Boronated pyrimidines and purines as cytotoxic, hypolipidemic and anti-inflammatory agents.
The simple boronated bases, e.g. cytosine, adenine and guanine, containing no sugar residues retained good pharmacological activity as hypolipidemic, anti-neoplastic and anti-inflammatory agents in mice at 8 mg/kg. Their activities were generally identical to their respective nucleoside derivatives. Interestingly the boronated acyclovir derivative was a very potent hypolipidemic agent achieving better activity than clofibrate and lovastatin. The boronated adenine derivatives appeared to have the best anti-inflammatory activity in reducing local edema and analgesic effects. The agents were active against the growth of murine and human leukemias and human HeLa-S(3) suspended uterine carcinoma. Only the boronated adenine derivatives were effective in blocking the growth of human SW480 adenocarcinoma and the KB nasopharynx.
Hall
I H
IH
Division of Medicinal Chemistry and Natural Products School of Pharmacy University of North Carolina Chapel Hill North Carolina 27599-7360 USA.
Burnham
B S
BS
Elkins
A
A
Sood
A
A
Powell
W
W
Tomasz
J
J
Spielvogel
B F
BF