Bioorganic and Medicinal Chemistry Letters p. 935 - 938 (1998)
Update date:2022-08-03
Topics:
Kawai, Megumi
Gunawardana, Indrani W. K.
Mollison, Karl W.
Hsieh, Gin C.
Lane, Benjamin C.
Luly, Jay R.
Ascomycin 2, a close analogue of the immunosuppressant FK506 1, was modified to incorporate a hydroxyl group at the C-33 position. This increased the aqueous solubility of ascomycin by a hundred-fold at pH 7.4 and by approximately 300-fold at pH 6.5. Ascomycin 3 also exhibited an excellent immunosuppressive activity in vitro, as tested in a human mixed lymphocyte proliferation (HuMLR) assay, and in vivo using a rat popliteal lymph node (rPLN) hyperplasia assay.
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