TY - JOUR
T1 - Inhibition of aromatase activity and of endocrine-responsive tumor growth by 10-propargylestr-4-ene-3, 17-dione and its 17-propionate derivative
AU - Zimniski, Steven J.
AU - Brandt, Mark E.
AU - Covey, Douglas F.
AU - Puett, David
N1 - Funding Information:
We thank Dr. Enrique Mendoza for his assistance with the in vitro aromatase assays in the presence of PEDP. This work was supported by the National Institutes of Health (Research Grants CA43226, CA23582, and AM33973), the Florida Division American Cancer Society Carl B. Ferguson Fund and the American Cancer Society/Women's Cancer Association Institutional Grant. D.F.C. is the recipient of a Research Career Development Award (CAO0829).
PY - 1987
Y1 - 1987
N2 - Two androstenedione derivatives, 10-propargylestr-4-ene-3,17-dione and its 17-propionated form, were administered to normal cycling rats, and both compounds led to an inhibition of ovarian aromatase. Under in vitro conditions, only the former compound exhibited high potency as an inhibitor of rat ovarian and human placental microsomal aromatase. At 1 mg/kg/day both compounds were effective in promoting regression of 9,10-dimethyl-1,2-benzanthracene-induced mammary tumors in rats without terminating their estrous cycle. PED also inhibited growth of a human ovarian carcinoma in athymic mice. The results with the 17-propionated compound testify to the necessity of in vivo assays in screening antitumor agents. In summary, PED and its propionated derivative inhibited ovarian aromatase in vivo and inhibited the growth of hormone-responsive tumors.
AB - Two androstenedione derivatives, 10-propargylestr-4-ene-3,17-dione and its 17-propionated form, were administered to normal cycling rats, and both compounds led to an inhibition of ovarian aromatase. Under in vitro conditions, only the former compound exhibited high potency as an inhibitor of rat ovarian and human placental microsomal aromatase. At 1 mg/kg/day both compounds were effective in promoting regression of 9,10-dimethyl-1,2-benzanthracene-induced mammary tumors in rats without terminating their estrous cycle. PED also inhibited growth of a human ovarian carcinoma in athymic mice. The results with the 17-propionated compound testify to the necessity of in vivo assays in screening antitumor agents. In summary, PED and its propionated derivative inhibited ovarian aromatase in vivo and inhibited the growth of hormone-responsive tumors.
UR - http://www.scopus.com/inward/record.url?scp=0023515690&partnerID=8YFLogxK
U2 - 10.1016/0039-128X(83)90067-3
DO - 10.1016/0039-128X(83)90067-3
M3 - Article
C2 - 3504057
AN - SCOPUS:0023515690
SN - 0039-128X
VL - 50
SP - 135
EP - 146
JO - Steroids
JF - Steroids
IS - 1-3
ER -