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Twenty phenylpropenamide analogs with structural novelty were designed and synthesized upon pharmacophore-combination strategy. The structures of target compounds were elucidated by IR, 1H NMR, 13C NMR and MS, and all the target compounds were biologically evaluated for the inhibitory activities of platelet aggregation induced by adenosine diphoshate（ADP） and（AA） arachidonic acid via Bron method. As a result, compounds 6b, 9b, 9d and 9h demonstrated potent inhibitory activity against platelet aggregation induced by AA. Meanwhile, compounds 6b, 6d, 6j, 9b and 9g exhibited significant suppression of platelet aggregation induced by ADP.

To discover novel antitumor rhodanine unsaturated ketones, a series of fluoroquinolone (rhodanine α, β-unsaturated ketone) amine derivatives (5a-5r) were designed and synthesized with fluoroquinolone amide scaffold as a carrier. The structures of eighteen title compounds were characterized by elemental analysis, 1H NMR and MS. The in vitro anti-proliferative activity against Hep-3B, Capan-1 and HL60 cells was evaluated by MTT assay. The results showed that the title compounds not only had more significant anti-proliferative activity against three tested cancer cell lines than that of the parent ciprofloxacin 1, but also exhibited the highest activity against Capan-1 cells. The SAR revealed that some compounds carrying aromatic heterocyclic rings or phenyl attached to an electron-withdrawing carboxyl or sulfonamide substituent were comparable to or better than comparison doxorubicin against Capan-1 cells. As such, it suggests that fluoroquinolone (rhodanine α, β-unsaturated ketone) amines are promising leads for the development of novel antitumor fluoroquinolones or rhodanine analogues.

It has been demonstrated by our previous research that 4-(2-acetoxybenzoylamino) butyramide derivatives exhibited good antiepileptic activities. In this paper, to explore the SAR and improve the antiepileptic activities of these derivatives, a series of novel 4-(2-acetoxybenzoylamino) butyramide heterocyclic compounds (5a-5n) were synthesized and biologically evaluated. Their structures were confirmed by 1H MNR, ESI-MS and elemental analysis. Pharmacological test in vivo showed that target compounds (5f, 5i-5n) displayed strong antiepileptic activities on 4-AP induced epilepsy in mice with ED50 values ranging from 0.3137 to 0.3604 mmol x kg(-1).

To explore new agents of gamma-aminobutyric acid (GABA) derivatives with more potent antiepileptic activity, a series of 4-(2-acetoxybenzoylamino) butyramide derivatives were designed and synthesized. All of the novel compounds (5a-51) were synthesized from GABA as starting material, and their structures were confirmed with IR, 1H NMR, EI-MS and elemental analysis. Preliminary pharmacological test in vitro showed that all target compounds displayed strong antiepileptic activities and were worth for further study. The structure-activity relationship of 4-(2-acetoxybenzoylamino) butyramide derivatives was also discussed preliminarily.

N, N'-bis(2-pyridinecarboxamide)-1,2-ethane(H2L1), N, N'-bis(2-pyridinecarboxamide)-1, 2-beneze(H2L2) and N-phenylpyridine-2-carboxamide(HL3) were synthesized, and characterized by elemental analysis, IR and HNMR spectra. UV-visible (UV-Vis) spectra, fluorescence spectra and SERS spectra to study the interaction of the three ligands with calf thymus DNA. UV-visible (UV-Vis) spectra show that with the incremental addition of DNA, the bands of H2L1, H2L2 and HL3 all show Hypochromism. Meanwhile fluorescence spectra show that the addition of the three ligands to DNA pretreated with EB causes an appreciable reduction in fluorescence intensity, indicating that the ligands compete with ethidium bromide in binding to DNA, and free ethidium bromide increases. The addition of DNA causes the SERS signals of the ligands to weakened and some bands to disappeared. Based on the above experimental results, we conclude that the three ligands bind to DNA mainly through the intercalation mode. The binding constant of the three compouds Kb was calculated, 1.20 x 10(4) for H2L1, 1.33 x 10(4) for H2L2 and is 1.52 x 10(4) for HL3. Kr was also calculated to be 0.67, 1.52 and 1.73 for H2L1, H2L2 and HL3, respectively. The value indicates that the binding of HL3 to DNA is stronger than that of H2L1 and H2L2, as HI3 has proper planar structure, smaller molecular volume and less steric hindrance. The three ligands can all induce the cleavage of plasmid pBR322 DNA. An increase in H2L1, H2L2 and HL3 concentrations causes more transformation of plasmid DNA from closed circular conformations to nicked conformations. But linear conformations have not been observed. The cleavage of plasmid pBR322 DNA caused by the three ligands is not selective.

In the present paper, citric acid, acetic anhydride, polyethyleneoxide nonyl phenyl ether and diethanolamine were used as raw materials. The raw materials were purified, and the intermediate products were synthesized. Finally, the citric acid mono polyethyleneoxide nonyl phenyl ether amber diehylene glycol dinitrate diglycollic amide was made. The acidamide of the product synthesized was determined by IR. There is a characteristic peak of C=O in acidamide at 1 642.39 cm(-1). Using potassium rhodanate as a internal standard, and according to Lambert-Beer law, a method to determine the citric acid mono polyethyleneoxide nonyl phenyl ether amber diehylene glycol dinitrate diglycollic amide was developed. The linear regression equation is A = 0.007 6m+0.325 6 with a correlation coefficient (r2) of 0.998 9. The experimental results of the precisions and recoveries are satisfied. The method is very necessary for confirming the reaction extent and controlling quality of citric acid mono polyethyleneoxide nonyl phenyl ether amber diehylene glycol dinitrate diglycollic amide. So, the synthesis process conditions were right according to the IR data.

In the present paper, citric anhydride was made using citric acid. The citric acid mono-polyethyleneoxide nonyl phenyl ether was synthesized by using citric anhydride and polyethyleneoxide nonyl phenyl ether. Finally, the citric acid mono-polyethyleneoxide nonyl phenyl ether amber diehylene glycol dinitrate diglycollic amide was synthesized by using diethanolamine. The raw material, intermediate and product were characterized by IR. The two absorption peaks at 1866.90 cm(-1) and 1781.08 cm(-1) respectively are both strong, with the latter stronger than the former. It was indicated that citric acid had changed into citric anhydride. The absorption peak at 1736.14 cm(-1) is attributable to the stretching vibration of C==O in ester, and that at 1642.39 cm(-1) is attributable to the stretching vibration of C==O in acidamide. It was indicated that the product was citric acid mono-polyethyleneoxide nonyl phenyl ether amber diehylene glycol dinitrate diglycollic amide. So, the synthesis process conditions were right according to the IR data.

Aim: To design and synthesize new arylsubstituted imidazolin-2-one analogues as antitumor compounds., Methods: Arylsubstituted imidazolin-2-ones were prepared by condensation the appropriate omega-amino-acetophenone hydrochloride with arylisocyanate in toluene. The target compounds prepared in this study were tested for cytotoxicity against PC-3, A549, HO-8910, Hela, HL60, K562 and HL60R cancer cell lines, and mechanism of one of the products 4y was further evaluated with its mechanium., Results: Thirty-six new compounds were synthesized and confirmed by 1H NMR, MS and elemental analysis. One of the synthesized products, compound 4y, displayed an encouraging selective activity against HL60 cells, and it was partlydue to the cell cycle arrest and cell apoptosis., Conclusion: Compound 4y is worthy to be intensively studied.

Aim: To explore the synthetic methods of polypeptides containing new heart of kidney imaging agents., Methods and Results: Five new target chelators--2-N-(2'-s-triphenylmethylacetyl) amino-(N'-2"-N",N"-diethylethylamine) phenylpropamide (MPNE), 2-N-(2'-s-triphenylmethyl acetyl) amino-(N'-2"-N",N"-dimethylethylamine) phenylpropamide (MPNM), 2-N-(2's-triphenylmethylacetyl) amino-3-methyl-(N'-2"-N",N"-dimethylethylamine) butyramide (MVNM), 2-N-(2'-s-triphenyl methylacetyl) amino-3-methyl-(N'-2"-N",N"-diethylethylamine) butyramide (MVNE), 2-N-(2'-s-triphenylmethylacetyl) amino-(N'-acetylglycine) phenylpropamide (MPG2)--were synthesized through five steps with mercaptoacetic acid as primitive materials, all of which were identified on the basis of spectroscopic data, such as IR, 1HNMR, MS or elementary analysis. The protection of the mercapto group was improved and the relatively new reaction condition of active ester with amino acid is developed. All the chelators were labeled with Technetium-99m and their biological activities in mice given in ID values was tested to explore new heart imaging agents, where ID is the percentage injected dose per organ. The ID was determined by in vivo biodistribution study. Tc-99m complexes 0.1 mL was injected into the laterial tail vein of 3 anaesthetised rats. At 2, 5, 10, 30, 60 min post-injection, rats were sacrificed by decapitation, bled from the neck and dissected. Organs were removed at dissection. The radioactivities in various organs were determined in an automatic twin crystal gamma counter., Conclusion: The bio-distribution results in mice indicate that 99Tcm-MVNM have higher heart uptake (ID = 8.40%/g, 2 min post-injection) and quicker blood clearance (ID = 4.3%/g, 60 min post-injection); 99Tcm-MPNE and 99Tcm-MPNM also have fairly high heart uptake and quick blood clearance; 99Tcm-MPG2 has better kidney accumulation and higher activity ratios of kidney to blood (about 4).

In search for cancer chemoprevention agents, seven new amide compounds have been synthesized. The structures have been determined based on spectral and chemical data. N-4-(ethoxycarbophenyl)-alpha-naphthamide and N-4-(ethoxycarbophenyl)-beta-naphthamide were shown to be 81% and 79% effective, respectively, for inducing different in HL-60 human promyelocytic leukemia cells at the concentration of 10(-5) mol/L in NBT tests.

In searching for new chelation therapy drugs against uranium intoxication, a series of N-carboxymethyl-N-(substituted carbamoylmethyl)-2,3-dihydroxy-4-carbomethoxybenzylamine was synthesized starting with o-vanillin. The effect on detoxication of UO2(NO3)2, CuSO4 and NiCl2 in mice was tested. Some of them (IVa, IVd, IVf and IVg) were shown to be good antidotes for acute uranium intoxication, but all were less effective for Cu2+ and Ni2+.

Podocarpamide, isolated from the bark of Zanthoxylum podocarpum Hemsl., is a new compound with platelet aggregation inhibiting and SGPT level lowering activities. Its structure was inferred to have two possible forms, either I or II, from its spectra. The structure of podocarpamide was identified as I by synthesis.