21203-74-7Relevant academic research and scientific papers
Kras-G12C inhibitor heterocyclic compounds
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Paragraph 0056; 0058-0059, (2021/03/31)
The invention relates to Kras-G12C inhibitor heterocyclic compounds and a preparation method thereof, and application of the compounds in prevention and treatment of tumor diseases such as lung cancer, colorectal cancer and pancreatic cancer. In the preparation process, the compounds provided by the invention are obtained through a series of reactions such as a condensation reaction, an intramolecular cyclization reaction, a chlorination reaction, an SN2 reaction, a coupling reaction, deprotection and the like.
Efficient synthesis of ribonucleotide reductase inhibitors 3- aminopyridine-2-carboxaldehyde thiosemicorbazone (3-AP) and 3-amino-4- methylpyridine-2-carboxaldehyde thiosemicarbazone (3-AMP) via palladium mediated cross-coupling reactions
Li, Jun,Chen, Shu-Hui,Li, Xiuyan,Niu, Chuansheng,Doyle, Terrence W.
, p. 393 - 400 (2007/10/03)
An efficient synthesis of potent ribonucleotide reductases inhibitors 3- amino-pyridine-2-carboxaldehyde thiosemicarbazone (3-AP) end 3-amino-4- methyl-pyridine-2-carboxaldehyde thiosemicarbazone (3-AMP) is described. The synthesis of 3-AP and 3-AMP was achieved in 4 and 5 steps, with overall yields of 61% and 39%, respectively. The synthesis featured a convergent approach utilizing a Stille coupling strategy to prepare vinylpyridine derivatives. A more economic way to synthesize vinylpyridine using Heck reaction was also discussed.
Synthesis and Antitumor Activity of 3- and 5-Hydroxy-4-methylpyridibe-2-carboxaldehyde Thiosemicarbazones
Wang, Yuqiang,Liu, Mao-Chin,Lin, Tai-Shun,Sartorelli, Alan C.
, p. 3667 - 3671 (2007/10/02)
To develop an α-(N)-heterocyclic carboxaldehyde thiosemicarbazone with clinical utility as an anticancer agent, two analogues, 3-hydroxy-4-methylpyridine-2-carboxaldehyde thiosemicarbazone (3-HMP) and 5-hydroxy-4-methylpyridine-2-carboxaldehyde thiosemicarbazone (5-HMP), of 5-hydroxypyridine-2-carboxaldehyde thiosemicarbazone (5-HP) have been designed and synthesized by two different methods. 3-HMP and 5-HMP both showed better antitumor activity than their respective parent compounds, 3-hydroxypyridine-2-carboxaldehyde thiosemicarbazone and 5-HP, in mice bearing the L1210 leukemia.
