ChemInform Abstract: Microwave-Assisted One-Pot Synthesis of Steroid-Quinoline Hybrids and an Evaluation of Their Antiproliferative Activities on Gynecological Cancer Cell Lines.

ChemInform ◽  
2016 ◽  
Vol 47 (30) ◽  
Author(s):  
Adam Baji ◽  
Andras Gyovai ◽  
Janos Woelfling ◽  
Renata Minorics ◽  
Imre Ocsovszki ◽  
...  
RSC Advances ◽  
2016 ◽  
Vol 6 (33) ◽  
pp. 27501-27516 ◽  
Author(s):  
Ádám Baji ◽  
András Gyovai ◽  
János Wölfling ◽  
Renáta Minorics ◽  
Imre Ocsovszki ◽  
...  

Steroidal and nonsteroidal ring-fused quinolines were efficiently synthesized under microwave conditions and their antiproliferative activities were investigated.


2012 ◽  
Vol 9 (1) ◽  
pp. 48-57 ◽  
Author(s):  
Joanna Matysiak ◽  
Monika M. Karpińska ◽  
Andrzej Niewiadomy ◽  
Joanna Wietrzyk ◽  
Dagmara Kłopotowska

2019 ◽  
Vol 16 (2) ◽  
pp. 117-121 ◽  
Author(s):  
Peipei Han ◽  
Wenhua Zhou ◽  
Mingxia Chen ◽  
Qiuan Wang

A series of eight polymethoxychalcone Mannich base derivatives 2a-2h was synthesized via the microwave-assisted Mannich reaction of natural product 2'-hydroxy-3,4,4',5,6'-pentamethoxychalcone (1) with various secondary amines and formaldehyde. Compared to conventional heating method (80°C), the microwave-assisted method (700W, 65°C) is efficient with short reaction time (0.5-1 h) and good yields (74-88%). The antiproliferative activities of eight Mannich base derivatives were evaluated in vitro on a panel of three human cancer cell lines (Hela, HCC1954 and SK-OV-3) by CCK-8 assay. The results showed that all of the Mannich base derivatives exhibited potential antiproliferative activities on tested cancer cell lines with the IC50 values of 9.13-48.51 µM. Some active compounds exhibited more activity as compared to positive control cis-Platin. Among them, compound 2b revealed to have the strongest antiproliferative activity against all the three cancer cell lines with IC50 values ranging from 9.13 to 11.24 µM.


2018 ◽  
Vol 11 (3) ◽  
pp. 264-274 ◽  
Author(s):  
Huda R. M. Rashdan ◽  
Sobhi M. Gomha ◽  
Marwa S. El-Gendey ◽  
Maher A. El-Hashash ◽  
Abdel Mohsen M. Soliman

2018 ◽  
Vol 15 (2) ◽  
pp. 160-168 ◽  
Author(s):  
Chekuri Sharmila Rani ◽  
Meda Haritha ◽  
Mandava V. Basaveswara Rao ◽  
Manojit Pal

Background: We report the design, synthesis and evaluation of a series of 4-biaryl substituted 2-amino benzo[h]chromene derivatives as potential cytotoxic agents. Methods: The one-pot synthesis of this class of compounds was carried out under ultrasound irradiation using an MCR involving Pd/C-catalyzed Suzuki-Miyaura coupling as a key step. Result and Conclusion: Several of these compounds showed promising cytotoxicities when tested against cancer cell lines but no or little effects on non-cancerous cell lines.


Plants ◽  
2021 ◽  
Vol 10 (2) ◽  
pp. 368
Author(s):  
Elda M. Melchor Martínez ◽  
Luisaldo Sandate-Flores ◽  
José Rodríguez-Rodríguez ◽  
Magdalena Rostro-Alanis ◽  
Lizeth Parra-Arroyo ◽  
...  

Cacti fruits are known to possess antioxidant and antiproliferative activities among other health benefits. The following paper evaluated the antioxidant capacity and bioactivity of five clarified juices from different cacti fruits (Stenocereus spp., Opuntia spp. and M. geomettizans) on four cancer cell lines as well as one normal cell line. Their antioxidant compositions were measured by three different protocols. Their phenolic compositions were quantified through high performance liquid chromatography and the percentages of cell proliferation of fibroblasts as well as breast, prostate, colorectal, and liver cancer cell lines were evaluated though in vitro assays. The results were further processed by principal component analysis. The clarified juice from M. geomettizans fruit showed the highest concentration of total phenolic compounds and induced cell death in liver and colorectal cancer cells lines as well as fibroblasts. The clarified juice extracted from yellow Opuntia ficus-indica fruit displayed antioxidant activity as well as a selective cytotoxic effect on a liver cancer cell line with no toxic effect on fibroblasts. In conclusion, the work supplies evidence on the antioxidant and antiproliferative activities that cacti juices possess, presenting potential as cancer cell proliferation preventing agents.


Molecules ◽  
2021 ◽  
Vol 26 (20) ◽  
pp. 6305
Author(s):  
Abdullah Mohammed Al-Majid ◽  
M. Ali ◽  
Mohammad Shahidul Islam ◽  
Saeed Alshahrani ◽  
Abdullah Saleh Alamary ◽  
...  

A new series of di-spirooxindole analogs, engrafted with oxindole and cyclohexanone moieties, were synthesized. Initially, azomethine ylides were generated via reaction of the substituted isatins 3a–f (isatin, 3a, 6-chloroisatin, 3b, 5-fluoroisatin, 3c, 5-nitroisatin, 3d, 5-methoxyisatin, 3e, and 5-methylisatin, 3f, and (2S)-octahydro-1H-indole-2-carboxylic acid 2, in situ azomethine ylides reacted with the cyclohexanone based-chalcone 1a–f to afford the target di-spirooxindole compounds 4a–n. This one-pot method provided diverse structurally complex molecules, with biologically relevant spirocycles in a good yields. All synthesized di-spirooxindole analogs, engrafted with oxindole and cyclohexanone moieties, were evaluated for their anticancer activity against four cancer cell lines, including prostate PC3, cervical HeLa, and breast (MCF-7, and MDA-MB231) cancer cell lines. The cytotoxicity of these di-spirooxindole analogs was also examined against human fibroblast BJ cell lines, and they appeared to be non-cytotoxic. Compound 4b was identified as the most active member of this series against prostate cancer cell line PC3 (IC50 = 3.7 ± 1.0 µM). The cyclohexanone engrafted di-spirooxindole analogs 4a and 4l (IC50 = 7.1 ± 0.2, and 7.2 ± 0.5 µM, respectively) were active against HeLa cancer cells, whereas NO2 substituted isatin ring and meta-fluoro-substituted (2E,6E)-2,6-dibenzylidenecyclohexanone containing 4i (IC50 = 7.63 ± 0.08 µM) appeared to be a promising agent against the triple negative breast cancer MDA-MB231 cell line. To explore the plausible mechanism of anticancer activity of di-spirooxindole analogs, molecular docking studies were investigated which suggested that spirooxindole analogs potentially inhibit the activity of MDM2.


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