- Human estrogen receptor α antagonists, part 2: Synthesis driven by rational design, in vitro antiproliferative, and in vivo anticancer evaluation of innovative coumarin-related antiestrogens as breast cancer suppressants
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New twelve in silico designed coumarin-based ERα antagonists, namely 3DQ-1a to 3DQ-1е, were synthesized and confirmed as selective ERα antagonists, showing potencies ranging from single-digit nanomolar to picomolar. The hits were confirmed as selective es
- Kurtanovi?, Nezrina,Toma?evi?, Nevena,Mati?, Sanja,Mitrovi?, Marina M.,Kosti?, Danijela A.,Sabatino, Manuela,Antonini, Lorenzo,Ragno, Rino,Mladenovi?, Milan
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supporting information
(2021/10/29)
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- Method for preparing diloxitol fumarate
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The invention relates to the technical field of a bulk drug preparation method and in particular relates to a method for preparing a bulk drug diloxitol fumarate. The preparation method comprises thefollowing steps: 1) performing an ammoniation reaction, namely enabling succinic anhydride to react with an ammoniating reagent so as to produce succinimide; 2) performing an alkylation reaction, namely enabling succinimide to react with 1,2 halogenated ethane in the presence of a catalyst and a base so as to generate a compound of a formula IV shown in the description; and 3) performing an esterification reaction, namely enabling a compound of a formula IV compound shown in the description to react with trans-monomethyl fumarate, so as to generate diloxifyl fumarate. The method has the advantages that material reagents used in the method are convenient and easy to obtain, the reaction steps are short, the total yield is high, the product is easy to purify through recrystallization, and base toxic impurities are easy to be controlled through recrystallization, and the like.
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Paragraph 0081; 0084-0085
(2020/02/14)
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- A Thiophene Analogue of Praziquantel, and Related Systems, by Intramolecular Cyclisation of Acyliminium Salts
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N--succinimide (7a) and -glutarimide (7b) on reduction with sodium borohydride in methanol at -10 deg C yield the respective hydroxylactams which on treatment with formic acid cyclise via the intermediate acyliminium ions to 4,5,9,9a-tetrahydropyrrolothienopyridin-7-one (9a) and 4,5,8,9,10,10a-hexahydropyridothienopyridin-7-one (9b) respectively.In a similar manner, 4-cyclohexylcarbonyl-1-piperazine-2,6-dione (11) is converted into the thiophene isostere (2) of praziquantel (1).Likewise, formic acid induced cyclisations of the hydroxylactams derived from N-- (16) and N-succinimide (19) furnish 5,6,10,10a-tetrahydropyrrolothienothiazepin-8(9H)-one (18) and 5,6,10,10a-tetrahydropyrrolothienothiazepin-8(9H)-one (21), respectively.
- Meth-Cohn, Otto,Vij, Rup Rani,Smalley, Robert K.,Bass, Robert J.
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p. 1001 - 1018
(2007/10/02)
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- Excited-State ? Succimidyl and Glutarimidyl Radicals: Reversible Ring Opening
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The free-radical isomerization of N-bromosuccinimide to β-bromopropionyl isocyanate has been examined.Of the two varieties of succinimidyl radical (S? or S?), only the ? excited state undergoes the ring opening to the β propionyl isocyanatyl radical.The conversion optimally takes place in >95percent yield.The dependence of NBS concentration along with results obtained from deuterium labeling studies indicate that the ring opening of S? is a reversible process.This explains the failure of N-chlorosuccinimide to produce β-chloropropionyl isocyanate, as well as the increase in ring-opened product for N-bromosuccinimides upon methyl substitution at the 2- and/or 3-position of the succinimidyl ring, since the open-chain radical intermediates are more stable.In the N-bromoglutarimide system, methyl groups on the 2-position are required for the glutarimidyl radicals to undergo the isomerization, ultimately producing isocyanates.The radical-chain nature of these systems is confirmed.
- Tlumak, Robert L.,Day, James C.,Slanga, Joseph P.,Skell, Philip S.
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p. 7257 - 7267
(2007/10/02)
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- Acylation of bis(2 chloroethyl)amine (nitrogen mustard)
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The preparation is described of N,N bis [2 chloroethyl] amides of fatty and keto acids, of N,N bis [2 chloroethyl] amino acids and of N [2 chloroethyl] imides and amides as potential cytostatic agents.
- Hauptmann,Poge
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p. 520 - 522
(2007/10/05)
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