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.
|
Authors | Hanumegowda Raju, Siddappa Chandrappa, Doddakunche S Prasanna, Hanumappa Ananda, Tandaga S Nagamani, Sonnahallipura M Byregowda, Kanchugarakoppal S Rangappa |
Journal | Recent 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 |
PMID | 21247401
(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
|