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

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Title Synthesis, characterization, cytotoxicity evaluation and molecular docking study of new bis-chalcone, fused-pyrimidine and fused-pyrazoline derivatives
 
Creator Bakar, Bazri Izwan
Alidmat, Mohammad Murwih
Khairuddean, Melati
Ibrahim, Wan Nuaralia Asyikin Wan
Mun, Kwan Wai
Kamal, Nik Nur Syazni Nik Mohammad
Muhammad, Musthahimah
 
Subject Chalone
Pyrimidine
Pyrazoline
Anticancer
Claisen-Schmidt condensation
 
Description 251-264
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 1 and 2 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, 1H-NMR,
and 13C-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 1Aii and 1Aiii are showing the
minimum inhibition against MCF-7 with the IC50 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 (IC50 = 42.66±2.19 μM).
 
Date 2023-03-17T07:14:37Z
2023-03-17T07:14:37Z
2023-03
 
Type Article
 
Identifier 2583-1321 (Online); 0019-5103 (Print)
http://nopr.niscpr.res.in/handle/123456789/61534
https://doi.org/10.56042/ijc.v62i3.72060
 
Language en
 
Publisher NIScPR-CSIR,India
 
Source IJC Vol.62(03) [Mar 2023]