Patinote, Cindy; Deleuze-Masquefa, Carine; Kaddour, Kamel Hadj; Vincent, Laure-Anais; Larive, Romain; Zghaib, Zahraa; Guichou, Jean-Francois; Assaf, Mona Diab; Cuq, Pierre; Bonnet, Pierre-Antoine published an article in 2021. The article was titled 《Imidazo[1,2-a]quinoxalines for melanoma treatment with original mechanism of action》, and you may find the article in European Journal of Medicinal Chemistry.Reference of N-Boc-1,6-Diaminohexane The information in the text is summarized as follows:
The malignant transformation of melanocytes causes several thousand deaths each year, making melanoma an important public health concern. Melanoma is the most aggressive skin cancer, which incidence has regularly increased over the past decades. We described here the preparation of new compounds based on the 1-(3,4-dihydroxyphenyl)imidazo[1,2-a]quinoxaline structure. Different positions of the quinoxaline moiety were screened to introduce novel substituents in order to study their influence on the biol. activity. Several alkylamino or alkyloxy groups were also considered to replace the methylamine of our first generation of Imiqualines. Imidazo[1,2-a]pyrazine derivatives were also designed as potential minimal structure. The investigation on A375 melanoma cells displayed interesting in vitro low nanomolar cytotoxic activity. Among them, 9d (EAPB02303) is particularly remarkable since it is 20 times more potent than vemurafenib, the reference clin. therapy used on BRAF mutant melanoma. Contrary to the first generation, EAPB02303 does not inhibit tubulin polymerization, as confirmed by an in vitro assay and a mol. modelisation study. The mechanism of action for EAPB02303 highlighted by a transcriptomic anal. is clearly different from a panel of 12 well-known anticancer drugs. In vivo EAPB02303 treatment reduced tumor size and weight of the A375 human melanoma xenografts in a dose-dependent manner, correlated with a low mitotic index but not with necrosis. The experimental part of the paper was very detailed, including the reaction process of N-Boc-1,6-Diaminohexane(cas: 51857-17-1Reference of N-Boc-1,6-Diaminohexane)
N-Boc-1,6-Diaminohexane(cas: 51857-17-1) is a compound useful in organic synthesis used in the preparation of mixed self-assembled monolayers (SAMs) that resist adsorption of proteins using the reaction of amines with a SAM that presents interchain carboxylic anhydride groupsReference of N-Boc-1,6-Diaminohexane
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