348152-30-7Relevant academic research and scientific papers
Design, synthesis and biological evaluation of new series of hexahydroquinoline and fused quinoline derivatives as potent inhibitors of wild-type EGFR and mutant EGFR (L858R and T790M)
Shaheen, Mennatallah A.,El-Emam, Ali A.,El-Gohary, Nadia S.
, (2020/12/01)
New series of hexahydroquinoline and fused quinoline derivatives were designed and synthesized. The thirty seven new compounds were screened for in vitro antitumor activity against HepG2, HCT-116 and MCF-7 cancer cells. Results indicated that compounds 2e
1,4,5,6,7,8-Hexahydroquinolines and 5,6,7,8-tetrahydronaphthalenes: A new class of antitumor agents targeting the colchicine binding site of tubulin
El-Emam, Ali A.,El-Gohary, Nadia S.,Shaheen, Mennatallah A.
supporting information, (2021/06/14)
New series of 2-amino-1,4,5,6,7,8-hexahydroquinoline-3-carbonitriles 3a,b and 2-amino-5,6,7,8-tetrahydronaphthalene-1,3-dicarbonitriles 4a-h were synthesized and evaluated for their antitumor activity. In vitro antitumor screening of the new members again
Hypervalent Iodine(III)-Catalyzed Epoxidation of β-Cyanostyrenes
Mangaonkar, Saeesh R.,Singh, Fateh V.
, p. 4473 - 4486 (2019/11/21)
A convenient approach for the synthesis of β-cyanoepoxides is illustrated by iodine(III)-catalyzed epoxidation of electron-deficient β-cyanostyrenes, wherein the active catalytic iodine(III) species was generated in situ. The epoxidation of β-cyanostyrenes was performed using 10 molpercent PhI as precatalyst in the presence of 2.0 equivalents Oxone as an oxidant and 2.4 equivalents of TFA as an additive at room temperature under ultrasonic radiations. The β-cyanoepoxides were isolated in good to excellent yields in a short reaction time.
An Efficient One-pot Three-component Process for Synthesis of Perfluoroalkylated Quinolizines
Shen, Dandan,Xu, Yanjie,He, Dong,Han, Jing,Chen, Jie,Deng, Hongmei,Shao, Min,Zhang, Hui,Cao, Weiguo
, p. 524 - 532 (2016/06/01)
A facile multi-component process for the synthesis of perfluoroalkylated quinolizine derivatives was achieved using various arylidenemalononitriles, pyridine, and methyl perfluoroalk-2-ynoates as starting materials. Moderate yields were obtained under mil
Synthesis of Novel 4 H-Chromenes Containing a Pyrimidine-2-Thione Function in the Presence of Fe3O4 Magnetic Nanoparticles and Study of Their Antioxidant Activity
Khoobi, Mehdi,Ramazani, Ali,Hojjati, Zahra,Shakeri, Raheleh,Khoshneviszadeh, Mehdi,Ardestani, Susan Kaboudanian,Shafiee, Abbas,Foroumadi, Alireza,Joo, Sang Woo
, p. 1586 - 1595 (2015/10/29)
The aim of the present work was to search for identification of novel reactive oxygen species (ROS) scavengers by testing new fused chromenopyrimidinethiones, which was synthesized using Fe3O4 nanoparticles. The new compounds were also tested for their cytotoxic activity. The obtained results showed that the incorporated pyrimidinethione moiety significantly increase antioxidant activity. In conclusion, the study of the pharmacological properties of the new chromenopyrimidinethiones allowed establishing new structure-activity relationships for splitting antioxidant and cytotoxic activity of these compounds.
A PEG bridged tertiary amine functionalized ionic liquid exhibiting thermoregulated reversible biphasic behavior with cyclohexane/isopropanol: Synthesis and application in Knoevenagel condensation
Luo, Jun,Xin, Tantan,Wang, Yinglei
, p. 269 - 273 (2013/02/25)
A novel poly(ethylene glycol) bridged tertiary amine functionalized ionic liquid PEG800-DPIL(Cl) was synthesized. It can form a temperature driven reversible biphasic system with cyclohexane/isopropanol mixed solvent. This biphasic system was applied in Knoevenagel condensation up to 99%. PEG 800-DPIL(Cl) could be simply recovered and recycled for several runs.
Structure-based design of pyridopyrimidinediones as dipeptidyl peptidase IV inhibitors
Lam, Betty,Skene, Robert J.,Zhang, Zhiyuan,Stafford, Jeffery A.,Shi, Lihong,Gwaltney II, Stephen L.
, p. 6628 - 6631,4 (2012/12/12)
Dipeptidyl peptidase IV (DPP-4) inhibitors have been shown to enhance GLP-1 levels and thereby improve hyperglycemia in type II diabetes. From a small fragment hit, using structure-based design, we have discovered a new class of non-covalent, potent and s
Structure-activity relationship study of prion inhibition by 2-aminopyridine-3,5-dicarbonitrile-based compounds: Parallel synthesis, bioactivity, and in vitro pharmacokinetics
May, Barnaby C. H.,Zorn, Julie A.,Witkop, Juanita,Sherrill, John,Wallace, Andrew C.,Legname, Giuseppe,Prusiner, Stanley B.,Cohen, Fred E.
, p. 65 - 73 (2007/10/03)
2-Aminopyridine-3,5-dicarbonitrile compounds were previously identified as mimetics of dominant-negative prion protein mutants and inhibit prion replication in cultured cells. Here, we report findings from a comprehensive structure-activity relationship study of the 6-aminopyridine-3,5-dicarbonitrile scaffold. We identify compounds with significantly improved bioactivity (approximately 40-fold) against replication of the infectious prion isoform (PrPSc) and suitable pharmacokinetic profiles to warrant evaluation in animal models of prion disease.
