Chemical and Pharmaceutical Bulletin p. 2280 - 2286 (1996)
Update date:2022-07-30
Topics:
Watanabe, Hiroyoshi
Hatakeyama, Susumi
Tazumi, Kazuki
Takano, Seiichi
Masuda, Sonoko
Okano, Toshio
Kobayashi, Tadashi
Kubodera, Noboru
As putative metabolites of 1α,25-dihydroxy-22-oxavitamin D3 (OCT), 24-hydroxylated OCT in 24(R) and 24(5) forms, 24-ketoOCT, 26-hydroxylated OCT in 25(S) and 25(R) forms, pentanorOCT and pentanor-ketoOCT were synthesized from the steroidal 20(S)-alcohol. Their antiproliferation activities towards human promyelocytic leukemia cells (HL-60 cells) are also reported. Oxidized derivatives at the C-24 position, 24-ketoOCT, 24(R)-hydroxylated OCT and 24(S)-hydroxylated OCT, showed activities comparable to or slightly weaker than that of OCT, while 26-hydroxylated OCT was less active than OCT. Truncated OCT, pentanor OCT and pentanor-ketoOCT, were inactive at 10-7-10-10M.
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(1996)Doi:10.1021/jo970383s
(1997)Doi:10.1021/jm980400l
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(1996)Doi:10.1016/S0008-6215(96)00272-8
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(1997)
