苟少华
研究领域为配位超分子化学、药物化学、精细化工品的研发
个性化签名
- 姓名:苟少华
- 目前身份:
- 担任导师情况:
- 学位:
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学术头衔:
博士生导师
- 职称:-
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学科领域:
化学工程基础学科
- 研究兴趣:研究领域为配位超分子化学、药物化学、精细化工品的研发
苟少华现为南京大学化学化工学院教授、博士生导师,国际超分子科学与技术会议国际组织委员,国家和江苏省新药评审咨询专家。主要研究领域为配位超分子化学、药物化学、精细化工品的研发。迄今已在国内外化学刊物上发表论文100余篇,授权国家发明专利4项,开发国家原二类新药6项和四类新药一项。主要成果如下:
1.基础研究主要成果采用独特的方法第一次将金属钠作为模板离子系统地应用至 Schiff 碱类的成环反应中,由此得到了一些其它方法难以得到的新型大环,并以大环双核金属基团为基元开展了有关分子自组装方面的研究。设计和合成了多个系列的功能配体,在金属离子导致的配位自组装方面开展了系统的研究工作。
2.应用基础成果设计和制备了上百个新型铂类配合物,开展了体外和体内实验,已筛选出数个与顺铂或奥沙利铂活性相当的治疗肺癌和结直肠癌铂的化合物,已申请国家发明专利多项,目前正在开展毒理方面的研究,为进一步获得具有自主知识产权的铂类抗肿瘤新药打下了基础。此外还研发了具有绿色环保特性的酚类化合物的硝化技术,已申请了国家发明专利。
3. 应用成果开发了原国家四类新药奥沙利铂,原国家二类新药庚铂、依达拉奉、帕珠沙星、蓓沙罗叮、氯法他滨和度洛西丁等,有的已获新药证书,其中奥沙利铂已创造了六亿多元的产值和销售额。此外领导的课题组还为江苏省地方企业开发了数个精细化工产品,如医药和农药中间体等,已实现了产业化。
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2530
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成果阅读
596
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成果数
15
【期刊论文】Novel cisplatin-type platinum complexes and their cytotoxic activity
苟少华, Kai Cui, Lianhong Wang, Haibin Zhu, Shaohua Gou*, and Yun Liu
Bioorg. Med. Chem. Lett. 16(2006)2937-2942,-0001,():
-1年11月30日
A series of novel cisplatin-type platinum complexes, formulated as [PtA2(OCOCH2OR)2] (A2 = two monoamines or one diamine, R is an alkyl group), were designed, characteristic of alkoxyacetate as carboxylato ligands. The pertinent compounds were prepared and characterized by elementary analyses, IR, 1H NMR, and ESI-MS spectra. The cytotoxic activities of compound 1a in vitro toward HL-60 human leukemia and BEL-7402 human hepatocellular carcinoma cell lines were pioneeringly studied. Then, compounds 1b-3d were evaluated for their in vitro cytotoxicity against Ramos human lymphoma, 3AO human ovarian carcinoma, and A549 human non-small cell lung cancer cell lines. Most of them showed better cytotoxic activity than carboplatin against above selected cell lines.
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【期刊论文】Self-assembly directed by dinuclear zinc(II) macrocyclic species
苟少华, Wei Huang, Hai-Bin Zhu, Shao-Hua Gou∗
Coordination Chemistry Reviews 250(2006)414-423,-0001,():
-1年11月30日
Supramolecular compounds assembled by dinuclear zinc(II) species containing Robson-type macrocycles and diverse organic subunits (4,4 -bipyridine, 2,2 -bipyridine, pyrazine, 4-aminopyridine, 4-pyridinecarboxylate, pyridine, and quinoline) are reviewed. Various structural motifs such as molecular ladder, molecular ladder element and so forth have been generated. Structural attributes associated with each motif will be elucidated based on unambiguous single crystal X-ray analysis. Hydrogen bonding especially of the non-classical type, involved in the assembly are also discussed because of its crucial impact on the architecture of the final product.
Self-assembly, Coordination bond, Hydrogen bond, Dinuclear zinc(, II), , Macrocycle
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苟少华, Haibin Zhu, Kai Cui, Lianhong Wang, and Shaohua Gou*
Bioorg. Med. Chem. Lett. 15(2005)4936-4943,-0001,():
-1年11月30日
Twenty-six new hydrophilic chiral 2-alkoxy-1,4-butanediamine platinum (II) complexes having a seven-membered ring structure between a bidentate carrier ligand and a platinum atom have been synthesized and most of them were evaluated for their in vitro cytotoxicity toward A549 human non-small cell lung carcinoma and HCT-116 human colon cancer cell lines. The cytotoxicities of platinum complexes are related to the nature of the carrier ligand and leaving group. Complex 50b, viz. cis-dichloro[(2R)-ethoxy-1,4-butanediamine] platinum (II), exhibits the greatest potency among those 21 tested platinum complexes in both cell lines.
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苟少华, Lianhong Wang, Shaohua Gou, *, Yongjiang Chen, and Yun Liu
Bioorg. Med. Chem. Lett. 15(2005)3417-3422,-0001,():
-1年11月30日
Abstract-Eight new camphorato platinum complexes have been synthesized and evaluated for their in vitro cytotoxicity against HL-60 human leukemia, 3AO human ovarian carcinoma, BEL-7402 human hepatocarcinoma, and A549 human lung carcinoma cell lines. Most complexes showed good cytotoxic activity against the above-selected cell lines. Among the complexes, two compounds were assayed for their in vivo antitumor activity against LS-174T human colon carcinoma cells implanted in mice. One complex exhibited not only higher in vivo antitumor activity, but also less toxicity than oxaliplatin when it was administered intravenously at a dose of 6mg/kg three times.
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苟少华, Haibin Zhu, Chunhui Huang, Wei Huang, Shaohua Gou*
Inorganic Chemistry Communications 7(2004)1095-1099,-0001,():
-1年11月30日
A novel 1D neutral coordination polymer, {[Cu(dtmp)(dmf)Cl2]dmf}n (1) (dtmp=1,6-di(triazole-1-yl-methyl)-4-methylphenol, dmf=dimethyl formamide) was synthesized by reacting CuCl2 Æ 2H2O with the dtmp ligand. The crystal and molecular structure of the complex was determined by X-ray diffraction, in which the coordination geometry around the copper center is slightly distorted trigonal bypyramidal. One-dimensional chains have been formed through the metal and the ligand via oordination bonds, which are assembled further into a two-dimensional network by inter-chain synergic π-π stacking and hydrogen bonding.
1D coordination polymer, Crystal structure, π-π stacking, Hydrogen bonding
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苟少华, Hai-Bin Zhua, Zhen-Ya Daib, Wei Huanga, Kai Cuia, Shao-Hua Goua, b, *, Cheng-Jian Zhub
Polyhedron 23(2004)1131-1137,-0001,():
-1年11月30日
Several chiral copper(II) complexes of optically active Schiff bases (R,R)-4a-c, which have central seven-membered chelate rings, have been synthesized and characterized. X-ray single crystal analysis of a typical compound indicated that the complex is monomeric and the geometry around the metal atom is very distorted tetrahedral. All the complexes have been tested as catalysts for asymmetric oxidation of methyl phenyl sulfide. The mechanism of the catalytic reaction in the presence of these complexes has been tentatively elucidated.
Asymmetric oxidation, Chiral copper(, II), complexes, Schiff base, Sulfide, Seven-membered
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【期刊论文】Assembly of Seven Nickel(II) Metals by Chiral, Salen-Type Ligands with μ3-OH Bridges
苟少华, Xuan Xu, [a], Shaohua Gou, *[a], Wei Huang, Yonglin Ma, and Yizhi Li[a]
Eur. J. Inorg. Chem. 2003, 2054-2057,-0001,():
-1年11月30日
A chiral heptanuclear nickel(II) complex [NiII(NiII 2L)3(μ3-OH)2]·3H2O [H4L=(2R,3R)-1,4-bis(3,5-di-tert-butylsalicylideneamino)-2,3-butanediol], containing two μ3-OH bridges, has been prepared and structurally characterized; its thermal and magnetic properties were investigated.
Nickel/, Chirality/, Bridging ligands
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苟少华, Wei Huang, [a], Shaohua Gou, *[a], Huifen Qian, [b], Dahua Hu, Suchada Chantrapromma, [c], Hoong-Kun Fun, and Qingjin Meng[a]
Eur. J. Inorg. Chem. 2003, 947-954,-0001,():
-1年11月30日
Two macrocyclic dinuclear zinc(II) complexes (1a and 1b) have been self-assembled in the presence of pyridine and 2,2 -bipyridine, respectively, to form μ2-OH-bridged bimacrocycles with a Zn4O4 cavity through coordination bonding. The X-ray structural analysis reveals that both compounds {2a: [Zn4La 2(OH)2]2(ClO4)2; 2b: [Zn4Lb 2(OH)2]2(ClO4)2} have an open-mouthed sandwich-like structure with π−π interactions between parts of two phenyl rings to strengthen two hydroxyl groups connecting the metal atoms in the same direction of the macrocycle. Furthermore, nonclassical C−H•••Cl intermolecular interactions have been observed in the crystal of 2b. In addition, the reaction of 1a with quinoline derivatives has yielded novel hydrogen-bond-supported donor-acceptor complexes {3a: [Zn2 La(H2O)2(C10H9N)2](ClO4)2}. The crystallographic study of the complex containing 2-methylquinoline indicates that two 2-methylquinoline molecules are linked to two coordinating water molecules above and below the macrocyclic framework through O−H•••N hydrogen bonds. The 2-methylquinoline plane interacts in a face-to-face fashion with the phenyl ring of adjacent macrocyclic frameworks, forming an ordered arrangement where one macrocycle and two 2-methylquinolines are arrayed alternately with almost the same separation. The interplanar distance mentioned before is ca. 3.6Å.
N,, O ligands/, Macrocycles/, Zinc/, Self-assembly/, Structure elucidation/, Hydrogen bonds
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苟少华, Wei Huanga, Dahua Hua, Shaohua Goua, Suchada Chantraprommab, Hoong-Kun Funb, Yan Xua, Qinjing Menga
Inorganica Chimica Acta 342(2003)9-15,-0001,():
-1年11月30日
Two coordination polymers (2a and 2b) containing dinuclear zinc(II) macrocyclic components have been unexpectedly obtained when pyrazine and 2-methylpyrazine were used to react with dinuclear zinc(II) macrocyclic complexes 1a and 1b, respectively. The X-ray crystal structural study indicated that the coordination environment around each Zn(II) atom in 2 is a five-coordinated distorted pyramid in which the apical position is occupied by a bridging formate anion, unlocalized, in an end to end fashion. The formate group acts as a bidentate bridging ligand to link two adjacent macrocyclic units forming a chain polymer. In addition, Hbonding interactions are observed in the crystal packing of 2a and 2b, which could be described as two-dimensional networks.
Crystal structure, Zinc complexes, Macrocyclic complexes, Coordination polymers, Complexes
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苟少华, Jing-cai Yaoa, b, Wei Huangb, Bin Lib, Shaohua Goub, *, Yan Xub
Inorganic Chemistry Communications 5(2002)711-714,-0001,():
-1年11月30日
The self-assembly assisted by 2,20-bipyridine (2,20-bpy) protected zinc(II) species with 1,2-benzenedicarboxylate (1,2-BDC) has yielded a novel one-dimensional single helical coordination polymer of
Self-assembly, Crystal structure, Zn(, II), complex, Single helix coordination polymer
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