药物化学学科依托于药物化学教研室,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
(一)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。
(二)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
(一)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
(二)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。
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。
8.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。
9.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。
(三)近三年代表性论文
1.Electrochemicallymediateddirect C(sp3)?H Sulfonylation ofxanthenederivatives.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 receptorγt 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 of Inula hupehensis. J Nat Prod, 2022, 85:185-195.(张贵杰,通讯作者)
7.Anti-inflammatory constituents from Caulis Trachelospermi.Planta Med,2022, 88(9-10): 721-728.(谭钦刚,通讯作者)
8.Dimeric Erythrinaalkaloids as well as their key units from Erythrina variegate.Phytochemistry,2022, 198: 113160.(谭钦刚,通讯作者)
9.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)
10.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)
11.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)
12.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)
13.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)
14.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)
15.Visible-light-induced radical cascade reaction of 1-allyl-2-ethynylbenzoimidazoles withthiosulfonates to assemble thiosulfonylated pyrrolo[1,2-a]benzimidazoles.J Org Chem, 2021, 86:16882-16891.(陈艳艳,通讯作者)
16.Phloroglucinol derivatives rhotomensones A-G from Rhodomyrtus tomentosa. Phytochemistry, 2021, 190:112890.(梁成钦,通讯作者)
17.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)
18.Bioactive dammarane triterpenoid saponins from the leaves of Cyclocarya paliurus. Phytochemistry, 2021, 183:112618.(梁成钦,通讯作者)
19.Designing a lysosome targeting nanomedicine for pH triggered enhanced phototheranostics.Mater Chem Front, 2021, 5:2694-2701.(邹登峰,第一作者)
20.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)
21.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)
22.Naturally available hypericin undergoing electron transfer for type I photodynamic and photothermal synergistic therapy. Biomater Sci, 2020, 8:2481-2487.(邹登峰,通讯作者)
23.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)
24.Discovery of novel N-aryl pyrrothine derivatives as bacterial RNA polymerase inhibitors. Chem Biol Drug Des,