Being an axial chiral compound with optical activity, 2,2'-naphthol (BINOL) has become one of the basic units for constructing various chiral fluorescent chemosensors in recent years. According to the literatures, chiral BINOL derivatives chemosensors carry out highly enantioselective, sensitive recognition of amino acid and its derivatives, chiral amino alcohols, and α-hydroxycarboxylic acids. In this progress, BINOL derivatives as enantioselective chemosensors for chiral enantiomers are summarized.

Nine novel naphthalimide-polyamine conjugates were synthesized and their structures were confirmed by elemental analysis, 1 H NMR, 13 C NMR and MS techniques. Their antitumor activities in vitro using MTT [3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] assay were assessed on leukemia cells (K562), human breast cancer cells (MB-231) and human hepatoma cells (7721). The results showed that most of them exhibited antitumor activities. Especially, compound 5a was better than amonafide which has been in phase III clinical trials. Fluorescence data revealed that the fluorescence quenching of herring sperm DNA-EB complex by compound 5a was a static quenching type and naphthalimide-polyamine conjugates intercalate into the DNA base pairs.

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With the aim of obtaining potential antitumor candidates with more efficiency and more economic value. 40 2,4,6-trisubstituted pyrimidine derivatives bearing chalcone moiety were synthesized via cyclization, chlorination, substitution with benzoylacetate and ethylacetoacetate as the starting materials. The structures of target products were confirmed by 1 H NMR, I3 C NMR and HRMS. 2,4,6-Trisubstituted pyrimidine derivatives bearing chalcone moiety were evaluated for anticancer activity on four human cancer cell lines including EC-109, MGC-803, HepG-2 and MDA-MB-231 by CCK-8 (cell counting Kit-8) assay. Among them, (E)-1-(4-((2-(((1H-benzo[d]imidazol-2-yl)methyl)thio)-6-methylpyrimidin-4-yl)amino)phenyl)-3-(3,4,5-trimethoxyphenyl)prop-2-en-1-one (13u) were more cytotoxic against MGC-803 and MDA-MB-231 cell lines, with IC 50 values of 0.99 and 1.77 μmol•L-1 , respectively.