70059-65-3Relevant academic research and scientific papers
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.
Design, synthesis & evaluation of condensed 2H-4-arylaminopyrimidines as novel antifungal agents
Jain, Kishor S.,Khedkar, Vijay M.,Arya, Nikhilesh,Rane, Prasad V.,Chaskar, Pratip K.,Coutinho, Evans C.
, p. 166 - 175 (2014/04/03)
A small, focussed library of condensed 2H-4-arylaminopyrimidines, with 3-diversity points, based on an initial design by molecular docking study of this scaffold at the active site of the fungal enzyme of cytochrome P 450 family, lanosterol 14α
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
TRICYCLIC BENZO[4,5]THIENO-[2,3-D]PYRIMIDINE-4-YL-AMIN DERIVATIVES, THEIR SALTS, PROCESS FOR PRODUCING THE COMPOUNDS AND THEIR PHARMACEUTICAL USE
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Page/Page column 5, (2011/02/18)
The invention relates to novel tricyclic benzo[4,5]thieno-[2,3-d]pyrimidine-4-yl-amin derivatives, as well as their pharmaceutically acceptable salts. The subject of the invention too the process for producing the compounds and their use as a pharmaceutic
TRICYCLIC BENZO[4,5]THIENO-[2,3-D]PYRIMIDINE-4-YL-AMIN DERIVATIVES, THEIR SALTS, PROCESS FOR PRODUCING THE COMPOUNDS AND THEIR PHARMACEUTICAL USE
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Page/Page column 11-12, (2009/10/18)
The invention relates to novel tricyclic benzo[4,5]thieno-[2,3-d]pyrimidine-4-yl-amin derivatives, as well as their pharmaceutically acceptable salts. The subject of the invention too the process for producing the compounds and their use as a pharmaceutic
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.
