Phosphonate-containing analogs of cholesteryl ester as novel inhibitors of cholesteryl ester transfer protein

Bioorganic and Medicinal Chemistry Letters

Volumn 6, Issue 16, 1996, Pages 1951-1954

  Pietzonka, Thomas ^b   Damon, Robert ^a   Russell, Mary ^a   Wattanasin, Sompong ^a  

^a Sandoz Pharma Ltd   (Switzerland)

^b Preclinical Research   (Switzerland)

Author keywords

[No Author keywords available]

Indexed keywords

CHOLESTEROL ESTER; CHOLESTEROL ESTER TRANSFER PROTEIN;

ANIMAL CELL; ARTICLE; CHO CELL; CHOLESTEROL TRANSPORT; DRUG SYNTHESIS; GENE TRANSFER; HUMAN; NONHUMAN; STRUCTURE ACTIVITY RELATION;

ANIMALIA;

EID: 0030594966     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/0960-894X(96)00350-2     Document Type: Article

References (22)

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16. 50 of 1.5 μM. PD 140195 (figure presented)
17. 13. Replacement of the ester group in cholesteryl oleate with the corresponding amide group showed no effect in CETP inhibitory activity.
18. 14 The corresponding amide, urea, and acyl ester of 7 showed no CETP inhibitory activity.
19. 15. For the discussion on binding energies of phosphorus-containing groups, see: (a) Bartlett, P. A.; Marlowe, C. Science 1987, 235, 569.;
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21. 16. Since desirable compounds must inhibit CETP activity in the plasma components, secondary assays have been established to test these compounds for CETP inhibition in the presence of plasma components. Preliminary results showed that compound 7 inhibited CETP activity in the presence of plasma components.
22. 17. For newly published 1,3,5-triazines as CETP inhibitors, see: Xia, Y.; Mirzai, B.; Chackalamannil, S.; Czarniecki, M.; Wang, S.; Clemmons, Ahn, H. S.; Boykow, G. C. Bioorg. Med. Chem. Lett. 1996, 6, 919.