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Synthesis and Evaluation of Steroidal Hydroxamic Acids as Inhibitors of P450 17 (17α‐Hydroxylase/C17‐20‐Lyase)
Author(s) -
Haidar Samer,
Klein Christian D.P.,
Hartmann Rolf W.
Publication year - 2001
Publication title -
archiv der pharmazie
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.468
H-Index - 61
eISSN - 1521-4184
pISSN - 0365-6233
DOI - 10.1002/1521-4184(200104)334:4<138::aid-ardp138>3.0.co;2-y
Subject(s) - hydroxylamine , chemistry , hydroxamic acid , enzyme , microsome , substrate (aquarium) , tris , trimethylsilyl , lyase , biochemistry , stereochemistry , organic chemistry , biology , ecology
With the aim of developing new inhibitors of 17α‐hydroxylase/ C17,20‐lyase (P450 17, CYP 17), two steroidal hydroxamic acids (compounds 2 and 3 ) were synthesized and evaluated as inhibitors of CYP 17. The synthesis was performed using carboxylic acids as starting material to give acid chlorides which were reacted with N,N,O ‐tris(trimethylsilyl) hydroxylamine. Using microsomal fractions of human and rat testes and progesterone as a substrate, both compounds moderately inhibited the human and rat enzyme.