1436573-02-2

Upstream product

• 1383628-29-2 2-amino-4,5-bis(4-chlorophenyl)thiophene-3-carboxylic acid 
• 6850-65-3 p-hydroxycyclohexylamine 
• 108-90-7 chlorobenzene 
• 25026-34-0 4-chlorophenacetyl chloride 
• 51490-05-2 1,2-bis(4-chlorophenyl)ethanone 
• 1383628-19-0 C₁₈H₁₃Cl₂NO₂ 
• 1383628-25-8 C₁₈H₁₃Cl₂NO₂S 

Relevant academic research and scientific papers

Design, synthesis and biological evaluation of novel 3,4,5-trisubstituted aminothiophenes as inhibitors of p53-MDM2 interaction. Part 1

A series of 3,4,5-trisubstituted aminothiophenes were designed, synthesized, and evaluated for their p53-MDM2 binding inhibitory potency and anti-proliferation activities against A549 and PC3 tumor cell lines. Fourteen compounds had appreciably improved MDM2 binding affinities than lead compound MCL0527 (3) and a few compounds showed comparable activities to that of Nutlin-3. Meanwhile, most of the 3,4,5-trisubstituted aminothiophenes displayed better or equivalent anti-proliferation activities against wild-type p53 cell line A549 compared to that of Nutlin-3. Over ten compounds exhibited desirable selective profiles of p53 status. Particularly, compounds 9, 16 and 18 displayed 22-, 6- and 22-fold selectivity of p53 status, respectively, much better than that of Nutlin-3 (fourfold).