Molecular docking, synthesis and anticancer activity of thiosemicarbazone derivatives against MCF-7 human breast cancer cell line

Life Sciences ◽  
2021 ◽  
pp. 119305
Author(s):  
Belay Zeleke Sibuh ◽  
Sonia Khanna ◽  
Pankaj Taneja ◽  
Paratpar Sarkar ◽  
Neetu Kumra Taneja
2020 ◽  
Author(s):  
Belay Zeleke Sibuh ◽  
Pankaj Taneja ◽  
Sonia Khanna

AbstractBackground/AimBreast cancer is one of the world’s leading cause of deaths in women. This study evaluated the in-vitro anticancer activity of different thiosemicarbazones (HacTSc, HSTsc, 3-MBTSc, 4-NBTSc and 4-HBTSc) against MCF-7 human breast cancer cell line and MCF-10 normal cell.Materials and MethodsThe ligands were prepared and characterized by UV vis, IR, 1H NMR. MTT assay was used to determine cell viability. Then data were analyzed using two-way ANOVA with Tukey post-hoc test. Result: The ligands have IC50 value ranging from 2.271µg/ml to 7.081µg/ml. Acetone thiosemicarbazone and 3-Methoxybenzaldehyde thiosemicarbazone, were identified as the most potent against MCF-7 breast cancer cells with IC50 value of 2.271µg/ml and 2.743µg/ml respectively. Whereas 4-Nitrobenzaldehyde thiosemicarbazone was the least potent. Also, the IC50 of the normal MCF-10 cell indicated their activity were selective. Conclusion: The activity of the ligands were dose, position and substituents dependent. Acetone thiosemicarbazone and 3-Methoxybenzaldehyde thiosemicarbazone are promising anticancer agents for further study.


2014 ◽  
Vol 21 (9) ◽  
pp. 1160-1170 ◽  
Author(s):  
Dharmendra Yadav ◽  
Komal Kalani ◽  
Abhishek Singh ◽  
Feroz Khan ◽  
Santosh Srivastava ◽  
...  

1992 ◽  
Vol 292 (1) ◽  
pp. 136-140 ◽  
Author(s):  
Ryuji Kitamura ◽  
Keiko Sato ◽  
Minoru Sawada ◽  
Susumu Itoh ◽  
Mitsukazu Kitada ◽  
...  

2002 ◽  
Vol 129 (1-2) ◽  
pp. 55-63 ◽  
Author(s):  
Christel M Olsen ◽  
Elise T.M Meussen-Elholm ◽  
Jørn A Holme ◽  
Jan K Hongslo

2021 ◽  
Vol 66 (1) ◽  
pp. 65-71
Author(s):  
Hung Nguyen Phi ◽  
Toan Tran Quoc ◽  
Tuan Nguyen Anh ◽  
Vy Trinh Ngoc Thao ◽  
Yen Ngo Thi Ngoc ◽  
...  

Three alkaloids (named rutaecarpine (1), evodiamine (2), schinifoline (3) and one phenylpropanoid, integrifoliodiol (4)) have been isolated from the EtOAc extract of the fruits of Tetradium ruticarpum (A. Juss.) T. G. Hartley collected in Lang Son province. Their structures have been identified by using 1D and 2D NMR spectroscopies. All four compounds were tested for their cytotoxicity against the human breast cancer cell line (MCF-7) and tamoxifen-resistant breast cancer cell line (MCF\TAMR). The results showed that rutaecarpine (1) inhibited the growth of MCF7 and MCF\TAMR with its IC50 values of 41.2 and 64.6 µM, respectively. In addition, compounds 1, 2, and 4 showed moderate activity toward MCF-7 cell line.


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