scholarly journals Synthesis of Alicyclic 2-Methylenethiazolo[2,3-b]quinazolinone Derivatives via Base-Promoted Cascade Reactions

Synthesis ◽  
2021 ◽  
Author(s):  
Márta Palkó ◽  
Mohamed El Haimer ◽  
Tünde Faragó ◽  
Zsuzsanna Schelz ◽  
István Zupkó
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
Carbon Disulfide ◽  
Cascade Reactions ◽  
Diels Alder ◽  
Ring Closure ◽  
Reaction Proceeds ◽  
Quinazolinone Derivatives ◽  
Norbornene Derivatives ◽  
Antiproliferative Activities

AbstractThe synthesis of alicyclic 2-methylenethiazolo[2,3-b]quinazo­l­inones is performed via base-promoted cascade reactions, starting from either alicyclic β-amino propargylamides using carbon disulfide, or from alicyclic ethyl 2-isothiocyanatocarboxylates by addition of propargylamine. In both cases the cascade reaction proceeds by way of a favoured 5-exo-dig process during the second ring closure, as confirmed by full NMR spectroscopic assignments. Moreover, a high-yielding retro­-Diels–Alder (RDA) reaction is performed on the norbornene derivatives leading to 2-methylene-2H-thiazolo[3,2-a]pyrimidin-5(3H)-ones. The obtained compounds exert modest antiproliferative activities against a panel of human gynaecological cancer cell lines.

Microwave-assisted Synthesis of Polymethoxychalcone Mannich Bases and Their Antiproliferative Activity

2019 ◽  
Vol 16 (2) ◽  
pp. 117-121 ◽  
Author(s):  
Peipei Han ◽  
Wenhua Zhou ◽  
Mingxia Chen ◽  
Qiuan Wang
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
Antiproliferative Activity ◽  
Mannich Base ◽  
Cancer Cell Lines ◽  
Secondary Amines ◽  
Conventional Heating ◽  
Microwave Assisted ◽  
Ic50 Values ◽  
Antiproliferative Activities

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.

scholarly journals Underutilized Mexican Plants: Screening of Antioxidant and Antiproliferative Properties of Mexican Cactus Fruit Juices

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 ◽  
...  
Keyword(s):  
Cell Proliferation ◽  
Liver Cancer ◽  
Cell Line ◽  
Cell Lines ◽  
Cancer Cell ◽  
Cancer Cell Lines ◽  
In Vitro Assays ◽  
Total Phenolic ◽  
Liver Cancer Cell ◽  
Antiproliferative Activities

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.

scholarly journals Correction: Colchicine metallocenyl bioconjugates showing high antiproliferative activities against cancer cell lines

2018 ◽  
Vol 47 (8) ◽  
pp. 2822-2822 ◽  
Author(s):  
Karolina Kowalczyk ◽  
Andrzej Błauż ◽  
Wojciech M. Ciszewski ◽  
Anna Wieczorek ◽  
Błażej Rychlik ◽  
...  
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
Cancer Cell Lines ◽  
Dalton Trans ◽  
Antiproliferative Activities

Correction for ‘Colchicine metallocenyl bioconjugates showing high antiproliferative activities against cancer cell lines’ by Karolina Kowalczyk et al., Dalton Trans., 2017, 46, 17041–17052.

scholarly journals Synthesis and Biological Activity of 2-Arylidene-N-(quinolin-6-yl)hydrazine-1-carboxamides

2020 ◽  
Vol 2020 ◽  
pp. 1-9
Author(s):  
Shengxian Zhao ◽  
Yin Cao ◽  
Zhenzhen Cui ◽  
Jiayun Zhang ◽  
Zhixiang Pan ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Cell Lines ◽  
Cancer Cell ◽  
Cancer Cell Lines ◽  
Breast Cancer Cell Lines ◽  
Colony Formation Assay ◽  
M Phase ◽  
Antiproliferative Activities ◽  
Mcf 7

A series of 2-arylidene-N-(quinolin-6-yl)hydrazine-1-carboxamides 5a–5o were synthesized and characterized. The synthesized compounds (5a–5o) were screened in vitro against three breast cancer cell lines: SKBR3, MDA-MB-231, and MCF-7 cancer cell lines by the MTT assay. According to MTT results, compounds 5k and 5l showed better antiproliferative activities over MCF-7 cell lines with IC50 values of 8.50 and 12.51 μM. Colony formation assay indicated 5k/5l treatment obviously inhibited the growth of MCF-7 cells and 5k/5l-induced cell cycle was arrested in the G2-M phase. Moreover, 5k/5l significantly increased the level of cleaved PARP and induced the apoptosis in MCF-7 cells. In addition, compared to Hela cells, MCF-7 cells were more sensitive to 5k/5l treatment.

Antiproliferative Activities of Parthenolide and Golden Feverfew Extract Against Three Human Cancer Cell Lines

2006 ◽  
Vol 9 (1) ◽  
pp. 55-61 ◽  
Author(s):  
Changqing Wu ◽  
Feng Chen ◽  
James W. Rushing ◽  
Xi Wang ◽  
Hyun-Jin Kim ◽  
...  
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
Human Cancer ◽  
Cancer Cell Lines ◽  
Human Cancer Cell ◽  
Human Cancer Cell Lines ◽  
Antiproliferative Activities

Microwave-assisted one-pot synthesis of steroid–quinoline hybrids and an evaluation of their antiproliferative activities on gynecological cancer cell lines

RSC Advances ◽  
2016 ◽  
Vol 6 (33) ◽  
pp. 27501-27516 ◽  
Author(s):  
Ádám Baji ◽  
András Gyovai ◽  
János Wölfling ◽  
Renáta Minorics ◽  
Imre Ocsovszki ◽  
...  
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
Gynecological Cancer ◽  
Cancer Cell Lines ◽  
One Pot ◽  
Microwave Assisted ◽  
One Pot Synthesis ◽  
Antiproliferative Activities

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

scholarly journals Synthesis and Antiproliferative Activity of Chlorinated Maprotiline Analogues

2020 ◽  
Author(s):  
Mujeeb A. Sultan ◽  
Usama Karama ◽  
Abdulrahman I. Almansour ◽  
Kamal Eldin El-Taher ◽  
Yasser A. Elnakady ◽  
...  
Keyword(s):  
Cell Line ◽  
Cell Lines ◽  
Cancer Cell ◽  
Antiproliferative Activity ◽  
Cancer Cell Lines ◽  
Alder Reaction ◽  
Diels Alder ◽  
Treated Cell ◽  
Diels Alder Reaction

Abstract A novel chlorinated tetracyclic compound 13 of the class ethanoanthracene, as analogue of maprotiline, was prepared via multistep syntheses. The tetracyclic key intermediates 4 and 5 with its [2.2.2] system were built via a Diels-Alder reaction between acrolein and 1,8-dichloroanthracene.The synthesized chlorinated maprotiline analogues 6 , 7 and 13 as well intermediates 4 and 5 exerted antiproliferative activity against cancer cell lines A549 and HepG2 at low micromolar concentrations. In addition, the intermediates 4 and 5 exerted high antiproliferative activity against HCT cell line. Interestingly, the intermediate 4 was the most active against all treated cell lines.

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