Huo, Haibo published the artcileSynthesis and biological evaluation of novel steroidal pyrazole amides as highly potent anticancer agents, SDS of cas: 73874-95-0, the main research area is androstynyl pyrazolyl amide preparation antitumor apoptosis SAR; Amide derivatives; Antiproliferative activity; Cell cycle; Hydrochloride derivatives; Steroidal pyrazoles.
A series of thirty-six steroidal pyrazole amides, I, II [R = methylamino, 4-fluoroanilino, piperazinyl, etc.] divided into two categories based on their main skeletons were designed and synthesized via a five-step synthetic route. The final product was obtained through Pinnick oxidation of pyrazole aldehydes to yield the corresponding acids, which then underwent amidation to afford the target products efficiently under mild reaction conditions. Structures of the desired compounds were confirmed by 1H NMR, 13C NMR, high resolution mass spectrometry; X-ray structural characterization of compound II [R = piperazinyl] was also obtained. The synthesized compounds I, II were screened for their antiproliferative activity against four cancer cell lines (Pc-3 A549, Hela, HepG2) using the SRB method. Amides I,II [R = piperazinyl], and hydrochlorides II [R = 2-aminoethylamino, 2-aminopyrrolidinyl, 4-aminopiperidyl, etc.] exhibited moderate to high cytotoxic activities with IC50 values ranging from 2.05 to 8.73μM. Of note, the hydrochloride derivative II [R = piperazinyl] displayed the highest activity towards PC-3 cells with IC50 values of 2.05μM. Anal. of structure-activity relationships indicated that the presence of the diamine moiety and the aqueous solubility of the derivatives were vital factors for antiproliferative potency. Furthermore, mol. hydrochloride II [R = piperazinyl] induced PC-3 cells apoptosis and arrested cell cycle at G1 phase in a dose-dependent manner.
Steroids published new progress about Amines Role: RCT (Reactant), RACT (Reactant or Reagent). 73874-95-0 belongs to class piperidines, name is tert-Butyl piperidin-4-ylcarbamate, and the molecular formula is C10H20N2O2, SDS of cas: 73874-95-0.
Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem