| Literature DB >> 25982416 |
Germain Revelant1, Mira Al-Lakkis-Wehbe1, Marjorie Schmitt2, Sarah Alavi1, Céline Schmitt1, Lionel Roux1, Mounir Al-Masri1, Nadège Schifano-Faux1, Carmen Maiereanu1, Céline Tarnus1, Sébastien Albrecht3.
Abstract
In order to probe the S1 and S1' mammalian aminopeptidase N subsites, racemic 1- or 4-substituted 7-aminobenzocyclohepten-6-one derivatives were synthesized and evaluated for their ability to inhibit mammalian aminopeptidase N. We focused on improving the physicochemical and ADME properties of this series by targeting lipophilicity and LELP score. Some 4-heteroaryl substituted analogues displayed reduced lipophilicity and enhanced inhibition potency with Ki values in the nanomolar range.Entities:
Keywords: Aminopeptidase N inhibitors; Cancer; Racemic 1- or 4-substituted aminobenzocycloheptenone derivatives; Suzuki reaction
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Year: 2015 PMID： 25982416 DOI： 10.1016/j.bmc.2015.04.066
Source DB: PubMed Journal: Bioorg Med Chem ISSN： 0968-0896 Impact factor: 3.641