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 1H and 13C 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, [3H] 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.
Keywords: 5- Amino pyrazole derivatives, aryl sulfonamide, breast cancer cells, cell proliferation, cyclisation, [3H] thymidine incorporation, trypan blue exclusion assay, vero normal cells, MTT assay, DNA fragmentation analysis
Recent Patents on Anti-Cancer Drug Discovery
Title: Synthesis, Characterization and In Vitro Antiproliferative Effects of Novel 5-Amino Pyrazole Derivatives against Breast Cancer Cell Lines
Volume: 6 Issue: 2
Author(s): Hanumegowda Raju, Siddappa Chandrappa, Doddakunche S. Prasanna, Hanumappa Ananda, Tandaga S. Nagamani, Sonnahallipura M. Byregowda and Kanchugarakoppal S. Rangappa
Affiliation:
Keywords: 5- Amino pyrazole derivatives, aryl sulfonamide, breast cancer cells, cell proliferation, cyclisation, [3H] thymidine incorporation, trypan blue exclusion assay, vero normal cells, MTT assay, DNA fragmentation analysis
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 1H and 13C 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, [3H] 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.
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Raju Hanumegowda, Chandrappa Siddappa, S. Prasanna Doddakunche, Ananda Hanumappa, S. Nagamani Tandaga, M. Byregowda Sonnahallipura and S. Rangappa Kanchugarakoppal, Synthesis, Characterization and In Vitro Antiproliferative Effects of Novel 5-Amino Pyrazole Derivatives against Breast Cancer Cell Lines, Recent Patents on Anti-Cancer Drug Discovery 2011; 6 (2) . https://dx.doi.org/10.2174/157489211795328459
DOI https://dx.doi.org/10.2174/157489211795328459 |
Print ISSN 1574-8928 |
Publisher Name Bentham Science Publisher |
Online ISSN 2212-3970 |
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Novel anti-cancer drugs in photoimmunotherapy management: from bench to translational research
In recent years, traditional cancer treatments, such as surgery, chemotherapy, and radiation treatment, etc., may damage the pathological tissue and normal cells. The ideal tumor treatment should be noninvasive, eliminating the primary tumor, making the body produce systemic tumor-specific immunity, eliminating metastases, and having less /no side effects. Recent Patents ...read more
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