36210-71-6Relevant academic research and scientific papers
Synthesis of α-santonin derived acetyl santonous acid triazole derivatives and their bioevaluation for T and B-cell proliferation
Dangroo, Nisar A.,Singh, Jasvinder,Dar, Alamgir A.,Gupta, Nidhi,Chinthakindi, Praveen K.,Kaul, Anpurna,Khuroo, Mohmmed A.,Sangwan, Payare L.
, p. 160 - 169 (2016/05/24)
A new series of α-santonin derived acetyl santonous acid 1,2,3-triazole derivatives were synthesised using Huisgen 1,3-dipolar cyclo-addition reaction (click chemistry approach) and evaluated for their in vitro inhibition activity on concanavalin A (ConA) induced T cell proliferation and lipopolysaccharide (LPS) induced B cell proliferation. Among the synthesised series, compounds 2-10 and 19 exhibited significant inhibition against ConA and LPS stimulated T-cell and B-cell proliferation in a dose dependent manner. More significantly compounds 4, 9-10 and 19 exhibited potent inhibition activity with remarkably lower cytotoxicity on the mitogen-induced T cell and B cell proliferation at 1 μM concentration. The compound 6 displayed potent immunosuppressive effects with ~89% against LPS induced B-cell and ~83% against ConA stimulated T-cell proliferation at 100 μM concentration without cytotoxicity. Compound 10 was more selective against B cell proliferation and exhibited 81% and 69% suppression at 100 and 1 μM concentration respectively. The present study led to the identification of several santonin analogs with reduced cytotoxicity and strong inhibition activity against the cell proliferation induced by the mitogens.
Synthetic modification of hydroxychavicol by Mannich reaction and alkyne-azide cycloaddition derivatives depicting cytotoxic potential
Kumar, Sunil,Pathania, Anoop S.,Satti, Naresh K.,Dutt, Parbhu,Sharma, Neha,Mallik, Fayaz A.,Ali, Asif
, p. 236 - 245 (2015/05/27)
Here we report the design, synthesis and lead optimization of hydroxychavicol (1) a high yielding metabolite ubiquitously present in the Piper betel leaves with the significant cytotoxic activity. This is the first report to describe the synthetic strateg
Synthesis of 3-O-propargylated betulinic acid and its 1,2,3-triazoles as potential apoptotic agents
Majeed, Rabiya,Sangwan, Payare L.,Chinthakindi, Praveen K.,Khan, Imran,Dangroo, Nisar A.,Thota, Niranjan,Hamid, Abid,Sharma, Parduman R.,Saxena, Ajit K.,Koul, Surrinder
, p. 782 - 792 (2013/07/25)
Cytotoxic agents from nature are presently the mainstay of anticancer chemotherapy, and the need to reinforce the arsenal of anticancer agents is highly desired. Chemical transformation studies carried out on betulinic acid, through concise 1,2,3-triazole
One-pot, efficient, and regioselective syntheses of 1,4-disubstituted 1,2,3-triazoles using aryldiazonium silica sulfates in water
Zarei, Amin
experimental part, p. 5176 - 5179 (2012/09/22)
A one-pot, efficient, and straightforward procedure for the copper-catalyzed synthesis of 1,4-disubstituted 1,2,3-triazoles is studied by in situ generation of aryl azides via the reaction of aryldiazonium silica sulfates and sodium azide, followed by coupling with a terminal alkyne. These reactions are carried out in water at room temperature without using any additional ligands.
Microwave-assisted click chemistry synthesis of 1,2,3-triazoles from aryldiazonium silica sulfates in water
Zarei, Amin,Khazdooz, Leila,Hajipour, Abdol R.,Azizi, Ghobad,Aghaei, Hamidreza
, p. 3353 - 3360,8 (2012/12/12)
A microwave-assisted click chemistry synthesis of 1,4-disubstituted 1,2,3-triazoles is studied by in situ generation of aryl azides via the reaction of aryldiazonium silica sulfates and sodium azide, followed by coupling with a terminal alkyne in the presence of copper catalyst. These reactions are carried out in water under mild and heterogeneous conditions without using any additional ligands.
A fast and efficient method for the preparation of aryl azides using stable aryl diazonium silica sulfates under mild conditions
Zarei, Amin,Hajipour, Abdol R.,Khazdooz, Leila,Aghaei, Hamidreza
experimental part, p. 4443 - 4445 (2009/11/30)
An efficient, fast, and straightforward procedure for the synthesis of aromatic azides using aryl diazonium silica sulfates and sodium azide at room temperature under mild conditions is described. The use of inexpensive materials, simple and clean work-up
Copper/HP20: Novel and polymer-supported copper catalyst for huisgen cycloaddition
Kitamura, Yoshiaki,Taniguchi, Kazumi,Maegawa, Tomohiro,Monguchi, Yasunari,Kitade, Yukio,Sajiki, Hironao
experimental part, p. 521 - 532 (2009/09/06)
A polymer-supported copper catalyst (Cu/HP20) is easily prepared in water and effectively catalyzed the Huisgen cycloaddition between azides and terminal alkynes.
Development of a practical and scalable preparation using sonication of Pd/fibroin catalyst for chemoselective hydrogenation
Kitamura, Yoshiaki,Tanaka, Asami,Sato, Mutsumi,Oono, Keiji,Ikawa, Takashi,Maegawa, Tomohiro,Monguchi, Yasunari,Sajiki, Hironao
, p. 4381 - 4388 (2008/03/13)
A practical and efficient preparation method of palladium-fibroin (Pd/Fib), silk-fibroin-supported Pd(0) by means of sonication, has been developed. The Pd/Fib catalyst could be prepared within 12 h at room temperature starting from commercial silk-fibroin and Pd(OAc)2 in MeOH, whereas our previous preparation method required at least 4 days. The present improved process is applicable to a large-scale preparation of Pd/Fib. The Pd/Fib prepared by the present method also catalyzed chemoselective hydrogenation of acetylenes, olefins, and azides in the presence of aromatic ketones, aldehydes, and halides; N-Cbz protective groups; and benzyl esters, which are readily hydrogenated under the Pd/C- or Pd/C(en)-catalyzed hydrogenation conditions. Copyright Taylor & Francis Group, LLC.
A convenient and efficient conversion of 4-aminobenzophenone into some new 1,2,3-triazole and benzothiazole derivatives
Kamel, Eman M.,Ahmad, Ragaa A.,Moustafa, Osama S.
, p. 149 - 153 (2007/10/03)
Several heterocyclic systems such as 1,2,3-triazoles (5-9), pyrimidotriazoles (10-13), benzothiazole (16), thiazolo (17), andpyrimidinone derivative (18) was obtained from 4-aminobenzophenone (1) and the appropriatere agents.
