15457-50-8Relevant articles and documents
Sulfonimide and amide derivatives as novel PPARα antagonists: Synthesis, antiproliferative activity, and docking studies
Ammazzalorso, Alessandra,Bruno, Isabella,Florio, Rosalba,de Lellis, Laura,Laghezza, Antonio,Cerchia, Carmen,de Filippis, Barbara,Fantacuzzi, Marialuigia,Giampietro, Letizia,Maccallini, Cristina,Tortorella, Paolo,Veschi, Serena,Loiodice, Fulvio,Lavecchia, Antonio,Cama, Alessandro,Amoroso, Rosa
, p. 624 - 632 (2020)
An agonist?antagonist switching strategy was performed to discover novel PPARα antagonists. Phenyldiazenyl derivatives of fibrates were developed, bearing sulfonimide or amide functional groups. A second series of compounds was synthesized, replacing the
Synthesis, biological evaluation, and molecular docking of new series of antitumor and apoptosis inducers designed as VEGFR-2 inhibitors
Abdallah, Abdallah E.,Mabrouk, Reda R.,Al Ward, Maged Mohammed Saleh,Eissa, Sally I.,Elkaeed, Eslam B.,Mehany, Ahmed B. M.,Abo-Saif, Mariam A.,El-Feky, Ola A.,Alesawy, Mohamed S.,El-Zahabi, Mohamed Ayman
, p. 573 - 591 (2022/01/20)
Based on quinazoline, quinoxaline, and nitrobenzene scaffolds and on pharmacophoric features of VEGFR-2 inhibitors, 17 novel compounds were designed and synthesised. VEGFR-2 IC50 values ranged from 60.00 to 123.85 nM for the new derivatives compared to 54.00 nM for sorafenib. Compounds 15a, 15b, and 15d showed IC50 from 17.39 to 47.10 μM against human cancer cell lines; hepatocellular carcinoma (HepG2), prostate cancer (PC3), and breast cancer (MCF-7). Meanwhile, the first in terms of VEGFR-2 inhibition was compound 15d which came second with regard to antitumor assay with IC50 = 24.10, 40.90, and 33.40 μM against aforementioned cell lines, respectively. Furthermore, Compound 15d increased apoptosis rate of HepG2 from 1.20 to 12.46% as it significantly increased levels of Caspase-3, BAX, and P53 from 49.6274, 40.62, and 42.84 to 561.427, 395.04, and 415.027 pg/mL, respectively. Moreover, 15d showed IC50 of 253 and 381 nM against HER2 and FGFR, respectively.
Synthesis and pharmacological evaluation of piperidine (piperazine)-amide substituted derivatives as multi-target antipsychotics
Huang, Ling,Gao, Lanchang,Zhang, Xiaohua,Yin, Lei,Hu, Jintao,Song, Ting,Chen, Yin
, (2020/09/01)
We report the optimisation of a series of novel amide-piperidine (piperazine) derivatives using the multiple ligand approach with dopamine and serotonin receptors. Of the derivatives, compound 11 exhibited high affinity for the D2, 5-HT1A, and 5-HT2A receptors, but low affinity for the 5-HT2C and histamine H1 receptors and human ether-a-go-go-related gene (hERG) channels. In vivo, compound 11 reduced apomorphine-induced climbing, MK-801-induced hyperactivity and DOI-induced head twitching without observable catalepsy, even at the highest dose tested. In addition, it exhibited suppression in a CAR test. Furthermore, in a novel object recognition task, it displayed procognition properties. Therefore, compound 11 is a promising candidate multi-target antipsychotic.