MULTIPLE SYNTHESIS OF SMALLPEPTIDE ANALOGS

Two peptide analogs H-Tyr-Thr-Pro-Arg-Lys-OH (1) and H-Tyr-Thr-Pro-Phe-Lys-OH (2) were prepared successfully by the technique of simultaneous multiple peptides synthesis(SMPS) on a single resin support. The profiles of HPLC and amino acid analysis indicated that the purity of 1 and 2 was satisfactory. The average yield(74.9％) of each peptide was reasonable. This new technique of SMPS offered significant savings not only in time but in many expensive reagents as well.

THE SYNTHESIS OF UNSYMMETRIC ANALOGS OF GOSSYPOL—6-O-METHYLGOSSYPOL

6—O—Mcthylgossypol (3) was obtained with the methods of synthesis for the first time.

Synthesis of F-alkylated MDP Analogs

Four F-alkylated muramyl dipeptides were synthesized by an efficient coupling reagent, Benzotriazol-1-yloxy-bis(pyrrolidino)carbo hexafluoro-phosphate(BBC)([1]).

SYNTHESIS OF ACYCLIC ANALOGS OF BENZOTRIAZOLE AND INDOLE NUCLEOSIDE CONTAINING PERFLUOROALKYL GROUP

1-[(2-hydroxyethoxy)methyl]benzotriazole and -indole containing perfluoroalkyl group have been synthesized.

Design,Synthesis and Biological Activities of Quinazoline Containing Sorafenib Analogs as Antitumor Agents

A series of novel sorafenib derivatives containing quinazoline moiety were designed and synthesized. Their anti-proliferative activities against HCT116 and HCT115 cell lines were evaluated using MTT assay. Most of the synthesized compounds showed significant cytotoxicity against the selected cell lines. These cytotoxicities were consistent with their inhibitory activity against the phosphorylation of c-Raf, MEK1/2 and ERK1/2. Compound GD-09 also showed much stronger anti-tumor activity than that of sorafenib in vivo by B16 melanoma xenograft model test.

Design and synthesis of novel coumarin analogs and their nematicidal activity against five phytonematodes

The presence of hydroxyl groups at the C4 and C7 positions in coumarin backbone has been proposed as a potential modification site for providing excellent bioactivity according to previous studies. A series of novel coumarin derivatives were rationally designed and synthesized by use of a complex catalytic system for a targeted modification at the above sites. These derivatives were assayed for nematicidal activity. As predicted, the derivatization enhanced the activity of the coumarins against five nematodes.Compounds 7b, 9a, 10 c and 11 c showed significant strong nematicidal broad spectrum activity against all tested nematodes. Compound 10 c was the most effective with the lowest LC50 values against Meloidogyne incognita（5.1 mmol/L）, Ditylenchus destructor（3.7 mmol/L）, Bursaphelenchus mucronatus（6.4 mmol/L）, Bursaphelenchus B. xylophilus（2.5 mmol/L） and Aphelenchoides besseyi（3.1 mmol/L）,respectively. A brief investigation on the structure–activity relationships（SAR） revealed that the targeted modification by a C7 hydroxyl was optimum compared with that of a C4 hydroxyl and that the coupling chain length was crucial for the nematicidal activity.

A solid phase approach to PDMP analogs: A general strategy for combinatorial library

The present work reports the first solid phase synthesis of biologically interesting D-threo-l-phenyl-2- decanoylamino-3-morpholino-l-propanol （D-threo-PDMP） derivatives. This synthetic strategy includes facile preparation of versatile azido intermediate （5） in a relatively short sequence and the subsequent derivatization of 5, which led to a series of sulfonamide, urea and heterocycle substituted PDMP analogs （10 and 10＇）. With this method, a 5280-member compound library has been successfully built by IRORI Nanokan system.

A platform of digital brain using crowd power

A powerful platform of digital brain is proposed using crowd wisdom for brain research,based on the computational artificial intelligence model of synthesis reasoning and multi-source analogical generating.The design of the platform aims to make it a comprehensive brain database,a brain phantom generator,a brain knowledge base,and an intelligent assistant for research on neurological and psychiatric diseases and brain development.Using big data,crowd wisdom,and high performance computers may significantly enhance the capability of the platform.Preliminary achievements along this track are reported.