293766-33-3Relevant academic research and scientific papers
Design, synthesis and biological evaluation of 4-aniline-thieno[2,3-d]pyrimidine derivatives as MNK1 inhibitors against renal cell carcinoma and nasopharyngeal carcinoma
Zhang, Min,Jiang, Li,Tao, Jia,Pan, Zhaoping,He, Mingyao,Su, Dongyuan,He, Gu,Jiang, Qinglin
, p. 2268 - 2279 (2019/04/25)
MAP Kinase Interacting Serine/Threonine Kinase 1 (MNK1)play important roles in the signaling transduction of MAPK pathways. It is significantly overexpressed in renal clear cell carcinoma and head-neck squamous cell carcinoma tissues in both mRNA and prot
A Microwave-Enhanced Synthesis and Biological Evaluation of N-Aryl-5,6,7,8-tetrahydrobenzo[4,5]thieno[2,3-d]pyrimidin-4-amines
Han, Qing,Yin, Zijian,Sui, Jingjiao,Wang, Qingming,Sun, Yaquan
, p. 1483 - 1497 (2019/08/26)
A series of N-aryl-5,6,7,8-tetra-hydrobenzo[4,5]thieno[2,3-d]pyrimidin-4-amines were synthesized in moderate to good yield by using a microwave-enhanced conditions. The selected compounds were evaluated for their cytotoxic effects (IC50 values) on human pulmonary carcinoma (A549), murine BALB/c spontaneous colon adenocarcinoma (CT26) and human hepatocellular liver carcinoma (HepG2) cell lines in vitro. Amongst these compounds, one compound was found to have the better cytotoxic activity with reference to the standard Erlotinib hydrochloride (TarcevaTM) against A549 (IC50 = 16.06 ± 0.09 μM) and HepG2 (IC50 = 15.01 ± 0.31 μM) cell lines. Especially, two compounds showed best cytotoxic effects against CT26 (IC50 = 11.38 ± 0.44 μM) and HepG2 (IC50 = 8.51 ± 0.52 μM) cell lines, respectively. The preliminary structure-activity relationships were disclosed and the thieno[2,3-d]pyrimidine skeleton could be exploited to potential antitumor agents in the future.
Novel dual use of formamide-POCl3 mixture for the efficient, one-pot synthesis of condensed 2 H-pyrimidin-4-amine libraries under microwave irradiation
Jain, Kishore S.,Kathiravan, Muthu K.,Bariwal, Jitender B.,Chaskar, Pratip K.,Tompe, Santosh S.,Arya, Nikhilesh
, p. 719 - 727 (2013/01/15)
The novel dual use of formamide-POCl3 mixture for the incorporation of a C-N fragment to form the pyrimidine nucleus and its subsequent chlorination in an efficient, one-pot synthesis of potentially bioactive condensed 2H-pyrimidin-4-amine libraries under
THERAPEUTIC APPLICATION OF TRICICLIC AROMATIC AND SATURATED BENZO(4,5)THIENO-(2,3-D)PYRIMIDINE DERIVATES, AS WELL AS THEIR THERAPEUTICALLY ACCEPTABLE SALTS
-
Page/Page column 8-10, (2009/10/18)
The subject of the invention is therapeutic application of tricyclic aromatic and saturated benzo[4,5]thieno[2,3-d]pyrimidine derivatives and their therapeutically acceptable salts. The compounds according to the invention is used particularly as active agent of therapeutic preparations of tyrosine-kinase inhibiting action.
Microwave-based synthesis of novel thienopyrimidine bioisosteres of gefitinib
Phoujdar, Manisha S.,Kathiravan, Muthu K.,Bariwal, Jitender B.,Shah, Anamik K.,Jain, Kishor S.
, p. 1269 - 1273 (2008/09/18)
A series of novel 2-unsubstituted 4-(substituted)anilinothieno[2,3-d]pyrimidines is synthesized through the chlorination of the corresponding 2-unsubstituted-thieno[2,3-d]-pyrimidin-4-ones, followed by the nucleophilic displacement of the 4-Cl group of 9, with a variety of anilines. All four steps of this synthesis involve microwave irradiation (MWI) and the entire synthesis requires only 2 h.
