1670-85-5Relevant articles and documents
Imidazolone and imidazolidinone artifacts of a pivotal imidazolthione, zyzzin, from the poecilosclerid sponge Zyzza massalis from the Coral Sea. The first thermochromic systems of marine origin
Mancini,Guella,Debitus,Duhet,Pietra
, p. 1886 - 1894 (1994)
Dry acetone extracts of the freeze-dried, deep-red powder of the poecilosclerid sponge Zyzza massalis (Dendy) from the Coral Sea gave the orange alkaloid zyzzin (=4-(1H-indol-3-yl)-1,5-dihydro-5-thioxo-1H-imidazol-2-one; 14), which underwent exchange of the 5-thioxo for the 5-oxo group during aqueous chromatographic workup, giving yellow 13. Both 13 and 14 added hydroxylic solvents at C(4)=N giving colourless, racemic products, 3 and 8, respectively, by incorporation of MeOH and 10 and 11, respectively, by incorporation of H2O. On warming 3 or 10 in DMSO, 13 was recovered, thus furnishing a novel thermochromic system. Optically active (±)-12, which may be viewed to derive from enzymatic reduction of 14 at C(4)=N followed by S→O exchange, was also isolated from this sponge, along with the linear amides 16 and 19. Compound 3 proved to have antibacterial and antifungal activities.
PYRIMIDINE COMPOUND, PREPARATION METHOD THEREOF AND MEDICAL USE THEREOF
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, (2021/04/10)
The present invention discloses a pyrimidine compound, a preparation method thereof and a medical use thereof. Specifically, the present invention discloses a pyrimidine compound represented by formula (I), pharmaceutically acceptable salts thereof, a preparation method thereof, and a use thereof as a cyclin-dependent kinase 9 (CDK9) inhibitor, particularly for the treatment of cancer. The definition of each group in formula (I) is the same as that in the specification.
Screening of NOS activity and selectivity of newly synthesized acetamidines using RP-HPLC
Fantacuzzi, Marialuigia,Maccallini, Cristina,Di Matteo, Mauro,Ammazzalorso, Alessandra,Bruno, Isabella,De Filippis, Barbara,Giampietro, Letizia,Mollica, Adriano,Amoroso, Rosa
, p. 419 - 424 (2016/02/16)
Nitric Oxide Synthase (NOS) inhibitors could play a powerful role in inflammatory and neurodegenerative diseases. In this work, novel acetamidine derivatives of NOS were synthesized and the inhibitor activity was evalued. To screen the activity and selectivity, the l-citrulline residue, after the enzymatic NOS assay, was derivatized with o-phthaldialdehyde/N-acetyl cysteine (OPA/NAC) and then evaluated by RP-HPLC method with fluorescence detection.All compounds did not affect the activity of endothelial and neuronal isoforms, while nine of them possessed a percentage of iNOS activity at 10 μM lower than 50%, and were selected for IC50 evaluation. Among them, a compound emerged as a very potent (IC50 of 53 nM) and selective iNOS inhibitor.
Synthesis and antitumor activity of new thiazole nortopsentin analogs
Attanzio, Alessandro,Barraja, Paola,Carbone, Anna,Cascioferro, Stella,Cirrincione, Girolamo,Diana, Patrizia,Montalbano, Alessandra,Parrino, Barbara,Spanò, Virginia,Tesoriere, Luisa
, (2017/01/04)
New thiazole nortopsentin analogs in which one of the two indole units was replaced by a naphthyl and/or 7-azaindolyl portion, were conveniently synthesized. Among these, three derivatives showed good antiproliferative activity, in particular against MCF7 cell line, with GI50 values in the micromolar range. Their cytotoxic effect on MCF7 cells was further investigated in order to elucidate their mode of action. Results showed that the three compounds act as pro-apoptotic agents inducing a clear shift of viable cells towards early apoptosis, while not exerting necrotic effects. They also caused cell cycle perturbation with significant decrease in the percentage of cells in the G0/G1 and S phases, accompanied by a concomitant percentage increase of cells in the G2/M phase, and appearance of a subG1-cell population.
