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Zhongshan, China

Liao S.-R.,Chinese Academy of Sciences | Qin X.-C.,Guangzhou Institutes of Biomedicine and Health | Wang Z.,Guangzhou Institutes of Biomedicine and Health | Li D.,Sun Yat Sen University | And 4 more authors.
European Journal of Medicinal Chemistry | Year: 2016

A series of novel N-1-monoallylated 2,5-diketopiperazine derivatives were designed, synthesized, and evaluated as cytotoxic agents against eight cancer cell lines by using CCK8 assay. These derivatives were substituted with methoxyphenyl groups at C-6 position, and various long alkyl side chains at C-3-position of the 2,5-diketopiperazine ring. The cytotoxic results showed that 4-methoxyphenyl group was better than 2-methoxyphenyl group as optimal substitutive group, while 3-methoxyphenyl group was not a suitable one. When the number (n value) of the methylene groups for the long alkyl side chain was 3 (compounds 1c and 3c), the derivatives had the strongest cytotoxicities. Compound 3c substituted with 4-methoxyphenyl group and pentylidene side chain exhibited strong activity (IC50=0.36-1.9 μM) against all cancer cell lines, and could obviously induce apoptosis of cancer cell line U937 at 1.0 μM after 48 h treatment. © 2016 Elsevier Masson SAS.

Li Y.,CAS Shanghai Institute of Organic Chemistry | Zhou Y.,Enantiotech Corporation | Shi Q.,CAS Shanghai Institute of Organic Chemistry | Ding K.,CAS Shanghai Institute of Organic Chemistry | And 2 more authors.
Advanced Synthesis and Catalysis | Year: 2011

Readily available and modular hybrid amine/benzimidazole-based 1H-benzimidazole-2-methanamine (BIMA) ligands in combination with 2,3-O-isopropylidene-2,3-dihydroxy-1,4-bis(diphenylphosphino)butane (DIOP) afford efficient catalytic systems for the ruthenium(II)-catalyzed asymmetric hydrogenation (AH) of a number of aryl ketones. The AH proceeds smoothly with substrate-to-catalyst (S/C) molar ratios of up to 100,000 (TOF of 6500ah -1, 8aatm) giving chiral alcohols in up to 99% ee. © 2011 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.

Sun M.,Anhui Medical University | Lv N.,Anhui Medical University | Li Z.,Anhui Medical University | Xiong Q.,Anhui Medical University | And 2 more authors.
Journal of the Iranian Chemical Society | Year: 2016

Expanding our studies on the anti-angiogenesis activities of 2,4-disubstituted quinazoline derivatives [8], a series of novel N-(2-(quinazolin-2-yl)phenyl)benzamide (SZ) derivatives were designed and synthesized. Cytotoxicity assays indicated that most of these compounds displayed similar cytotoxicity against tumor cells in comparison with our previously reported, but showed a higher cytotoxicity against HUVECs. The SZ derivatives showed a remarkable inhibitive effect against the migration and adhesion of HUVECs, in addition to demonstrating significant in vivo anti-angiogenesis activities in the chick embryo chorioallantoic membrane (CAM) assay. The results proved that the introduction of an aryl group with a basic amide side chain on the 4′ position linked to the amide of the C-2 substituted quinazoline scaffold is an effective approach to improve the anti-angiogenic activity of quinazoline derivatives. © 2015 Iranian Chemical Society.

Matsuoka A.,Nagoya University | Sandoval C.A.,Enantiotech Corporation | Uchiyama M.,RIKEN | Uchiyama M.,University of Tokyo | And 2 more authors.
Chemistry - An Asian Journal | Year: 2015

The global reaction route mapping (GRRM) methods conveniently define transition states in asymmetric hydrogenation and transfer hydrogenation of aromatic ketones via the [RuH{(S,S)-TsNCH(C6H5)CH(C6H5)NH2}(η6-pcymene)] intermediate. Multiple electrostatic CH/π interactions are the common motif in the preferred diastereometric structures. © 2015 Wiley-VCH Verlag GmbH & Co. KGaA, Weinheim.

Liao S.,CAS South China Sea Institute of Oceanology | Xu Y.,Shenzhen University | Tang Y.,CAS South China Sea Institute of Oceanology | Wang J.,CAS South China Sea Institute of Oceanology | And 3 more authors.
RSC Advances | Year: 2015

A small library of soluble 2,5-diketopiperazine derivatives were designed, synthesized and evaluated as antifouling agents against two species of marine organisms: Balanus amphitrite and Bugula neritina by larval attachment assay. The results showed that different derivatives had different antifouling activities. Among these compounds, 3a (EC50 = 2.5 μg mL-1), 3b (EC50 = 3.2 μg mL-1) and 3d (EC50 = 1.6 μg mL-1) had strong activities, and 2d (EC50 = 20.5 μg mL-1), 3l (EC50 = 25.0 μg mL-1) and 3m (EC50 = 18.5 μg mL-1) had moderate activities against Balanus amphitrite, but other compounds had no activities. Differently, compounds 3d (EC50 = 3.1 μg mL-1) and 3i (EC50 = 2.3 μg mL-1) exhibited strong activities, and 3a (EC50 = 11.3 μg mL-1) and 3c (EC50 = 17.2 μg mL-1) showed moderate activities against Bugula neritina, whereas other compounds had no activities. All of the active compounds had stronger antifouling activities than those of the natural product cyclo-(l-Phe-l-Pro). Compound 3d could be a new template molecule for further development as an antifouling agent because of its strong inhibitory activities against both species of fouling organisms with low or no toxicity to the environment. © The Royal Society of Chemistry 2015.

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