Design and Synthesis of Estrogen Derivative

Abstract

Some estrogen derivatives have been developed for use in different biological and analytical methods 1-3 . For example, there are studies which show the synthesis of 2-alkylsulfanyl estrogens which are achieved by a directed ortho-lithiation reaction of suitably protected estrone followed by disulfide quench and final deprotection 4 . Other data showed the synthesis of nitrile derivatives of estrogens by reaction of 7α-cyano-19-nortestosterone with copper(II ) bromide in acetonitrile at room temperature, resulting in aromatization of the A-ring of steroid 5 . In addition, other estradiol derivative (17α-(ruthenocenylmethyl)estra-1,3,5(10)-trien-3,17β-diol) was synthetized by the reaction between 17β-spiro-oxiranyl estradiol and lithium ruthenocenyl in THF 6 . Also, several 17β-O-alkyl ethers (methyl, ethyl, propyl, butyl, hexyl and octyl) of estradiol were obtained from 3-O-benzyl-17β-estradiol with sodium hydride/ alkyl halide, followed by the removal of O-benzyl protecting group via catalytic transfer hydrogenation 7 . Additionally, there are some reports which shown the synthesis of an estradiol derivative by the Reformatsky reaction of 3,17β-bis [(2trimethylsilyl

Evaluation of Biological Activity Exerted by Dibenzo[b,e]Thiophene-11(6H)-One on Left Ventricular Pressure Using an Isolated Rat Heart Model

“…Furthermore, another report display that some pyranopyrazole derivatives can act as positive inotropic agents in a spontaneously hypertensive rats model 24 . Recently was prepared a pyridine-hexacyclic-steroid derivative which produce positive inotropic activity in an isolated rat heart model 25 . All these data showed that several drugs can exert changes in the system cardiovascular; however, the molecular mechanism involved in their biological activity of each compound is very unclear; perhaps these effects are due to differences in the chemical structure of each drug or to different methods used in each experiment.…”