140421-65-4Relevant articles and documents
Synthesis and antiproliferative activity of some androstene oximes and their O-Alkylated derivatives
Acharya, Pratap Chandra,Bansal, Ranju
, p. 193 - 199 (2014/03/21)
In order to study the structure-activity relationship with respect to the cytotoxicity of steroidal oximes, several 6E-hydroximino-4-ene steroids and their O-alkylated derivatives were synthesized. The oxime ethers were solidified and purified by preparing their corresponding oxalate salts. The new derivatives as well as some previously synthesized ones were evaluated for in vitro antineoplastic activity against a panel of 60 cancer cell lines at 10 μM. The oximes and oxime ethers were found to have moderate to good antiproliferative activity against various leukemia, colon, melanoma, and renal cancer cell lines. Several 6E-hydroximino-4-ene steroids and their O-alkylated derivatives were synthesized. Their structure-activity relationship with respect to the cytotoxicity of steroidal oximes was studied. The oximes and oxime ethers were found to have moderate-to-good antiproliferative activity against various leukemia, colon, melanoma, and renal cancer cell lines.
AZAHETEROCYCLYL DERIVATIVES OF ANDROSTANES AND ANDROSTENES AS MEDICAMENTS FOR CARDIOVASCULAR DISORDERS
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Page/Page column 138-139, (2008/06/13)
Compounds of formula (I) wherein: the groups are as defined in the description, are useful for the preparation of medicaments for the treatment of cardiovascular disorders, in particular heart failure and hypertension. The compounds are inhibitors of the enzymatic activity of the Na+,K+-ATPase. They are useful for the preparation of a medicament for the treatment of a disease caused by the hypertensive effects of endogenous ouabain, such as renal failure progression in autosomal dominant polycystic renal disease (ADPKD), preeclamptic hypertension and proteinuria and renal failure progression in patients with adducin polymorphisms.
Synthesis of cytotoxic 6E-hydroximino-4-ene steroids: Structure/activity studies
Deive,Rodríguez,Jiménez
, p. 2612 - 2618 (2007/10/03)
In an effort to determine the pharmaceutical utility and the structural requirements for activity against various tumor cell lines, several 6E-hydroximino-4-ene steroids with different side chains and degrees of unsaturation on ring A were synthesized in our laboratory. Evaluation of the synthesized compounds for cytotoxicity against P-388, A-549, HT-29, and MEL-28 tumor cells revealed that some important structural features are required for activity. The presence of a cholesterol-type side chain, which appears to play a major role in determining the biological activity, the existence of a ketone functionality at C-3, and an elevated degree of oxidation on ring A all result in higher bioctivity than other structural motifs.
A synthesis of oximes from olefins by cobalt(II) porphyrin-catalyzed reduction-nitrosation
Sugamoto, Kazuhiro,Hamasuna, Yutaka,Matsushita, Yoh-Ichi,Matsui, Takanao
, p. 1270 - 1272 (2007/10/03)
Various olefins such as styrenes, α,β-unsaturated carbonyl compounds, and α,β,γ,δ-unsaturated carbonyl compounds were directly converted to the corresponding acetophenoximes, α-hydroxyimino carbonyl compounds and γ-hydroxyimino-α,β-unsaturated carbonyl compounds in good or moderate yields by reduction-nitrosation with t-butyl nitrite and triethylsilane in the presence of cobalt(II) porphyrin as a catalyst.
Synthesis of 6-Hydroximino-3-oxo Steroids, aNew Class of Aromatase Inhibitor
Holland, Herbert L.,Kumaresan, Sudalaiyandi,Tan, Liat,Njar, Vincent C. O.
, p. 585 - 588 (2007/10/02)
(E)-3β,17β-Dihydroxyandrost-4-en-6-one oxime has been converted into (E)-6-hydroximinotestosterone and (E)-6-hydroximinoandrost-4-ene-3,17-dione by chemical methods, and into (E)-6-hydroximinoandrosta-1,4-diene-3,17-dione by biotransformation using Arthrobacter simplex ATCC 6946.
