953724-33-9Relevant academic research and scientific papers
Synthesis, In Vitro Antiproliferative Activity, and In Silico Studies of New Anilinoquinazoline Derivatives as Potential AntitumorAgents
Abdulwahab,Dzulkeflee,Han,Ruslan,Leong,Heh,Ariffin
, p. 2410 - 2418 (2021/02/12)
Abstract: A series of anilinoquinazoline derivatives with modification on the 2nd carbon of the aniline ring has been synthesized and characterized. The compounds have been tested for their in vitro antiproliferative activity against three NSCLC cell lines, including A549, H1650 and H1975. One of the products has demonstrated the highest IC50 value against A549 (17.60 ± 1.70 μM), surpassing the standard drug, gefitinib (34.32 ± 1.30 μM), another one has exhibited IC50 value against H1975 (9.75 ± 1.06 μM), surpassing gefitinib (31.12 ± 0.38 μM). The best performing derivatives in the antiproliferative assay have been selected for further in silico study for investigating their plausible binding mode in different EGFR kinases through molecular docking and molecular dynamics simulations.
Anthranilic sulfonamide CCK1/CCK2 dual receptor antagonists I: Discovery of CCKR1 selectivity in a previously CCKR2-selective lead series
Pippel, Marna,Allison, Brett D.,Phuong, Victor K.,Li, Lina,Morton, Magda F.,Prendergast, Clodagh,Wu, Xiaodong,Shankley, Nigel P.,Rabinowitz, Michael H.
scheme or table, p. 6373 - 6375 (2010/04/30)
A series of CCK2R-selective anthranilic amides is shown to derive CCK1R affinity via selective substitution of the amide side chain. Thus, extending the length of the original benzamide side chain by a single methylene unit imparts CCK1R affinity to the s
