In 2022,Perrone, Maria Grazia; Vitale, Paola; Miciaccia, Morena; Ferorelli, Savina; Centonze, Antonella; Solidoro, Roberta; Munzone, Cristina; Bonaccorso, Carmela; Fortuna, Cosimo Gianluca; Kleinmanns, Katrin; Bjoerge, Line; Scilimati, Antonio published an article in Pharmaceuticals. The title of the article was 《Fluorochrome Selection for Imaging Intraoperative Ovarian Cancer Probes》.Name: N-Boc-1,6-Diaminohexane The author mentioned the following in the article:
The identification and removal of all gross and microscopic tumor to render the patient disease free represents a huge challenge in ovarian cancer treatment. The presence of residual disease is an independent neg. prognostic factor. Herein, we describe the synthesis and the “”in vitro”” evaluation of compounds as cyclooxygenase (COX)-1 inhibitors, the COX-1 isoform being an ovarian cancer biomarker, each bearing fluorochromes with different fluorescence features. Two of these compounds N-[4-(9-dimethylimino-9H-benzo[a]phenoxazin-5-ylamino) butyl]-2-(3,4-bis(4-methoxyphenyl)isoxazol-5-yl)acetamide chloride (RR11) and 3-(6-(4-(2-(3,4-bis(4-methoxyphenyl)isoxazole-5-yl)acetamido)butyl)amino-6-oxohexyl)-2-[7-(1,3-dihydro-1,1-dimethyl-3-Et 2H-benz[e]indolin-2-yl-idene)-1,3,5-heptatrienyl]-1,1-dimethyl-3-(6-carboxilato-hexyl)-1H-benz[e]indolium chloride, 23 (MSA14) were found to be potent and selective inhibitors of cyclooxygenase (COX)-1 “”in vitro””, and thus were further investigated “”in vivo””. The IC50 values were 0.032 and 0.087 μM for RR11 and 23 (MSA 14), resp., whereas the COX-2 IC50 for RR11 is 2.4 μM while 23 (MSA14) did not inhibit COX-2 even at a 50 μM concentration Together, this represented selectivity index = 75 and 874, resp. Structure-based virtual screening (SBVS) performed with the Fingerprints for Ligands and Proteins (FLAP) software allowed both to differentiate highly active compounds from less active and inactive structures and to define their interactions inside the substrate-binding cavity of hCOX1. Fluorescent probes RR11 and 23 (MSA14), were used for preliminary near-IR (NIR) fluorescent imaging (FLI) in human ovarian cancer (OVCAR-3 and SKOV-3) xenograft models. Surprisingly, a tumor-specific signal was observed for both tested fluorescent probes, even though this signal is not linked to the presence of COX-1.N-Boc-1,6-Diaminohexane(cas: 51857-17-1Name: N-Boc-1,6-Diaminohexane) was used in this study.
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 groupsName: N-Boc-1,6-Diaminohexane
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