摘要:
The invention provides N-acyl amino acid derivatives of general formula salts and esters thereof, wherein X represents an oxygen or sulphur atom, R 1 is an optionally substituted alkyl, alkenyl, cycloalkyl, aryl or aralkyl group or an optionally substituted alkylamino, cycloalkylamino, arylamino or aralkylamino group, R 2 is an optionally substituted alkyl, cycloalkyl or aryl group andR 3 is a hydrogen atom or an optionally substituted alkyl, cycloalkyl or aryl group; processes for their preparation and their use as fungicides.
摘要:
&bgr;-Substituted γ-amino acids, &bgr;-substituted γ-amino acid derivatives, and &bgr;-substituted γ-amino acid analogs and (bio)isosteres and their use as chemotherapeutic agents are disclosed. The &bgr;-substituted γ-amino acid derivatives and &bgr;-substituted γ-amino acid analogs and (bio)isosteres are selective LAT1/4F2hc substrates, capable of passing through the blood-brain barrier, and exhibit rapid uptake and retention in tumors expressing the LAT1/4F2hc transporter. Methods of synthesizing the &bgr;-substituted γ-amino acid derivatives and &bgr;-substituted γ-amino acid analogs and (bio)isosteres and methods of using the compounds for treating tumors are also disclosed. The &bgr;-substituted γ-amino acid derivatives and &bgr;-substituted γ-amino acid analogs and (bio)isosteres exhibit an improved selectivity toward tumor cells expressing the LAT1/4F2hc transporter and accumulate in cancerous cells when administered to a subject in vivo. The &bgr;-substituted γ-amino acid derivatives and &bgr;-substituted γ-amino acid analogs and (bio)isosteres exhibit an increased efficacy on a variety of tumor types.
摘要:
The present invention relates to alkoxyamines of general formula (I), and to compounds of general formula (lla), (lIb), (lIc), (IId), IIe), (Ilf) or (Ilg), as such and for the treatment of cancers.