- Synthesis of sorafenib analogues incorporating a 1,2,3-triazole ring and cytotoxicity towards hepatocellular carcinoma cell lines
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A series of 1,2,3-triazole-containing Sorafenib analogues, in which the aryl urea moiety of Sorafenib (1) was replaced with a 1,2,3-triazole ring linking a substituted phenoxy fragment, were prepared successfully via Huisgen 1,3-dipolar cycloaddition and
- Palakhachane, Sarinya,Ketkaew, Yuwaporn,Chuaypen, Natthaya,Sirirak, Jitnapa,Boonsombat, Jutatip,Ruchirawat, Somsak,Tangkijvanich, Pisit,Suksamrarn, Apichart,Limpachayaporn, Panupun
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- Enantioselective Palladium-Catalyzed Hydrophosphinylation of Allenes with Phosphine Oxides: Access to Chiral Allylic Phosphine Oxides
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A Pd-catalyzed hydrophosphinylation of alkyl and aryl-oxyallenes with phosphine oxides has been developed for the efficient and rapid construction of a family of chiral allylic phosphine oxides with a diverse range of functional groups. This methodology was further applied in the facile construction of chiral 2H-chromene and later stage functionalization of cholesterol.
- Wang, Jun,Yang, Zhiping
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supporting information
p. 27288 - 27292
(2021/11/17)
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- Water-Tolerant ortho-Acylation of Phenols
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A metal-free, water-tolerant, and one-pot process for ortho-acylation of phenols promoted by the iodine source/hydrogen peroxide system has been developed. This transformation undergoes ether formation, iodocyclization, C-C bond cleavage, and oxidative hydrolysis in a one-step manner, which is supported by control experiments.
- Dong, Shuang-Feng,Gao, Zhi-Yuan,He, Yu,Liu, Xu,Loh, Teck-Peng,Tian, Jie-Sheng,Wu, Peng
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supporting information
p. 6594 - 6598
(2021/09/02)
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- Discovery of a novel series of hDHODH inhibitors with anti-pulmonary fibrotic activities
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Human dihydroorotate dehydrogenase (hDHODH) is a flavin-dependent enzyme essential to pyrimidine de novo biosynthesis, which serves as an attractive therapeutic target for the treatment of autoimmune disorders. A novel series of hDHODH inhibitors was deve
- Lu, Kuan,Zhao, Yanfang,Wu, Guodong,Hu, Hao,Wang, Mingzhong,Gong, Guowei,Jiang, Yuyang
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- Bimetal-Catalyzed Cascade Reaction for Efficient Synthesis of N-Isopropenyl 1,2,3-Triazoles via In-Situ Generated 2-Azidopropenes
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A bimetal-catalyzed cascade reaction for the synthesis of N-isopropenyl 1,2,3-triazoles in high yield is reported. This reaction involves the generation of 2-azidopropenes in situ by C(sp3)-OAr bond cleavage for click reaction and features a broad substrate scope, good functional group tolerance and readily available substrates.
- Liu, Zhenhua,Hao, Wenjing,Liu, Zhixian,Gao, Wen,Zhang, Zhihai,Zhang, Yanan,Li, Xiang,Tong, Lili,Tang, Bo
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supporting information
p. 2149 - 2154
(2019/06/13)
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- 1,4-Substituted Triazoles as Nonsteroidal Anti-Androgens for Prostate Cancer Treatment
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Prostate cancer (PC) is the fifth leading cause of cancer death in men, and the androgen receptor (AR) represents the primary target for PC treatment, even though the disease frequently progresses toward androgen-independent forms. Most of the commerciall
- Ferroni, Claudia,Pepe, Antonella,Kim, Yeong Sang,Lee, Sunmin,Guerrini, Andrea,Parenti, Marco Daniele,Tesei, Anna,Zamagni, Alice,Cortesi, Michela,Zaffaroni, Nadia,De Cesare, Michelandrea,Beretta, Giovanni Luca,Trepel, Jane B.,Malhotra, Sanjay V.,Varchi, Greta
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supporting information
p. 3082 - 3093
(2017/04/21)
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- Discovery of cyclopropyl chromane-derived pyridopyrazine-1,6-dione γ-secretase modulators with robust central efficacy
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Herein we describe the discovery of a novel series of cyclopropyl chromane-derived pyridopyrazine-1,6-dione γ-secretase modulators for the treatment of Alzheimer's disease (AD). Using ligand-based design tactics such as conformational analysis and molecul
- Pettersson, Martin,Johnson, Douglas S.,Rankic, Danica A.,Kauffman, Gregory W.,Am Ende, Christopher W.,Butler, Todd W.,Boscoe, Brian,Evrard, Edelweiss,Helal, Christopher J.,Humphrey, John M.,Stepan, Antonia F.,Stiff, Cory M.,Yang, Eddie,Xie, Longfei,Bales, Kelly R.,Hajos-Korcsok, Eva,Jenkinson, Stephen,Pettersen, Betty,Pustilnik, Leslie R.,Ramirez, David S.,Steyn, Stefanus J.,Wood, Kathleen M.,Verhoest, Patrick R.
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supporting information
p. 730 - 743
(2017/04/27)
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- Synthesis of new generation triazolyl- and isoxazolyl-containing 6-nitro-2,3-dihydroimidazooxazoles as anti-TB agents: In vitro, structure-activity relationship, pharmacokinetics and in vivo evaluation
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The nitroimidazole scaffold has attracted great interest in the last decade, which ultimately led to the discovery of the successful drug Delamanid for multi-drug resistant tuberculosis (MDR-TB). Herein, we report medicinal chemistry on a 6-nitro-2,3-dihy
- Munagala, Gurunadham,Yempalla, Kushalava Reddy,Singh, Samsher,Sharma, Sumit,Kalia, Nitin Pal,Rajput, Vikrant Singh,Kumar, Sunil,Sawant, Sanghapal D.,Khan, Inshad Ali,Vishwakarma, Ram A.,Singh, Parvinder Pal
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supporting information
p. 3610 - 3624
(2015/03/30)
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- Synthesis and biological evaluation of 4-(1,2,3-triazol-1-yl)coumarin derivatives as potential antitumor agents
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In this research, a series of 4-(1,2,3-triazol-1-yl)coumarin conjugates were synthesized and their anticancer activities were evaluated in vitro against three human cancer cell lines, including human breast carcinoma MCF-7 cell, colon carcinoma SW480 cell and lung carcinoma A549 cell. To increase the biological potency, structural optimization campaign was conducted focusing on the C-4 position of 1,2,3-triazole and the C-6, C-7 positions of coumarin. In addition, to further evaluate the role of 1,2,3-triazole and coumarin for antiproliferative activity, 9 compounds possessing 4-(piperazin-1-yl)coumarin framework and 3 derivatives baring quinoline core were also synthesized. By MTT assay in vitro, most of the compounds display attractive antitumor activities, especially 23. Further flow cytometry assays demonstrate that compound 23 exerts the antiproliferative role through arresting G2/M cell-cycle and inducing apoptosis.
- Zhang, Wenjuan,Li, Zhi,Zhou, Meng,Wu, Feng,Hou, Xueyan,Luo, Hao,Liu, Hao,Han, Xuan,Yan, Guoyi,Ding, Zhenyu,Li, Rui
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supporting information
p. 799 - 807
(2014/02/14)
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- Natural products in parallel synthesis: Triazole libraries of nonactic acid
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The synthesis of a library of nonactic acid-derived triazoloamide derivatives and their evaluation as antimicrobial agents is described.
- Luesse, Sarah B.,Wells, Gregg,Nayek, Abhijit,Smith, Adrienne E.,Kusche, Brian R.,Bergmeier, Stephen C.,McMills, Mark C.,Priestley, Nigel D.,Wright, Dennis L.
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body text
p. 3946 - 3949
(2009/04/07)
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- 16-Substituted polyunsaturated hexadecanoic fatty acids
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Sixteen carbon atom carboxylic acids having 16-phenoxy or 16-phenylthio substituents, and 0, 1, or 4 triple bonds, methods of preparing them, and pharmaceutical preparations containing them. These compounds are useful as lipoxygenase inhibitors.
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