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基于组蛋白去乙酰化酶靶点的羟肟酸类化合物及其抗肿瘤活性研究进展

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化学通报 2024年第3期87卷 310-316页

作者：梁正会刘钦洲黄燕敏展军颜甘春芳广西天然高分子化学与物理重点实验室、南宁师范大学化学与材料学院南宁530001

组蛋白去乙酰化酶(HDACs)是肿瘤治疗的靶点之一,组蛋白去乙酰化酶抑制剂(HDACi)可通过包括抑制肿瘤细胞活力、迁移、侵袭、血管生成、增殖、DNA修复和诱导细胞凋亡等多种机制发挥抗肿瘤作用。本文对近年来以HDACs为单靶点和多靶点的羟... 详细信息

组蛋白去乙酰化酶(HDACs)是肿瘤治疗的靶点之一,组蛋白去乙酰化酶抑制剂(HDACi)可通过包括抑制肿瘤细胞活力、迁移、侵袭、血管生成、增殖、DNA修复和诱导细胞凋亡等多种机制发挥抗肿瘤作用。本文对近年来以HDACs为单靶点和多靶点的羟肟酸类衍生物的合成及其抗肿瘤活性进行综述,并对此方面的发展趋势、应用前景进行展望。

关键词：组蛋白去乙酰化酶抑制剂抗肿瘤羟肟酸

Rapid Microwave Assisted Synthesis and Antiproliferative Evaluation of Novel Steroidal Thiazole Derivatives

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Chemical Research in Chinese Universities 2017年第2期33卷 206-212页

作者： HUANG Yanmin ZHAO Dandan LIU Chang gan chunfang ZHAN Junyan LIN Qifu SHI Haixin CUI Jianguo College of Chemistry and Material Science Guangxi Teachers Education University Nanning 530001 P. R. China Guangxi Colleges and University Key Laboratory of Beibu Gulf Oil and Natural Gas Resource Effectfve Utffizat~'on Qizhou University Qizhou 535011 P. R. China

Three series of novel steroidal thiazole derivatives were synthesized by microwave assisted one-potreaction from pregnenolone, testosterone and estrone, respectively. Their structures were characterized by IR, NMRand HRMS, and the antiproliferative activities of all the synthesized compounds against human cervical carcinoma（HeLa）, human liver carcinoma（HepG2）, human lung carcinoma（A549）, nasopharyngeal carcinoma（CNE2） andnormal kidney epithelial cells（HEK293T） were screened. Among the compounds, 1-estron-17＇-ylidene-2-[4＇-（p-bromophenyl）-2＇-thiazol]hydrazone（12） displayed distinct antiproliferative activity against all the tested cancercell lines and was almost inactive to normal kidney epithelial cells.

关键词： Microwave assisted synthesis Pregnenolone Testosterone Estrone Steroidal thiazole derivative

Palladium-catalyzed tandem Heck/carbonylation/ aminocarbonylation en route to chiral heterocyclic α-ketoamides

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Organic Chemistry Frontiers 2022年第4期9卷 939-945页

作者： Huaanzi Hu Ting Yu Sidi Cheng Jing Li chunfang gan Shuang Luo Qiang Zhu State Key Laboratory of Respiratory Disease Guangzhou Institutes of Biomedicine and HealthChinese Academy of Sciences190 Kaiyuan AvenueGuangzhou 510530China School of Pharmacy Changzhou UniversityChangzhouJiangsu 213164China University of Chinese Academy of Sciences No.19(A)Yuquan RoadShijingshan DistrictBeijing100049China Guangxi Key Laboratory of Natural Polymer Chemistry and Physics College of Chemistry and MaterialsNanning Normal UniversityNanning 530001China Bioland Laboratory(Guangzhou Regenerative Medicine and Health Guangdong Laboratory) 510005 GuangzhouChina

An unprecedented tandem carbonylation/aminocarbonylation triggered by palladium-catalyzed enantio-selective Heck-type exocyclopalladation delivering chiral heterocyclicα-ketoamides has been developed.The uncommon double CO insertion into theσ-alkylpalladium intermediate takes place selectively under atmospheric pressure of CO using alkylamine as the nucleophile.Unique structures hybridizing alkylα-ketoamides with indolin-2-one containing a C3 all-carbon quaternary stereogenic center and 5,7-dihydro-6H-dibenzo[b,d]azepin-6-one containing a thermodynamically stabilized stereogenic biaryl axis are produced in good yields with excellent enantio-and/or diastereoselectivities.

关键词： heterocyclic palladium catalyzed

鹅去氧胆酸喹啉缀合物的合成及对Hg^(2+)高选择性识别

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化工技术与开发 2024年第1期53卷 1-7页

作者：展军颜赵杰甘春芳黄燕敏南宁师范大学广西天然高分子化学与物理重点实验室广西南宁530001

汞离子被列为最具毒性和危险性的重金属离子之一,灵敏高效地识别Hg^(2+)具有重要意义。目前报道的汞离子荧光传感器的选择性差,响应速度慢,容易受到Cu^(2+)、Fe^(3+)、Al^(3+)等竞争性金属离子的干扰,因此设计选择性好、抗干扰能力强的H... 详细信息

汞离子被列为最具毒性和危险性的重金属离子之一,灵敏高效地识别Hg^(2+)具有重要意义。目前报道的汞离子荧光传感器的选择性差,响应速度慢,容易受到Cu^(2+)、Fe^(3+)、Al^(3+)等竞争性金属离子的干扰,因此设计选择性好、抗干扰能力强的Hg2+荧光传感器非常有必要。本文将8-羟基喹啉偶联到鹅去氧胆酸结构中,制备了鹅去氧胆酸荧光分子CDCA-3。荧光数据表明,Hg^(2+)使得鹅去氧胆酸荧光分子的荧光淬灭96%;紫外数据表明,加入Hg^(2+)后,在222nm处出现了1个新的吸收峰,且紫外吸光度明显升高,而其它金属离子基本没有变化。因此,鹅去氧胆酸喹啉荧光传感器对Hg^(2+)具有高选择性的识别性能。由Benesi-Hildebrand方程的计算结果可知,通过荧光滴定实验和紫外滴定实验得到的络合常数,分别为4.09×10^(5)M^(-1)和9.26×10^(4)M^(-1),说明鹅去氧胆酸荧光分子对Hg^(2+)具有强的络合能力。在有其他离子共存的情况下,鹅去氧胆酸荧光分子可以实现对Hg^(2+)的识别,说明该化学传感器具有良好的抗干扰能力。

关键词：荧光传感器鹅去氧胆酸汞离子

Inherently Chiral 6,7-Diphenyldibenzo [e,g][1,4]diazocine: Enantioselective Synthesis and Application as a Ligand Platform

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CCS Chemistry 2023年第4期5卷 982-993页

作者： Yu Luo Xilong Wang Weiming Hu Yan Peng Chaoqin Wang Ting Yu Sidi Cheng Jing Li Yimiao He chunfang gan Shuang Luo Qiang Zhu State Key Laboratory of Respiratory Disease Guangzhou Institutes of Biomedicine and HealthChinese Academy of SciencesGuangzhou 510530 University of Chinese Academy of Sciences Shijingshan DistrictBeijing 100049 Guangxi Key Laboratory of Natural Polymer Chemistry and Physics College of Chemistry and MaterialsNanning Normal UniversityNanning 530001

Inherently chiral 6,7-diphenyldibenzo[e,g][1,4]diazocine(DDD)has been synthesized enantioselectively for the first time via chiral phosphoric acid(CPA)-catalyzed cyclocondensation of readily available[1,1′-biphenyl]-2,2′-diamine(1a)and benzil(2a)in 82%yield,with 98%ee under mild reaction conditions.The strategy could also be applied to racemic biaryl diamines through kinetic resolution.The unexpectedly high interconversion energy barriers between the enantiomers(ΔG=39.5 kcal/mol)and the chemical stability rendered DDD an ideal platform for developing new chiral ligands and catalysts.Unique inherently chiralDDD-based phosphoramidites,phosphoric acid,mono-and diphosphine ligands were prepared from optically pure diphenol derivative DDDOL as a common precursor.Preliminary asymmetric reactions catalyzed by Pd or Rh in the presence of newly developed ligands exhibited comparable or even better enantioselectivities than the corresponding BINOLor SPINOL-derived ligands.Density functional theory calculation revealed the origin of the enantioselectivity during the process.

关键词： inherent chirality enantioselective synthesis 6,7-diphenyldibenzo[e,g]diazocine chiral phosphoric acid chiral phosphorus ligand

Rapid microwave assisted synthesis and antiproliferative evaluation of novel steriadal thiazole derivatives

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Rapid microwave assisted synthesis and antiproliferative eva...

海洋物质中的活性B-降甾醇分子作为先导化合物的合成及抗肿瘤活性研究（英文）

中国化学会全国第十二届有机合成化学学术研讨会

作者： Huang,Yanmin Zhao,Dandan gan,chunfang Liu,Zhipin Lin,Qifu Yang,Chunhui Shi,Haixin Cui,Jianguo College of Chemistry and Material Science Guangxi Teachers Education University Guangxi Colleges and University Key Laboratory of Beibu Gulf Oil and Natural Gas Resoure Effective Utilization Qizhou University

Heterocycles can enhance binding affinity and improve in vitro potency via hydrogen bond interactions.The compounds containing heterocycles had been widely applied to the field of medicine or pesticide because of its good biological activity 1].Thiazole is an important five-membered aromatic heterocycle possessing N and S atom.Compounds containing thiazole cycle display various biological functions due to its special chemical structure,such as antimicrobial,antiinflammatory,anticancer,anti-HIV-1 etc,and have obtained an extensive application in drugs,pesticides,and materials science etc2].Recently,some steroidal thiazole derivatives possessing a D-ring fused a thiazole were reported as anti-inflammatory and anti-tumor agents[3].In present studies,three series of novel steroidal thiazole derivatives were respectively synthesized through microwave assisted one-pot reaction of pregnenolone,testosterone and estrone with thiosemicarbazide and 4-substituted-ω-bromoacetophenones.Their structures were characterized by IR,NMR and HRMS,and the anticancer activity of all synthesized compounds against human cervical carcinoma(He La),human lung carcinoma(A549),human liver carcinoma cells(HEPG2) and normal kidney epithelial cells(HEK293T) was screened.Some compounds displayed distinct antiproliferative activity against all tested cancer cell lines,and was almost inactive to normal kidney epithelial cells.

关键词： microwave assisted synthesis pregnenolone testosterone estrone steroidal thiazole derivatives

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海洋物质中的活性B-降甾醇分子作为先导化合物的合成及抗肿瘤活性...

中国化学会全国第十二届有机合成化学学术研讨会

作者： Huang,Yanmin Qi,Binbin Cui,Jianguo Liu,Zhiping gan,chunfang Zhao,Dandan Lin,Qifu Shi,Haixin College of Chemistry and Material Science Guangxi Teachers Education University Guangxi Colleges and University Key Laboratory of Beibu Gulf Oil and Natural Gas Resoure Effective Utilization Qizhou University

Some novel B-norcholesterol derivatives with thiazole ring were synthesized and their structures were characterized by IR,NMR and HRMS.The antiproliferative activity of synthesized compounds against human cervical carcinoma（HeL a）,lung carcinoma（A549）,liver carcinoma cells（HEPG2） and normal kidney epithelial cells（HEK293T） was assayed.The results revealed that some compounds with a structure of N-methylthiazole displayed distinct antiproliferative activity against A549 and HEPG2 cells.Compounds with a structure of N-phenylthiazole displayed a selective antiproliferative activity on HeL a cells and were almost inactive to normal kidney epithelial cells（HEK293T）.

关键词： cholesterol B-norcholesteryl thiazoles B-norcholesteryl N-methylthiazoles B-norcholesteryl N-phenylthiazoles antiproliferative activity

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蒙脱土对膨胀型防火涂料阻燃性能的影响

涂料工业 2007年第10期37卷 15-18页

作者：甘春芳莫羡忠广西师范学院化学系南宁530001

采用锥形量热仪(CONE)研究蒙脱土(Na-MMT)对防火涂料阻燃性能的影响。结果表明,随着Na-MMT含量增加,膨胀型防火涂料的质量损失速率峰值(pk-MLR)和总耗氧量(TOC)相对于未添加蒙脱土的防火涂料降低,热释放速率峰值明显降低,热氧化降解推迟... 详细信息

采用锥形量热仪(CONE)研究蒙脱土(Na-MMT)对防火涂料阻燃性能的影响。结果表明,随着Na-MMT含量增加,膨胀型防火涂料的质量损失速率峰值(pk-MLR)和总耗氧量(TOC)相对于未添加蒙脱土的防火涂料降低,热释放速率峰值明显降低,热氧化降解推迟,热稳定性提高。对CONE燃烧过的膨胀型防火涂料进行扫描电镜(SEM)分析,添加了Na-MMT的体系炭层结构致密均匀,有效地防止了热量的散发。

关键词：蒙脱土防火涂料阻燃性能锥形量热

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7-位取代的甾体类化合物生物活性研究进展

化学通报 2022年第4期85卷 446-451页

作者：陈华龙刘钦洲黄燕敏崔建国陈小凤甘春芳广西天然高分子化学与物理重点实验室南宁师范大学化学与材料学院南宁530001

7-位取代的甾体类化合物是一类具有良好生物活性的化合物,在抗炎、抗肿瘤等领域发挥着重要作用。本文以7-位取代的甾体类化合物为研究对象,按照不同的甾体母核进行分类,对近年来有关7-位取代的甾体类化合物的生理活性研究进行综述,并为... 详细信息

7-位取代的甾体类化合物是一类具有良好生物活性的化合物,在抗炎、抗肿瘤等领域发挥着重要作用。本文以7-位取代的甾体类化合物为研究对象,按照不同的甾体母核进行分类,对近年来有关7-位取代的甾体类化合物的生理活性研究进行综述,并为此类化合物的发展趋势和应用作了展望,以期为抗肿瘤药物的研发提供一定的理论基础。

关键词：甾体 7-取代抗肿瘤生物活性