Diversity-Oriented Synthesis of Functionalized Imidazopyridine Analogues with Anti-Cancer Activity through a Transition-Metal Free, One-pot Cascade Reaction

2018 ◽  
Vol 360 (19) ◽  
pp. 3655-3661 ◽  
Author(s):  
Gui-Ting Song ◽  
Nicholas McConnell ◽  
Zhong-Zhu Chen ◽  
Xiao-Fang Yao ◽  
Jiu-Hong Huang ◽  
...  
Keyword(s):  
Transition Metal ◽  
Cascade Reaction ◽  
One Pot ◽  
Diversity Oriented Synthesis ◽  
Metal Free ◽  
Anti Cancer ◽  
Cancer Activity

Stereoselective three-component cascade synthesis of α-substituted 2,4-dienamides from gem-difluorochloro ethanes

2019 ◽  
Vol 55 (95) ◽  
pp. 14355-14358
Author(s):  
Shyamsundar Das ◽  
Nakeun Ko ◽  
Eunsung Lee ◽  
Sang Eun Kim ◽  
Byung Chul Lee
Keyword(s):  
Transition Metal ◽  
Claisen Rearrangement ◽  
Cascade Reaction ◽  
One Pot ◽  
Metal Free

Herein, we describe a new transition metal-free Claisen rearrangement for the synthesis of α-substituted 2,4-dienamide. This one-pot, stereoselective three-component cascade reaction affords various polysubstituted 2,4-dienamides in good yields.

One-pot transition-metal-free cascade synthesis of thieno[2,3-c]coumarins from chromones

RSC Advances ◽  
2016 ◽  
Vol 6 (106) ◽  
pp. 103895-103898 ◽  
Author(s):  
Yuhong Yang ◽  
Xueyu Qi ◽  
Ruiling Liu ◽  
Qian He ◽  
Chunhao Yang
Keyword(s):  
Transition Metal ◽  
Cascade Reaction ◽  
Free Base ◽  
One Pot ◽  
Metal Free

A one-pot transition-metal-free, base-mediated synthesis of a novel series of functionalized thieno[2,3-c]coumarins has been developed through a cascade reaction from chromones.

Facile synthesis of 4-quinolone derivatives via one-pot cascade reaction under transition-metal-free conditions

2015 ◽  
Vol 56 (24) ◽  
pp. 3777-3781 ◽  
Author(s):  
Chao Huang ◽  
Jia-Hui Guo ◽  
Huang-Mei Fu ◽  
Ming-Long Yuan ◽  
Li-Juan Yang
Keyword(s):  
Transition Metal ◽  
Cascade Reaction ◽  
Facile Synthesis ◽  
One Pot ◽  
Metal Free ◽  
Quinolone Derivatives

One-pot synthesis of natural-product inspired spiroindolines with anti-cancer activities

2022 ◽  
Author(s):  
Shiqiang Li ◽  
Wei Yan ◽  
Liu-Jun He ◽  
Ming Zhang ◽  
Dianyong Tang ◽  
...  
Keyword(s):  
Natural Product ◽  
Cascade Reaction ◽  
One Pot ◽  
Metal Free ◽  
One Pot Synthesis ◽  
Anti Cancer

A post-Ugi/diastereoselective cascade reaction was developed to construct naturally existing spiroindolines via a facile and metal-free one-pot protocol. During the construction, a new C-C bond was formed through a selective...

ChemInform Abstract: Facile Synthesis of 4-Quinolone Derivatives via One-Pot Cascade Reaction under Transition-Metal-Free Conditions.

ChemInform ◽  
2015 ◽  
Vol 46 (39) ◽  
pp. no-no
Author(s):  
Chao Huang ◽  
Jia-Hui Guo ◽  
Huang-Mei Fu ◽  
Ming-Long Yuan ◽  
Li-Juan Yang
Keyword(s):  
Transition Metal ◽  
Cascade Reaction ◽  
Facile Synthesis ◽  
One Pot ◽  
Metal Free ◽  
Quinolone Derivatives

A metal-free radical cascade reaction of phosphine oxides with 2-aryloxy phenylacetylenes to assemble diphosphonyl xanthene derivatives

2021 ◽  
Author(s):  
Tao Fan ◽  
Yan Liu ◽  
Caina Jiang ◽  
Yanli Xu ◽  
Yan-Yan Chen
Keyword(s):  
Free Radical ◽  
Transition Metal ◽  
Cascade Reaction ◽  
Phosphine Oxides ◽  
Metal Free ◽  
Mild Conditions ◽  
Xanthene Derivatives ◽  
Reaction Proceeds ◽  
Radical Cascade

A radical cascade reaction of 2-aryloxy phenylacetylene with phosphine oxides promoted by K2S2O8 was developed, provided diphosphonyl xanthenes as products. This reaction proceeds under transition metal-free and mild conditions with...

scholarly journals An entry to 2-(cyclobut-1-en-1-yl)-1H-indoles through a cyclobutenylation/deprotection cascade

2021 ◽  
Author(s):  
Philipp Natho ◽  
Zeyu Yang ◽  
Lewis Allen ◽  
Juliette Rey ◽  
Andrew J P White ◽  
...  
Keyword(s):  
Transition Metal ◽  
One Pot ◽  
Metal Free ◽  
Mild Conditions

A transition-metal-free strategy for the synthesis of 2-(cyclobut-1-en-1-yl)-1H-indoles under mild conditions is described herein. A series of substituted 2-(cyclobut-1-en-1-yl)-1H-indoles are accessed by a one-pot cyclobutenylation/deprotection cascade from N-Boc protected indoles....

ChemInform Abstract: Transition Metal Free Intramolecular S-Arylation: One-Pot Synthesis of Thiochromen-4-ones.

ChemInform ◽  
2014 ◽  
Vol 45 (13) ◽  
pp. no-no
Author(s):  
T. A. Jenifer Vijay ◽  
Kebbahalli N. Nandeesh ◽  
Goravanahalli M. Raghavendra ◽  
Kanchugarakoppal S. Rangappa ◽  
Kempegowda Mantelingu
Keyword(s):  
Transition Metal ◽  
One Pot ◽  
Metal Free ◽  
One Pot Synthesis

One Pot Synthesis, Quantum Chemical Stimulation and Anticancer Evaluation of Some New 8-Azacoumarin Derivatives

2021 ◽  
Author(s):  
Sameh Rizk ◽  
Mohamed Megahed ◽  
Monda Badawy ◽  
Mohamed Aly
Keyword(s):  
Liver Cancer ◽  
Cell Lines ◽  
Analytical Data ◽  
Liver Carcinoma ◽  
One Pot ◽  
Reference Drug ◽  
One Pot Synthesis ◽  
Ic50 Value ◽  
Anti Cancer ◽  
Cancer Activity

Abstract New anticancer agents are highly needed to overcome cancer cell resistance. Synthesis of newly pyrazole, derivatives via heterocyclic ring opening of azacoumarin promoted with grinding and ultrasonic reaction conditions. Efficient solvent less one pot synthesis can be well progressed to afford the good yield of new heterocyclic products that were characterized by IR, 1H-NMR, MS and micro-analytical data. Anticancer evaluation for the synthesized compounds exhibited good cytotoxiciy. The anti-liver cancer activity of all compounds was screened in vitro against hepatocellular carcinoma (HCC) cell lines (HepG-2) by viability assay. The synthesized compounds were evaluated for their anticancer activity and found to exhibit promising activities. All new compounds were tested for possible anti-cancer activity against HepG-2 cell lines in comparison to the reference drug doxorubicin (DOX). Compound 8 was the most active against the liver carcinoma cell line (HepG-2) giving promising half-maximal inhibitory concentration (IC50) value of 27.5 ± 1.3 μg/mL, compared with DOX with IC50 value of 0.36 ± 0.02 μg/mL. However it has weak cytotoxic effects against normal rat hepatocytes with 50% cytotoxic concentration (CC50) = 1820.5 µg/ml (= > 500 µg/ml). Compound 8 was selected to be tested in combination with ionizing gamma radiation. Gene expression levels of the cell cycle inhibitor p21 and caspase-3 was quantified. As well as, Oxidative stress was quantified by measuring the concentration of malondialdehyde (MDA), and antioxidant activity of reduced gluthatione (GSH). This study concluded that the new derivative of the azacomarin compound has an effective anti-cancer effect and it was found that using the new compound with ionizing radiation at a dose of 8 Gy improves the effectiveness of the compound on liver cancer cells.

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