769922-77-2Relevant articles and documents
Design and synthesis of a new series of 3,5-disubstituted-1,2,4-oxadiazoles as potential colchicine binding site inhibitors: Antiproliferative activity, molecular docking, and SAR studies
Abdel-Aal, Eatedal H.,Abdel-Sami, Zakaria K.,Abo-Dya, Nader E.,Al-Karmalawy, Ahmed A.,Diab, Rana T.
, p. 21657 - 21669 (2021/12/09)
The development of anticancer compounds targeting the colchicine-binding site of tubulin, termed colchicine-binding site inhibitors (CBSIs) is a promising research area for pharmaceutical companies and research institutes. A series of 3,5-disubstituted 1,
A simple and versatile method to synthesize N-acyl-benzotriazoles
Laconde, Guillaume,Amblard, Muriel,Martinez, Jean
supporting information, p. 341 - 343 (2019/01/04)
An efficient method for the synthesis of N-acyl-benzotriazoles from a wide variety of protected amino acids, as well as from compounds frequently used in drug discovery such as biotin and N-Fmoc polyethylene glycol, has been developed. The reaction of car
Synthesis, molecular docking and anticancer studies of peptides and iso-peptides
Jabeen, Farukh,Panda, Siva S.,Kondratyuk, Tamara P.,Park, Eun-Jung,Pezzuto, John M.,Ihsan-Ul-Haq,Hall, C. Dennis,Katritzky, Alan R.
supporting information, p. 2980 - 2984 (2015/06/22)
Chiral peptides and iso-peptides were synthesized in excellent yield by using benzotriazole mediated solution phase synthesis. Benzotriazole acted both as activating and leaving group, eliminating frequent use of protection and subsequent deprotection. The procedure was based on the hypothesis that epimerization should be suppressed in solution due to a faster coupling rate than SPPS. All the synthesized peptides complied with Lipinski's Ro5 except for the rotatable bonds. Inhibition of cell proliferation of cancer cell lines is one of the most commonly used methods to study the effectiveness of any anticancer agents. Synthesized peptides and iso-peptides were tested against three cancer cell lines (MCF-7, MDA-MB 231) to determine their anti-proliferative potential. NFkB was also determined. Molecular docking studies were also carried out to complement the experimental results.