scholarly journals Synthesis and Biological Evaluation of Febrifugine Analogues

2014 ◽  
Vol 9 (12) ◽  
pp. 1934578X1400901
Author(s):  
Huong Doan Thi Mai ◽  
Giang Vo Thanh ◽  
Van Hieu Tran ◽  
Van Nam Vu ◽  
Van Loi Vu ◽  
...  

A series of febrifugine analogues were designed and synthesized. Antimalarial activity evaluation of the synthetic compounds indicated that these derivatives had a strong inhibition against both chloroquine-sensitive and -resistant Plasmodium falciparum parasites. Many of them were found to be more active than febrifugine hydrochloride. The tested analogues had also a significant cytotoxicity against four cancer cell lines (KB, MCF7, LU1 and HepG2). Among the synthetic analogues, two compounds 17b and 17h displayed a moderate cytotoxicity while they exhibited a remarkable antimalarial activity.

MedChemComm ◽  
2017 ◽  
Vol 8 (5) ◽  
pp. 1000-1006 ◽  
Author(s):  
Ibrahim Bin Sayeed ◽  
V. Lakshma Nayak ◽  
Mohd Adil Shareef ◽  
Neeraj Kumar Chouhan ◽  
Ahmed Kamal

A library of imidazopyridine–propenone conjugates (8a–8u) were synthesized and evaluated for their antitumor activity against four human cancer cell lines.


RSC Advances ◽  
2018 ◽  
Vol 8 (62) ◽  
pp. 35744-35752 ◽  
Author(s):  
Marta Czarnecka ◽  
Marta Świtalska ◽  
Joanna Wietrzyk ◽  
Gabriela Maciejewska ◽  
Anna Gliszczyńska

A series of eight novel phosphatidylcholines containing CA or 3-OMe-CA acids (3a-b, 5a-b, 9a-b, 10a-b) at sn-1 and/or sn-2 positions were synthesized and tested for their antiproliferative activity against selected cancer cell lines.


MedChemComm ◽  
2016 ◽  
Vol 7 (4) ◽  
pp. 636-645 ◽  
Author(s):  
Hongtao Du ◽  
Hongling Gu ◽  
Na Li ◽  
Junru Wang

A series of novel bivalent β-carbolines were synthesized and evaluated for their anti-proliferative activities on a panel of cancer cell lines, apoptosis induction and cell cycle effects.


2015 ◽  
Vol 13 (5) ◽  
pp. 1404-1414 ◽  
Author(s):  
Pannala Padmaja ◽  
Garikapati Koteswara Rao ◽  
Adisherla Indrasena ◽  
Basireddy V. Subba Reddy ◽  
Nibedita Patel ◽  
...  

A series of novel pyrano[3,2-c]carbazole derivatives have been synthesized and antiproliferative activity of the derivatives were investigated on various cancer cell lines.


Author(s):  
Guoyi Yan ◽  
Jiang Luo ◽  
Xuan Han ◽  
Wenjuan Zhang ◽  
Chunlan Pu ◽  
...  

BACKGROUND: : Coumarin structures were widely employed in anti-cancer drug design. Herein we focused on the modifications of C4 and C6 positions on coumarin scaffold to get novel anti-cancer agents. OBJECTIVE: The objective of the current work was the synthesis and biological evaluation of a series of 4, 6-coumarin derivatives to get novel anticancer agents. METHODS: Thirty-seven coumarin derivatives were designed and synthesized, the antiproliferative activity of the compounds were evaluated against human cancer cell lines and non-cancerous cells by MTT assay. The bioactivities and underling mechanisms of active molecules were studied and the ADMET characters were predicted. RESULTS: Among the compounds, 4-phydroxy phenol-6-pinacol borane coumarin (25) exhibited a promising anti-cancer activity to cancer cell lines in dose-dependent manner and the toxicity to normal cells was low. The mechanism of action was observed through inducing G2/M phase arrest and apoptosis which was further confirmed via western blot. In silico ADMET prediction revealed that compound 25 is a drug-like small molecule with a favorable safety profile. CONCLUSION: The findings in this work may give vital information for further development of 6-pinacol borane coumarin derivatives as novel anti-cancer agents.


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