41212-96-8Relevant articles and documents
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
Kurtanovi?, Nezrina,Toma?evi?, Nevena,Mati?, Sanja,Mitrovi?, Marina M.,Kosti?, Danijela A.,Sabatino, Manuela,Antonini, Lorenzo,Ragno, Rino,Mladenovi?, Milan
supporting information, (2021/10/29)
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
A Thiophene Analogue of Praziquantel, and Related Systems, by Intramolecular Cyclisation of Acyliminium Salts
Meth-Cohn, Otto,Vij, Rup Rani,Smalley, Robert K.,Bass, Robert J.
, p. 1001 - 1018 (2007/10/02)
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.
Acylation of bis(2 chloroethyl)amine (nitrogen mustard)
Hauptmann,Poge
, p. 520 - 522 (2007/10/05)
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.