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Synthesis, characterization and in-vitro antiproliferative effects of novel 5-amino pyrazole derivatives against breast cancer cell lines.

Abstract
In search of synthetic chemotherapeutic substances capable of inhibiting, retarding, or reversing the process of multistage carcinogenesis, we synthesised a series of novel 1-(4-methoxybenzyl)-3-cyclopropyl-1H-pyrazol-5-amine derivatives 9(a-h) by a nucleophilic substitution reaction and characterized by (1)H and (13)C nuclear magnetic resonance (NMR), liquid chromatography mass spectrometry (LC/MS), Fourier-transform infrared (FTIR), and elemental analysis. These novel compounds were evaluated for their efficacy in inhibiting VERO normal and MCF-7 breast cancer cells proliferation by trypan blue exclusion assay, MTT assay, [(3)H] thymidine incorporation assay and DNA fragmentation analysis. Among the series, some compounds exhibited interesting growth inhibitory effects against cell lines. From the Structure-Activity Relationship studies, it has been revealed that, both novel patented compounds and therapeutic protocols of N-terminal pyrazole ring structures play key role in the antiproliferative activity.
AuthorsHanumegowda Raju, Siddappa Chandrappa, Doddakunche S Prasanna, Hanumappa Ananda, Tandaga S Nagamani, Sonnahallipura M Byregowda, Kanchugarakoppal S Rangappa
JournalRecent patents on anti-cancer drug discovery (Recent Pat Anticancer Drug Discov) Vol. 6 Issue 2 Pg. 186-95 (May 2011) ISSN: 2212-3970 [Electronic] United Arab Emirates
PMID21247401 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
Chemical References
  • Amines
  • Antineoplastic Agents
  • Pyrazoles
Topics
  • Amines (chemical synthesis, chemistry, pharmacology)
  • Animals
  • Antineoplastic Agents (chemical synthesis, chemistry, pharmacology)
  • Breast Neoplasms (drug therapy, pathology)
  • Cell Line, Tumor
  • Cell Proliferation (drug effects)
  • Chlorocebus aethiops
  • DNA Fragmentation (drug effects)
  • Drug Screening Assays, Antitumor
  • Female
  • Humans
  • Patents as Topic
  • Pyrazoles (chemical synthesis, chemistry, pharmacology)
  • Structure-Activity Relationship
  • Vero Cells

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