药物化学教研室

药物化学教研室

教研室由药物化学、天然药物化学和有机化学三门学科组成,所属的各学科成立于1976年11月。2009年因学科建设和管理工作的需要组建为有机药化、天然药化教研室,2013年更名为药物化学教研室。药物化学教研室主要承担药物化学、天然药物化学、有机化学、医用基础化学(2)、有机化合物结构解析和新药研究与开发等课程的教学任务。

目前本教研室共有教师20名,其中具有博士学位的占85%,具有高级职称的占65%,硕士生导师16名。

2020~2022年期间,本教研室教师共主持了1项省部级教改课题。近3年主持科研课题10项,其中国家级4项、省部级6项,累计科研经费260余万元,获授权发明专利16项。以第一作者或通讯作者发表的科研论文50余篇,其中SCI收录论文40篇。

一、教学情况

1.近三年承担的教改项目

李芳耀,药学专业硕士研究生高等有机化学混合式教学模式的研究与实践,广西教育厅,2022年。

2.近三年获得的教学成果奖

杨扬(排名前4),“产教融合,行业驱动”构建地方医药院校药学一流专业人才培养新模式,广西高等教育自治区级教学成果奖一等等次,2021年。

二、科研情况

1.教研室主要研究方向

新药分子的设计与合成;天然药物活性成分的研究和结构改造;手性催化剂的研究;药物合成方法学

2.近三年承担的科研项目

  1. 张业,靶向IDO1/STAT3的1,4-萘醌铂(IV)金属化学免疫治疗剂的研究,国家自然科学基金,2021年。

  2. 黄日镇,新型1,4-萘醌肟类IDO1/STAT3双靶点抑制剂的设计、合成及抗肿瘤活性研究,国家自然科学基金青年基金,2021年。

  3. 谭钦刚,基于代谢组学的壮药络石藤抗RA药效物质基础及作用机制研究,国家自然科学基金,2020年。

  4. 谭相端,新型FXR部分激动剂的设计合成及抗非酒精性脂肪性肝炎活性研究,国家自然科学基金,2020年。

  5. 张业,靶向IDO1/STAT3的1,4-萘醌-铂金属基肿瘤化学免疫治疗剂:设计合成、活性与作用机制研究,广西杰出青年基金,2020年。

  6. 张业,基于靶向载送-前药策略设计合成“聚乙二醇-靶向肽-伊立替康”抗肿瘤化合物的研究,广西自然科学基金,2020年。

  7. 马小盼,2-取代吲哚开环策略合成轴手性喹喔啉化合物,广西自然科学基金,2020年。

  8. 莫祖煜,电化学介导C(sp3)-H键磺酰化的研究,广西自然科学基金,2020年。

  9. 张妞妞,Osimertinib衍生物的结构设计、合成及抗肿瘤活性研究,广西科技基地和人才专项,2020年。

  10. 黄日镇,新型免疫-化疗功能一体化的IDO1/STAT3抑制剂研究,广西科技基地和人才专项,2020年。

3.近三年代表性论文

  1. Electrochemically mediated direct C(sp3)−H Sulfonylation of xanthene derivatives. Adv Synth Catal, 2022, 364(4): 726-731. (莫祖煜,通讯作者)

  2. Design, synthesis and evaluation of novel dehydroabietic acid-dithiocarbamate hybrids as potential multi-targeted compounds for tumor cytotoxicity. Arab J Chem, 2022,15: 104145.(李芳耀,通讯作者)

  3. Synthesis and biological evaluation of novel pentanediamide derivatives as S-adenosyl-L-homocysteine hydrolase inhibitors.Bioorg Med Chem Lett,2022, 72: 128880.(谭相端,通讯作者)

  4. Discovery of 2H-chromone-4-one based sulfonamide derivatives as potent retinoic acid receptor-related orphan receptor γt inverse agonists. Eur J Med Chem, 2022, 229:114065.(黄日镇,通讯作者)

  5. Visible-light-induced tandem reaction of allenes with selenesulfonates leading to (E)-2,3-disulfonylpropene derivatives. J Org Chem, 2022, 87: 5846-5855. (陈艳艳,通讯作者)

  6. Structures and biological activities of polyacylated ent-kaurane diterpenoid glycosides from the aerial parts ofInula hupehensis. J Nat Prod, 2022, 85:185-195. (张贵杰,通讯作者)

  7. Xanthones from the stems ofCalophyllum membranaceumGardn. et Champ. and their anti-inflammatory activity. Phytochemistry, 2022, 200: 113246. (张贵杰,通讯作者)

  8. Anti-inflammatory constituents from Caulis Trachelospermi. Planta Med, 2022, 88(9-10): 721-728.(谭钦刚,通讯作者)

  9. DimericErythrinaalkaloids as well as their key units fromErythrina variegate. Phytochemistry, 2022, 198: 113160.(谭钦刚,通讯作者)

  10. Synthesis of new chlorins photosensitizer for photodynamic therapy against colon cancer. Mater Chem Front, 2022, 6: 1129-1136.(邹登峰,通讯作者)

  11. A tricomponent semiconducting polymer with ultrahigh photothermal conversion efficiency as a biodegradable photosensitizer for phototheranostics. Mater Chem Front. 2022, 6: 8-14.(邹登峰,通讯作者)

  12. Visible light-promoted selenylation/cyclization of enaminones toward the formation of 3-selanyl-4H-chromen-4-ones. Adv Synth Catal, 2021, 363:1656-1661.(徐燕丽,通讯作者)

  13. Synthesis of indolo[2,1-a]isoquinolin-6(5H)-ones derivatives via Fe(OTf)3-promoted tandem selenylation/cyclization of 2-arylindoles. Adv Synth Catal, 2021, 363:497-504.(徐燕丽,通讯作者)

  14. Design, synthesis and antitumor evaluation of new 1,8-naphthalimide derivatives targeting nuclear DNA. Eur J MedChem, 2021, 210:112951. (张业,通讯作者)

  15. Visible-lght-induced cyclization/aromatization of 2-vinyloxy arylalkynes: synthesis of thio-substituted dibenzofuran derivatives. Org Lett, 2021, 23:376-381.(陈艳艳,通讯作者)

  16. Visible-light-induced radical cascade reaction of 1-allyl-2-ethynylbenzoimidazoles withthiosulfonates to assemble thiosulfonylated pyrrolo[1,2-a]benzimidazoles. JOrg Chem,2021, 86:16882-16891.(陈艳艳,通讯作者)

  17. A new triterpenoid from the leaves ofRhodomyrtus tomentosa(Ait.) Hassk.Nat Prod Res,2021, 35:2289-2294.(梁成钦,通讯作者)

  18. Phloroglucinol derivatives rhotomensones A-G fromRhodomyrtus tomentosa. Phytochemistry, 2021, 190:112890.(梁成钦,通讯作者)

  19. Anti-hepatitis B virus activity and hepatoprotective effect ofdes(rhamnosyl) verbascoside from Lindernia ruellioides in vitro. Phytother Res, 2021,35(8):4555-4566.(梁成钦,通讯作者)

  20. Bioactive dammarane triterpenoid saponins from the leaves ofCyclocarya paliurus.Phytochemistry, 2021, 183:112618.(梁成钦,通讯作者)

  21. A new glucopyranoside from theleaves ofMicrosoriumfortune. Nat Prod Res,2021, 35:3723-3728.(梁成钦,通讯作者)

  22. Designing a lysosome targeting nanomedicine for pH triggered enhanced phototheranostics.Mater Chem Front, 2021, 5:2694-2701.(邹登峰,第一作者)

  23. A heavy atom free miconducting polymer with high singlet oxygen quantum yield for photodynamic and photothermal synergistic therapy. Mater Design,2021,109263-109270.(邹登峰,通讯作者)

  24. Synthesis and biological evaluation of dehydroabietic acid-pyrimidine hybrids as antitumor agents. RSC Adv, 2020, 10:18008-18015.(李芳耀,通讯作者)

  25. Naturally available hypericin undergoing electron transferfor type I photodynamic and photothermal synergistic therapy. Biomater Sci,2020, 8:2481-2487.(邹登峰,通讯作者)

  26. Two photoactive Ru (II) compounds based on tetrazole ligands for photodynamic therapy. J Inorg Biochem, 2020.111127-111133.(邹登峰,通讯作者)

  27. Boosting type I process of Ru(II) compounds by changing tetrazole ligand for enhanced photodynamic therapy against lung cancer. J Inorg Biochem,2020, 111236-111242.(邹登峰,通讯作者)

  28. Two Ru(II) compounds with aggregation induced emission as promising photosensitizers for photodynamic therapy. J Inorg Biochem, 2020,212:111233-111238.(邹登峰,通讯作者)

  29. Dimerization of heavy atom free tetraphenylethylene with aggregation induced emission for boosting photodynamic therapy.New J Chem, 2020, 44:7029-7034.(邹登峰,通讯作者)

  30. Pyridazino[1,6-b]quinazolinones as new anticancer scaffold: Synthesis, DNA intercalation, topoisomerase I inhibition and antitumor evaluation in vitro and in vivo. Bioorg Chem, 2020, 99:103814-103825.(黄婉云,第一作者)

  31. Discovery of novel N-aryl pyrrothine derivatives as bacterial RNA polymerase inhibitors. Chem Biol Drug Des, 2020, 96:1262–1271.(谭相端,通讯作者)

  32. Synthesis, mechanisms of action, and toxicity of novel aminophosphonates derivatives conjugated irinotecanin vitroandin vivoas potent antitumor agents. Eur J Med Chem, 2020, 189:112067.(黄日镇,通讯作者)

  33. Potential anti-diabetic isoprenoids and a long-chainδ-lactone from frangipani(Plumeria rubra). Fitoterapia, 2020, 146: 104684.(谭钦刚,通讯作者)

  34. Bifunctional naphthoquinone aromatic amide-oxime derivatives exert combined immunotherapeutic and antitumor effects through simultaneous targeting of indoleamine-2,3-dioxygenase and signal transducer and activator of transcription 3. J Med Chem, 2020, 63: 1544‒1563.(张业,通讯作者)

  35. Design, synthesis and biological evaluation of naphthalenebenzimidizole platinum (II) complexes as potential antitumor agents. Eur J Med Chem, 2020, 188:112033.(张业,通讯作者)

  36. Design, synthesis and antitumor activity of a novel PEG-A6-conjugated irinotecan derivative. Bioorg Med Chem Lett, 2020, 30:126847.(张业,通讯作者)

  37. Design, synthesis and biological evaluation of 3-nitro-1,8-naphthalimides as potential antitumor agents. Bioorg Med Chem Lett, 2020, 30:127051.(张业,通讯作者)

  38. Saponin fromPeriploca forrestiiSchltr Mitigates oxazolone-induced atopic dermatitis via modulating macrophage activation.Mediators Inflamm, 2020, 2020:4346367. (孙广臣,第一作者)

  39. Electrochemical sulfonylation of alkynes with sulfonyl hydrazides:ametal- and oxidant- free protocol for the synthesis of alkynyl sulfones. Adv Synth Catal, 2020, 362(11): 2160-2167. (莫祖煜,第一作者)

  40. Sesquineolignan and neolignan enantiomers fromTriadica sebifera. Bioorg Chem, 2020, 103: 104147.(张贵杰,通讯作者)

4.近三年获得专利情况

  1. 陈艳艳,徐燕丽,陈慧.一种合成11-硫基萘并[2,3-b]苯并呋喃化合物的方法:中国,专利授权号ZL202011424026.0,授权公告日2022.09.20.

  2. 梁成钦,周先丽,罗琴,等.达玛烷三萜皂苷化合物及其应用:中国,专利授权号ZL 20201 1 048083.3,授权公告日2021.08.31.

  3. 邹登峰,朱华,柯珍,等.银杏内酯的提取方法:中国,专利授权号ZL201810438920.X,授权公告日2020.9.11.

  4. 徐燕丽,张嘉蓉,陈艳艳.一种合成5-硒基吲哚并[2,1-a]异喹啉-6(5H)-酮化合物的方法:中国,专利授权号ZL 202011168440.X,授权公告日2021.07.02.

  5. 张业,李芳耀,段小群,等.3-苯并咪唑-6,7-胡椒环-2(1H)-喹啉酮-锌配合物及其制备方法和应用:中国,专利授权号ZL2018107295134,授权公告日2021.03.02.

  6. 张业,马献力,余砚成,等.11,12-二氯苯并咪唑-1,8-萘酰亚胺-铂配合物及其制备方法和应用:中国,专利授权号ZL201810730055.6,授权公告日2020.09.25.

  7. 张业,马献力,余砚成,等.11-三氟甲基苯并咪唑-1,8-萘酰亚胺-铂配合物及其制备方法和应用:中国,专利授权号ZL201810729763.8,授权公告日2020.09.25.

  8. 张业,马献力,余砚成,等. 12-氯苯并咪唑-1,8-萘酰亚胺-铂配合物及其制备方法和应用:中国,专利授权号ZL201810729521.9,授权公告日2020.09.29.

  9. 张业,余砚成,马献力,等.苯并咪唑-1,8-萘酰亚胺-铂配合物及其制备方法和应用:中国,专利授权号ZL201810729771.2,授权公告日2020.09.29.

  10. 张业,马献力,余砚成,等.11,12-二甲基苯并咪唑-1,8-萘酰亚胺-铂配合物及其制备方法和应用:中国,专利授权号ZL201810730052.2,授权公告日2020.09.29.

  11. 张业,马献力,余砚成,等.12-氟苯并咪唑-1,8-萘酰亚胺-铂配合物及其制备方法和应用:中国,专利授权号ZL201810730053.7,授权公告日2020.09.29.

  12. 李芳耀,王秀,庞富华,等.去氢枞酸噁唑烷酮衍生物及其制备方法和应用:中国,专利授权号ZL201810119381.3,授权公告日2021-02-12.

  13. 黄婉云,张小蓉,吕良,等.哒嗪[6,1-b]并喹唑啉酮衍生物及其制备方法和应用:中国,专利授权号ZL201811385851.7,授权公告日2021.3.23.

  14. 黄婉云,张晓婷,郑彬,等.5-氨基苯并[b][1,8]萘啶类化合物的制备方法和应用:中国,专利授权号ZL201910698398.3,授权公告日2021.8.24.

  15. 谭相端,吕良,蒙杰雲,等. N-芳基二硫吡咯酮脲类和氨基酯类衍生物及其制备化合应用:中国,专利授权号ZL201911186804.4,授权公告日:2020.7.28

  16. 谭相端,段小群,刘文涛,等.一种N-芳基二硫吡咯酮-吡喃酮杂合衍生物及其制备方法和应用:中国,专利授权号ZL201811565381.2,授权公告日: 2020.6.12

     

(2022年11月10日)

(数据更新至2022年11月10日)