108191-29-3Relevant academic research and scientific papers
Small molecule compound for overcoming EGFR drug resistance mutation as well as preparation method and application of small molecule compound
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Paragraph 0053-0057; 0063, (2019/04/06)
The invention belongs to the field of chemical medicines and specifically relates to a small molecule compound for overcoming EGFR drug resistance mutation. The small molecule compound has a formula as shown in the specification. The small molecule compound provided by the invention has a good inhibition effect on an H1975 cell strain with EGFRT790M mutation in vitro, that is, a part of moleculeshave median inhibitory concentrations up to a nanomole grade level upon H1975, is small in toxicity, has IC50 of 10 [mu]M or greater upon most cell strains except the H1975, has good selectivity, doesnot directly inhibit the activity of the EGFR, is capable of avoiding compound drug resistance caused by drug resistance mutation, provides novel effective options for development and preparation ofa new generation of EGFRT790M drug resistant small molecule target medicines, and has good development prospects.
Synthesis and Anticonvulsant Activity of Analogues of 4-Amino-N-(1-phenylethyl)benzamide
Clark, C. Randall,Davenport, Timothy W.
, p. 1214 - 1218 (2007/10/02)
A group of amides and amines related to 4-amino-N-(1-phenylethyl)benzamide, 1, were prepared in a study on the relationship of structure to anticonvulsant activity in this compound. Acylation and alkylation of the amino group of 1 resulted in almost total loss of anticonvulsant activity. Insertion of a methylene between the 4-amino group and the aromatic ring of 1 produced a slight increase in anticonvulsant potency and a significant increase in toxicity. Hydride reduction of the amide carbonyl in 1 also yielded compounds having a slightly lower ED50 against convulsions induced by electroshock and a much lower TD50 in the rotorod assay. Modification of the 1-phenylethyl group of 1 also decreased anticonvulsant potency.
