging, O-phenonthroline, and lipid peroxidation assays. In conclusion, two test compounds bearing naphthalene substitutions exhibited potent anticancer activity that could be attributed to their ability to induce apoptosis, inhibit cancer cell migrations, provide anti-angiogenic properties, and also partly by reducing oxidative stress by scavenging free radicals.",
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Synthesis of newer piperidinyl chalcones and their anticancer activity in human cancer cell lines. / Jayashree, B. S.; Patel, Harshkumar H.; Mathew, Neethu Susan; Nayak, Yogendra.

In: Research on Chemical Intermediates, Vol. 42, No. 4, 01.04.2016, p. 3673-3688.

Research output: Contribution to journalArticle

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