Synthesis of imidazo[2,1-b][1,3,4]thiadiazole–chalcones as apoptosis inducing anticancer agents

MedChemComm ◽  
2014 ◽  
Vol 5 (11) ◽  
pp. 1718-1723 ◽  
Author(s):  
Ahmed Kamal ◽  
Vangala Santhosh Reddy ◽  
Karnewar Santosh ◽  
G. Bharath Kumar ◽  
Anver Basha Shaik ◽  
...  

A library of imidazothiadiazole–chalcone conjugates were synthesised and investigated for their cytotoxic activity against various human cancer cell lines. Some of the tested compounds like 7a, 7b, 11a and 11b exhibited promising anticancer activity.

2020 ◽  
Vol 17 (5) ◽  
pp. 345-351
Author(s):  
Syndla Premalatha ◽  
G. Rambabu ◽  
Islavathu Hatti ◽  
Dittakavi Ramachandran

A new series of 3-(3,4,5-trimethoxyphenyl)-5-(2-(5-arylbenzo[b]thiophen-3-yl)oxa zol-5- yl)isoxazole derivatives were designed and synthesized. All these derivatives were evaluated for their anticancer activity against various human cancer cell lines such as MCF-7 (breast cancer), A549 (lung cancer), DU-145 (prostate cancer) and MDA MB-231 (breast cancer)-four human cancer cell lines by using MTT assay. Here, etoposide was used as a standard reference drug and most of the compounds were exhibited good anticancer activity with respect to cell lines. Among all compounds, five compounds 11b, 11c, 11f, 11i and 11j showed more potent activity than standard drug, in which, compound 11f was the most promising compound.


2013 ◽  
Vol 6 (2) ◽  
pp. 246-252 ◽  
Author(s):  
Justin T. Fischedick ◽  
Milica Pesic ◽  
Ana Podolski-Renic ◽  
Jasna Bankovic ◽  
Ric C.H. de Vos ◽  
...  

Molecules ◽  
2020 ◽  
Vol 25 (4) ◽  
pp. 849 ◽  
Author(s):  
Florence N. Mbaoji ◽  
Steven Behnisch-Cornwell ◽  
Adaobi C. Ezike ◽  
Chukwuemeka S. Nworu ◽  
Patrick J. Bednarski

In western Africa ethnomedicine, Lannea barteri Oliv. (Anacardiaceae) is believed to have activity against gastrointestinal, neurological and endocrine diseases. Previous studies on this plant have revealed antimicrobial, anticholinestrase, anticonvulsant, antioxidant and anti-inflammatory activities. However, the anticancer potential of L. barteri has not been studied to date. The aim of this study was to evaluate the anticancer potential of hot and cold extracts and silica gel column chromatographic fractions of L. barteri leaf and stem bark. The extracts and fractions were tested for anticancer activity by using the crystal violet cell proliferation assay on four adherent human carcinoma cell lines—5637 (bladder), KYSE 70 (oesophagus), SiSo (cervical) and HepG2 (hepatic). The inhibitory concentration (IC50) of fractions IH, 1I, 2E and 2F were: 3.75 ± 1.33, 3.88 ± 2.15, 0.53 ± 0.41, and 0.42 ± 0.45 µg/mL against KYSE 70 and 1.04 ± 0.94, 2.69 ± 1.17, 2.38 ± 3.64, 2.17 ± 1.92 µg/mL against SiSo cell lines respectively. Fraction 2E showed weak apoptotic activity at double the IC50 and some sign of cell cycle arrest in the G2/M phase. Thus, phytoconstituents of L. barteri leaf and stem bark can inhibit the proliferation of cancer cell lines indicating the presence of possible anticancer agents in this plant.


2019 ◽  
Vol 14 (5) ◽  
pp. 1934578X1984413
Author(s):  
Thi Hong Van Nguyen ◽  
Thi Tuyen Tran ◽  
Thi Inh Cam ◽  
Minh Quan Pham ◽  
Quoc Long Pham ◽  
...  

Zanthoxylum nitidum (Roxb.) DC (Rutaceae) is a traditional medicine used for the treatment of various diseases like toothache, gingivitis, fever, colic vomiting, diarrhea, and cholera. Three new alkaloids, zanthocadinanine C (1), 7-methoxy-8-demethoxynitidine (2), and zanthonitiside I (3) were isolated from the stems and twigs of Z. nitidum. Their structures were determined on the basis of extensive spectroscopic, including 1-dimensional and 2-dimensional nuclear magnetic resonance and mass spectroscopy data. Compounds 1–3 were evaluated for cytotoxic activity against 5 human cancer cell lines, KB, MCF-7, LNCaP, HepG-2, and LU-1. Compound 2 showed significant cytotoxic activity against all tested human cancer cell lines with IC50 values ranging from 10.3 to 12.6 µM.


1996 ◽  
Vol 88 (11) ◽  
pp. 734-741 ◽  
Author(s):  
Scott H. Kaufmann ◽  
David Peereboom ◽  
Christopher A. Buckwalter ◽  
Phyllis A. Svingen ◽  
Louise B. Grochow ◽  
...  

2004 ◽  
Vol 203 (1) ◽  
pp. 59-69 ◽  
Author(s):  
Krzysztof Polkowski ◽  
Joanna Popiołkiewicz ◽  
Piotr Krzeczyński ◽  
Jan Ramza ◽  
Wiesław Pucko ◽  
...  

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