Cardoso, David S. P.; Kincses, Annamaria; Nove, Marta; Spengler, Gabriella; Mulhovo, Silva; Aires-de-Sousa, Joao; dos Santos, Daniel J. V. A.; Ferreira, Maria-Jose U. published an article on January 15 ,2021. The article was titled 《Alkylated monoterpene indole alkaloid derivatives as potent P-glycoprotein inhibitors in resistant cancer cells》, and you may find the article in European Journal of Medicinal Chemistry.Safety of 3-Chlorobenzylchloride The information in the text is summarized as follows:
Aiming at generating a series of monoterpene indole alkaloids with enhanced multidrug resistance (MDR) reversing activity in cancer, two major epimeric alkaloids isolated from Tabernaemontana elegans, tabernaemontanine and dregamine, were derivatized by alkylation of the indole nitrogen. Twenty-six new derivatives were prepared by reaction with different aliphatic and aromatic halides, whose structures were elucidated mainly by NMR, including 2D NMR experiments Their MDR reversal ability was evaluated through a functional assay, using as models resistant human colon adenocarcinoma and human ABCB1-gene transfected L5178Y mouse lymphoma cells, overexpressing P-glycoprotein (P-gp), by flow cytometry. A considerable increase of activity was found for most of the derivatives, being the strongest P-gp inhibitors those sharing N-phenethyl moieties, displaying outstanding inhibitory activity, associated with weak cytotoxicity. Chemosensitivity assays were also performed in a model of combination chemotherapy in the same cell lines, by studying the in vitro interactions between the compounds and the antineoplastic drug doxorubicin. Most of the compounds have shown strong synergistic interactions with doxorubicin, highlighting their potential as MDR reversers. QSAR models were also explored for insights on drug-receptor interaction, and it was found that lipophilicity and bulkiness features were associated with inhibitory activity, although linear correlations were not observed After reading the article, we found that the author used 3-Chlorobenzylchloride(cas: 620-20-2Safety of 3-Chlorobenzylchloride)
3-Chlorobenzylchloride(cas: 620-20-2) has been used in the reaction of 3-methoxybenzyl chloride and ethyl 4-bromobenzoate in pure water, using zinc dust and a Pd catalyst.Safety of 3-Chlorobenzylchloride
Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics