Synthesis, molecular docking and anticancer studies of peptides and iso-peptides

Research output: Contribution to journalArticle

5 Citations (Scopus)

Abstract

Chiral peptides and iso-peptides were synthesized in excellent yield by using benzotriazole mediated solution phase synthesis. Benzotriazole acted both as activating and leaving group, eliminating frequent use of protection and subsequent deprotection. The procedure was based on the hypothesis that epimerization should be suppressed in solution due to a faster coupling rate than SPPS. All the synthesized peptides complied with Lipinski's Ro5 except for the rotatable bonds. Inhibition of cell proliferation of cancer cell lines is one of the most commonly used methods to study the effectiveness of any anticancer agents. Synthesized peptides and iso-peptides were tested against three cancer cell lines (MCF-7, MDA-MB 231) to determine their anti-proliferative potential. NFkB was also determined. Molecular docking studies were also carried out to complement the experimental results.

Original languageEnglish (US)
Pages (from-to)2980-4
Number of pages5
JournalBioorganic and Medicinal Chemistry Letters
Volume25
Issue number15
DOIs
StatePublished - Aug 1 2015

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Peptides
Cells
Cell Line
Cell proliferation
Antineoplastic Agents
Neoplasms
Cell Proliferation
benzotriazole

Keywords

  • Antineoplastic Agents
  • Breast Neoplasms
  • Cell Line, Tumor
  • Cell Proliferation
  • Drug Screening Assays, Antitumor
  • Female
  • Humans
  • MCF-7 Cells
  • Molecular Docking Simulation
  • NF-kappa B
  • Peptides
  • Triazoles
  • Journal Article
  • Research Support, Non-U.S. Gov't

Cite this

Synthesis, molecular docking and anticancer studies of peptides and iso-peptides. / Panda, Siva S.

In: Bioorganic and Medicinal Chemistry Letters, Vol. 25, No. 15, 01.08.2015, p. 2980-4.

Research output: Contribution to journalArticle

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abstract = "Chiral peptides and iso-peptides were synthesized in excellent yield by using benzotriazole mediated solution phase synthesis. Benzotriazole acted both as activating and leaving group, eliminating frequent use of protection and subsequent deprotection. The procedure was based on the hypothesis that epimerization should be suppressed in solution due to a faster coupling rate than SPPS. All the synthesized peptides complied with Lipinski's Ro5 except for the rotatable bonds. Inhibition of cell proliferation of cancer cell lines is one of the most commonly used methods to study the effectiveness of any anticancer agents. Synthesized peptides and iso-peptides were tested against three cancer cell lines (MCF-7, MDA-MB 231) to determine their anti-proliferative potential. NFkB was also determined. Molecular docking studies were also carried out to complement the experimental results.",
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N2 - Chiral peptides and iso-peptides were synthesized in excellent yield by using benzotriazole mediated solution phase synthesis. Benzotriazole acted both as activating and leaving group, eliminating frequent use of protection and subsequent deprotection. The procedure was based on the hypothesis that epimerization should be suppressed in solution due to a faster coupling rate than SPPS. All the synthesized peptides complied with Lipinski's Ro5 except for the rotatable bonds. Inhibition of cell proliferation of cancer cell lines is one of the most commonly used methods to study the effectiveness of any anticancer agents. Synthesized peptides and iso-peptides were tested against three cancer cell lines (MCF-7, MDA-MB 231) to determine their anti-proliferative potential. NFkB was also determined. Molecular docking studies were also carried out to complement the experimental results.

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KW - Cell Proliferation

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KW - Humans

KW - MCF-7 Cells

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KW - Triazoles

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