Nicotinamide Phosphoribosyltransferase Inhibitors, Design, Preparation, and Structure-Activity Relationship was written by Christensen, Mette K.;Erichsen, Kamille D.;Olesen, Uffe H.;Tjoernelund, Jette;Fristrup, Peter;Thougaard, Annemette;Nielsen, Soeren Jensby;Sehested, Maxwell;Jensen, Peter B.;Loza, Einars;Kalvinsh, Ivars;Garten, Antje;Kiess, Wieland;Bjorkling, Fredrik. And the article was included in Journal of Medicinal Chemistry in 2013.Quality Control of N-(5-Bromopentyl)phthalimide This article mentions the following:
Existing pharmacol. inhibitors for nicotinamide phosphoribosyltransferase (NAMPT) are promising therapeutics for treating cancer. By using medicinal and computational chem. methods, the structure-activity relationship for novel classes of NAMPT inhibitors is described, and the compounds are optimized. Compounds are designed inspired by the NAMPT inhibitor APO866 and cyanoguanidine inhibitor scaffolds. In comparison with recently published derivatives, the new analogs exhibit an equally potent antiproliferative activity in vitro and comparable activity in vivo. The best performing compounds from these series showed subnanomolar antiproliferative activity toward a series of cancer cell lines (compound 15: IC50 0.025 and 0.33 nM, in A2780 (ovarian carcinoma) and MCF-7 (breast), resp.) and potent antitumor in vivo activity in well-tolerated doses in a xenograft model. In an A2780 xenograft mouse model with large tumors (500 mm3), compound 15 reduced the tumor volume to one-fifth of the starting volume at a dose of 3 mg/kg administered i.p., bid, days 1-9. Thus, compounds found in this study compared favorably with compounds already in the clinic and warrant further investigation as promising lead mols. for the inhibition of NAMPT. In the experiment, the researchers used many compounds, for example, N-(5-Bromopentyl)phthalimide (cas: 954-81-4Quality Control of N-(5-Bromopentyl)phthalimide).
N-(5-Bromopentyl)phthalimide (cas: 954-81-4) belongs to organobromine compounds. Bromine is more electronegative than carbon (2.9 vs 2.5). Consequently, the carbon in a carbon–bromine bond is electrophilic, i.e. alkyl bromides are alkylating agents. Commercially available organobromine pharmaceuticals include the vasodilator nicergoline, the sedative brotizolam, the anticancer agent pipobroman, and the antiseptic merbromin. Quality Control of N-(5-Bromopentyl)phthalimide
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary