10506-73-7Relevant articles and documents
Potent anti-ovarian cancer with inhibitor activities on Both Topoisomerase II and V600EBRAF of synthesized substituted estrone candidates
El-Naggar, Mohamed,Amr, Abd El-Galil E.,Fayed, Ahmed A.,Elsayed, Elsayed A.,Al-Omar, Mohamed A.,Abdalla, Mohamed M.
, (2019)
A series of 16-(α-alkoxyalkane)-17-hydrazino-estra-1(10),2,4-trien[17,16-c]-3-ol (3a-l) and estra-1(10),2,4-trien-[17,16-c]pyrazoline-3-ol derivatives (4a-d) were synthesized from corresponding arylidines 2a,b which was prepared from estrone 1 as starting material. Condensation of 1 with aldehydes gave the corresponding arylidine derivatives 2a,b which were treated with hydrazine derivatives in alcohols to give the corresponding derivatives 3a-l, respectively. Additionally, treatment of 2a,b with methyl- or phenylhydrazine in ethanolic potassium hydroxide afforded the corresponding N-substituted pyrazoline derivatives 4a-d, respectively. All these derivatives showed potent anti-ovarian cancer both in vitro and in vivo. The mechanism of anti-ovarian cancer was suggested to process via topoisomerase II and V600EBRAF inhibition.
Modification of estrone at the 6, 16, and 17 positions: Novel potent inhibitors of 17β-hydroxysteroid dehydrogenase type 1
Allan, Gillian M.,Lawrence, Harshani R.,Cornet, Josephine,Bubert, Christian,Fischer, Delphine S.,Vicker, Nigel,Smith, Andrew,Tutill, Helena J.,Purohit, Atul,Day, Joanna M.,Mahon, Mary F.,Reed, Michael J.,Potter, Barry V. L.
, p. 1325 - 1345 (2007/10/03)
The 17β-hydroxysteroid dehydrogenases (17β-HSDs) catalyze the interconversion between the oxidized and reduced forms of androgens and estrogens at the 17 position. The 17β-HSD type 1 enzyme (17β-HSD1) catalyzes the reduction of estrone to estradiol and is
