scholarly journals Synthesis and in vitro anti breast cancer activity of some novel 1,5-benzothiazepine derivatives

2012 ◽  
Vol 77 (6) ◽  
pp. 725-731 ◽  
Author(s):  
K.L. Ameta ◽  
Nitu Rathore ◽  
Biresh Kumar

The title compounds 3a-j, substituted 1,5-benzothiazepines were synthesized by the condensation of variously substituted chalcones 1 and 2- aminothiophenol 2 via conventional as well as non-conventional inorganic solid support microwave irradiation methods. The non-conventional protocol offers several advantages such as simple procedure, fast reaction rate, mild reaction conditions and improved yields compared to conventional methods. The structures of the products 3a-j were established by elemental analysis, FTIR, 1H-NMR, 13C-NMR and mass spectroscopic studies. The synthesized compounds have also been evaluated for the cytotoxicity against human breast cancer cell line MDA-MB-435 with some exhibiting in vitro anti-breast cancer activities.

PLoS ONE ◽  
2013 ◽  
Vol 8 (6) ◽  
pp. e64388 ◽  
Author(s):  
Chanel E. Smart ◽  
Brian J. Morrison ◽  
Jodi M. Saunus ◽  
Ana Cristina Vargas ◽  
Patricia Keith ◽  
...  

2011 ◽  
Vol 26 (1) ◽  
pp. 105-111 ◽  
Author(s):  
Ayfer Yurt Kilcar ◽  
F. Zumrut Biber Muftuler ◽  
Perihan Unak ◽  
Cigir Biray Avci ◽  
Cumhur Gunduz

Breast Cancer ◽  
1999 ◽  
Vol 6 (2) ◽  
pp. 87-92 ◽  
Author(s):  
Akihiko Suto ◽  
Nitin T. Telang ◽  
Hirokazu Tanino ◽  
Toshio Takeshita ◽  
Harumi Ohmiya ◽  
...  

Molecules ◽  
2020 ◽  
Vol 25 (18) ◽  
pp. 4250
Author(s):  
Vera M. S. Isca ◽  
Joana Andrade ◽  
Ana Sofia Fernandes ◽  
Paulo Paixão ◽  
Clara Uriel ◽  
...  

The antimicrobial evaluation of twelve natural and hemisynthetic isopimarane diterpenes are reported. The compounds were evaluated against a panel of Gram-positive bacteria, including two methicillin-resistant Staphylococcus aureus (MRSA) strains and one vancomycin-resistant Enterococcus (VRE) strain. Only natural compounds 7,15-isopimaradien-19-ol (1) and 19-acetoxy-7,15-isopimaradien-3β-ol (6) showed promising results. Isopimarane (1) was the most active, showing MIC values between 6.76 µM against S. aureus (ATCC 43866) and 216.62 µM against E. faecalis (FFHB 427483) and E. flavescens (ATCC 49996). Compound (6) showed moderated activity against all tested microorganisms (MIC between value 22.54 and 45.07 µM). These compounds were found to be active against the methicillin-sensitive strains of S. aureus (CIP 106760 and FFHB 29593), showing MIC values of 13.55 (1) and 22.54 (6) µM. Both compounds were also active against vancomycin-resistant E. faecalis (ATCC 51299) (MIC values of 54.14 and 45.07 µM, respectively). In addition, the cytotoxicity of nine compounds 7,15-isopimaradien-3β,19-diol (2); mixture: 15-isopimarene-8β-isobutyryloxy-19-ol and 15-isopimarene-8β-butyryloxy-19-ol (3); 3β-acetoxy-7,15-isopimaradiene-19-ol (5); 19-acetoxy-7,15-isopimaradiene-3β-ol (6); 3β,19-diacetoxy-7,15-isopimaradiene (8); 15-isopimarene-8β,19-diol (9); 19-O-β-d-glucopyranoside-7,15-isopimaradiene (10); lagascatriol-16-O-β-d-glucopyranoside (11) and lagascatriol-16-O-α-d-mannopyranoside (12) was evaluated in the human breast cancer cell line MDA-MB-231. Isopimarane (2) was the only compound showing some cytotoxicity. The IC50 value of compound (2) was 15 µM, suggesting a mild antiproliferative activity against these breast cancer cells.


INDIAN DRUGS ◽  
2019 ◽  
Vol 56 (12) ◽  
pp. 28-31
Author(s):  
D Nikam ◽  
◽  
S. Tanvar ◽  
A Kute ◽  
S Lokhande ◽  
...  

A series of dihydropyrimidone derivatives was synthesized by an efficient, simple and solvent less green method by using Beginelli reaction. Various aromatic aldehydes, urea and ethyl acetoacetate were refluxed for a few hours and the reaction monitored by periodic TLC (hexane: ethyl acetate 6:4 v/v) and products are purified by recrystallization, with characterization by FTIR, 1H NMR. All the purified compounds were subjected to evaluatation by in vitro human breast cancer cell line MDA-MB-231 and MCF-7. Compound I-k was found to be moderately active against MCF-7 with GI 50 value of -4.38.


Sign in / Sign up

Export Citation Format

Share Document