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1.
Neutron irradiation of Cp2MoCl2 for 24 h afforded the radiotracer Cp299MoCl2 which was characterised by UV–Vis spectroscopy and thin layer chromatography. Binding experiments with the thiol containing protein human serum albumin (HSA) or calf thymus DNA, were monitored for 99Mo using a gamma counter. Under the conditions investigated, molar ratios of binding of 0.2:1 (Cp2MoCl2:DNA) and 9.4:1 (Cp2MoCl2:HSA) were calculated. The results are consistent with in vitro coordination studies that have shown strong preferential interaction of Cp2MoCl2 with thiols versus other donor sites in biomolecules including DNA.  相似文献   
2.
碳铂类似物的合成,表征及对大鼠W—256肉瘤的抑制作用   总被引:2,自引:0,他引:2  
合成了十八种〔PtA_2X〕·yH_2O,其中A分别为NH_3、CH_3NH_2、1/2乙二胺和1/2(2,3-二甲基-2,3-丁二胺),X分别为1,1-环丙烷二羧酸根(CPrDCA)、2-甲-1,1-环丙烷二羧酸根(2-M-CPrDCA)、2-甲-1,1-环丁烷二羧酸根(2-M-CBDCA)、1,2-环戊烷二羧酸根(CPDCA)和1,1-环已烷二羧酸根(CHDCA),并进行了表征。测定了配合物抑制大鼠W-256肉瘤的活性,发现配合物〔Pt(NH_3)_2X〕系列按X不同有以下的活性次序:CPrDCA>2-M-CPrDCA>CPDCA>CBDCA(碳铂)≥2-M-CBDCA。  相似文献   
3.
A therapeutic method that selectively destroys malignant cells in the presence of normal cells is a highly valued goal of oncologists and the possible salvation of cancer patients afflicted with some incurable forms of the disease. Selective cell destruction is, in principle, possible with a binary therapeutic strategy based upon the neutron capture reaction observed with the 10B nucleus and a neutron of low kinetic energy (thermal neutron). This nuclear fission reaction produces both 4He and 7Li+ nuclei along with about 2.4 MeV of kinetic energy and weak γ-radiation. Since the energetic and cytotoxic product ions travel only about one cell diameter in tissue one may specify the cell type to be destroyed by placing innocent 10B nuclei on or within only the doomed cells. This article describes the current status of chemical research aimed at the eventual adoption of this therapeutic method (boron neutron capture therapy or BNCT). The multidisciplinary nature of this research effort involves chemistry, biology, nuclear physics, medicine, and related specialties. Methods devised for bringing 10B nuclei to tumor cells in therapeutic amounts are correlated with the structure of a generalized cell and the various cellular compartments available for boron localization. The synthesis methods employed for the creation of boron-containing biomolecules and drugs are presented along with representative data concerning their efficacy in tumor localization. The outlook for BNCT is especially bright at this time because of rapid developments in the fields of bioorganometallic chemistry, microbiology, immunology, and nuclear science, to name but a few. Very effective boron delivery vehicles have been demonstrated, and through the interaction of chemistry and biology these species are undergoing further improvement and evaluation of their suitability for BNCT.  相似文献   
4.
Zhigang Li  Xuhong Qian 《Tetrahedron》2005,61(36):8711-8717
Two kinds of thio-heterocyclic fused naphthalene carboxamides, 3a-b, 4a-b, were designed, synthesized and quantitatively evaluated as efficient antitumor and DNA photocleaving agents. Compound 3a or 3b, having the thiophene ring, intercalated into DNA more strongly than compound 4a or 4b, having the thioxanthene ring. Compound 4a or 4b, photocleaved DNA more efficiently than 3a or 3b via superoxide anion. Compound 4a was the strongest inhibitor for P388 (murine leukemia cell), while 3a was the most cytotoxic one against A549 (human lung cancer cell). Each new compound showed stronger DNA photocleaving activity than corresponding naphthalimide.  相似文献   
5.
卢水明  毛丽娟 《合成化学》1998,6(4):335-338
利用N,N-二(2-氯乙基)氨基磷酰二异氰酸酯和胺的加成反应,合成了2,4,6三氧-1,3,5,2三氮磷杂环己烷衍生物,它们的结构经^1HNMR,IR和元素分析所证实。初步生物活性测试结果表明,部分化合物具有一定的抗肿瘤活性。  相似文献   
6.
由2-氰-5-氟-3H-4-嘧啶酮和取代苯酚钠在常压下反应,合成了7个未见文献报道的2-芳氧基-5-氟-3H-4-嘧啶酮化合物,产率70 ̄87%,结构经IR、^1H NMR和MS证实。  相似文献   
7.
A convergent total synthesis of cis-solamin (1a) and its diastereomer (1b) was accomplished. A key reaction of this approach was the use of VO(acac)2-catalyzed diastereoselective epoxidation of (Z)-bis-homoallylic alcohol 3 followed by spontaneous cyclization for the cis-THF ring formation. By comparison of the optical rotation of the two possible diastereomers, it is suggested that the absolute configuration of natural cis-solamin is 1a. Inhibitory action of synthetic 1a and 1b with bovine heart mitochondrial complex I are reported.  相似文献   
8.
2',3'-O-异亚丙基-5'-O-[N,N-二(2-氯乙基)磷酰胺基]核苷的合成陈茹玉,迟国臣,陈小茹(南开大学元素有机化学研究所,天津,300071)关键词核苷,亚磷酰化,抗肿瘤活性很多核苷类化合物具有很好的抗肿瘤、抗病毒等生物活性,某些化合物已...  相似文献   
9.
Dibutyltin(IV) oxide reacts with the cantharidin analogue, 4′-(7-oxabicyclo [2,2,1]-5-heptane-2,3-dicarboximide) benzoic acid, A, to give the complexes [(p-C8H8NO3-C6H4-COOBu2Sn)2O]2 (1) and (p-C8H8NO3-C6H4-COO)2SnBu2 (2) which had been characterized by IR and 1H, 13C, 119Sn NMR. Single X-ray crystal structure analysis has been determined for compound (1), which was analogue to most other [(RCOOBu2Sn)2O]2. The dimer features central of Bu4Sn2O2 unit with the two Bu2Sn groups being linked via bridging oxygen atom. Each tin atom adopts distorted trigonal bipyramidal structures via two carbons from a dibutyl moiety and three oxygen atoms from cantharidin derivative and bridging oxygen atom. In vitro tests show compounds 1 and 2 exhibit high cytotoxicity against P388 and HL-60.  相似文献   
10.
符合经典构效关系的抗肿瘤铂类药物   总被引:3,自引:0,他引:3  
王联红  刘芸  苟少华  尤启冬 《化学通报》2003,66(12):828-836
综述了自顺铂、卡铂后符合经典构效关系的铂类抗肿瘤药物的发展概况,按载体配基和离去基团的结构特征进行了分类,总结了各类配合物的构效关系和临床进展,其中重点对手性二胺配体的铂(Ⅱ)配合物进行了介绍。并讨论了顺铂、卡铂、奥沙利铂的作用机理。  相似文献   
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