1955-61-9Relevant academic research and scientific papers
Fragment based search for small molecule inhibitors of HIV-1 Tat-TAR
Zeiger, Mirco,Stark, Sebastian,Kalden, Elisabeth,Ackermann, Bettina,Ferner, Jan,Scheffer, Ute,Shoja-Bazargani, Fatemeh,Erdel, Veysel,Schwalbe, Harald,G?bel, Michael W.
supporting information, p. 5576 - 5580 (2015/01/08)
Basic molecular building blocks such as benzene rings, amidines, guanidines, and amino groups have been combined in a systematic way to generate ligand candidates for HIV-1 TAR RNA. Ranking of the resulting compounds was achieved in a fluorimetric Tat-TAR
Synthesis and antiproliferative activity of 4-substituted-piperazine-1- carbodithioate derivatives of 2,4-diaminoquinazoline
Cao, Sheng-Li,Han, Ying,Yuan, Chong-Zhen,Wang, Yao,Xiahou, Zhi-Kai,Liao, Ji,Gao, Rui-Ting,Mao, Bei-Bei,Zhao, Bao-Li,Li, Zhong-Feng,Xu, Xingzhi
, p. 401 - 409 (2013/07/27)
A novel series of 4-substituted-piperazine-1-carbodithioate derivatives of 2,4-diaminoquinazoline were synthesized and tested for their antiproliferative activities against five human cancer cell lines including A549 (lung cancer), MCF-7 (breast adenocarcinoma), HeLa (cervical carcinoma), HT29 and HCT-116 (colorectal cancer). Most of the synthesized compounds showed broad spectrum antiproliferative activity (IC50 1.47-11.83 μM), of which 8f, 8m and 8q were the most active members with IC50 values in the range of 1.58-2.27, 1.84-3.27 and 1.47-4.68 μM against five cancer cell lines examined, respectively. Further investigations revealed that compounds 8f, 8m and 8q exhibited weak inhibition against dihydrofolate reductase and no activity against thymidylate synthase, while induced DNA damage and activated the G2/M checkpoint in HCT-116 cells.
Efficient copper-catalyzed synthesis of 4-aminoquinazoline and 2,4-diaminoquinazoline derivatives
Yang, Xiaobo,Liu, Hongxia,Futa, Hua,Qiao, Renzhong,Jiang, Yuyang,Zhao, Yufen
supporting information; experimental part, p. 101 - 106 (2010/08/06)
We have developed an efficient copper-catalyzed method for the synthesis of 4-aminoquinazoline and 2,4-diaminoquinazoline derivatives via reactions of substituted 2-bromobenzonitriles with amidines or guanidine, and the method is of economical and practic
Process for synthesizing antifolates
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Page 4, (2010/02/06)
This invention relates to a process for synthesizing certain folic acid analogues, which are useful in treating cancer, inflammatory diseases, autoimmune diseases, and are commonly referred to as antifolates. The process employs improved steps for annulation, derivatization and addition reactions to produce the described antifolates from commonly available starting materials.
