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<p>Synthesis, characterization, cytotoxicity evaluation and molecular docking study of new bis-chalcone, fused-pyrimidine and fused-pyrazoline derivatives</p>

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Title Statement <p>Synthesis, characterization, cytotoxicity evaluation and molecular docking study of new bis-chalcone, fused-pyrimidine and fused-pyrazoline derivatives</p>
 
Added Entry - Uncontrolled Name Bakar, Bazri Izwan; School of Chemical Sciences, University Sains Malaysia, 11800 Penang, Malaysia
Alidmat, Mohammad Murwih; School of Chemical Sciences, University Sains Malaysia, 11800 Penang, Malaysia
Khairuddean, Melati ; School of Chemical Sciences, University Sains Malaysia, 11800 Penang, Malaysia
Ibrahim, Wan Nuaralia Asyikin Wan; School of Chemical Sciences, University Sains Malaysia, 11800 Penang, Malaysia
Mun, Kwan Wai; School of Chemical Sciences, University Sains Malaysia, 11800 Penang, Malaysia
Kamal, Nik Nur Syazni Nik Mohammad; Advanced Medical and Dental Institute, Universiti Sains Malaysia, 13200 Kepala Batas, Penang, Malaysia
Muhammad, Musthahimah ; Advanced Medical and Dental Institute, Universiti Sains Malaysia, 13200 Kepala Batas, Penang, Malaysia
 
Uncontrolled Index Term Chalone, Pyrimidine, Pyrazoline, Anticancer, Claisen-Schmidt condensation
 
Summary, etc. <p class="Abstract" style="text-align: justify;"><span lang="EN-GB">Chemotherapeutic drug resistance and high-risk side effects are common limitations in cancer treatment. Thus, the continuous development of new drugs that target only the cancer cell without affecting the normal cells is needed. The simple structure of the chalcone and the ease of its synthesis showed promising functions. Such compounds have been reported to exhibit diverse pharmacological activities, particularly anticancer. This study involves the design of chalcones <strong>1</strong> and <strong>2 </strong>which have been synthesized via Claisen-Schmidt condensation. Further cyclo-condensation reactions of these chalcone compounds has formed five pyrazoline and three pyrimidine derivatives. All the desired derivatives are characterised by FT-IR, <sup>1</sup>H-NMR, and <sup>13</sup>C-NMR. These derivatives are tested for cytotoxicity against breast cancer cell lines (MCF-7 and MD-MB-231) and normal breast cell lines (MCF-10A). The results emphasized that pyrazoline compounds <strong>1Aii </strong>and<strong> 1Aiii </strong>are showing the minimum inhibition against MCF-7 with the IC<sub>50 </sub>values of56.73±3.3 µM and 37.74±1.32 µM, respectively, after 24 h of exposure, which are comparable to Tamoxifen, as reference anticancer drug (IC<sub>50</sub> = 42.66±2.19 µM).</span></p>
 
Publication, Distribution, Etc. Indian Journal of Chemistry (IJC)
2023-03-17 15:15:07
 
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http://op.niscair.res.in/index.php/IJC/article/view/72060
 
Data Source Entry Indian Journal of Chemistry (IJC); ##issue.vol## 62, ##issue.no## 3 (2023): Indian Journal of Chemistry-(IJC)
 
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