[1] Zhang HZ,Zhao ZL,Zhou CH.Recent advance in oxazole-based medicinal chemistry[J].Eur J Med Chem,2018,144:444-492.
[2] Zhang HZ,Gan LL,Wang H,et al.New progress in azole compounds as antimicrobial agents[J].Mini-Rev Med Chem,2017,17(2):122-166.
[3] Mayer JCP,Sauer AC,Iglesias BA,et al.Ferrocenylethenyl-substituted 1,3,4-oxadiazolyl-1,2,4-oxadiazoles:Synthesis,characterization and DNA-binding assays[J].J Organomet Chem,2017,841:1-11.
[4] Ohnmacht SA,Neidle S.Small-molecule quadruplex-targeted drug discovery[J].Bioorg Med Chem Lett,2014,24(12):2602-2612.
[5] Yamaguchi Y,Nishizono N,Kobayashi D,et al.Evaluation of synthesized coumarin derivatives on aromatase inhibitory activity[J].Bioorg Med Chem Lett,2017,27(12):2645-2649.
[6] Rafferty SW,Eisner JR,Moore WR,et al.Highly-selective 4-(1,2,3-triazole)-based P450c17a 17,20-lyase inhibitors[J].Bioorg Med Chem Lett,2014,24(11):2444-2447.
[7] Bell JL,Haak AJ,Wade SM,et al.Optimization of novel nipecotic bis(amide) inhibitors of the Rho/MKL1/SRF transcriptional pathway as potential anti-metastasis agents[J].Bioorg Med Chem Lett,2013,23(13):3826-3832.
[8] Naud S,Westwood IM,Faisal A,et al.Structure-based design of orally bioavailable 1H-pyrrolo[3,2-c]pyridine inhibitors of mitotic kinase monopolar spindle 1(MPS1)[J].J Med Chem,2013,56(24):10045-10065.
[9] Zhu HY,Desai J,Deng Y,et al.Discovery of hydroxyaniline amides as selective Extracellular Regulated Kinase (Erk) inhibitors[J].Bioorg Med Chem Lett,2015,25(7):1627-1629.
[10] Lu XW,Wu Y.On the structure of aspongopusin recently isolated from Aspongopus chinensis[J].Fitoterapia,2013,84:318-320.
[11] Wu C,Liang ZW,Xu YY,et al.Gold-catalyzed oxazoles synthesis and their relevant antiproliferative activities[J].Chin Chem Lett,2013,24(12):1064-1066.
[12] Dorsch D,Schadt O,Stieber F,et al.Identification and optimization of pyridazinones as potent and selective c-Met kinase inhibitors[J].Bioorg Med Chem Lett,2015,25(7):1597-1602.
[13] 黎龙香,谢龙勇,王风君,等.17-(2′,5′-二取代噁唑基)-雄甾-4,16-二烯-3-酮的合成及抗肿瘤活性研究[J].有机化学,2014,34(9):1864-1869.
[14] He SC,Peng YJ,Zhang HJ,et al.Design,synthesis and antimicrobial evaluation of novel benzimidazole-incorporated sulfonamide analogues[J].Eur J Med Chem,2017,136:165-183.
[15] Yang J,Zhou S,Ji L,et al.Synthesis and structure–activity of 4-azaheterocycle benzenesulfonamide derivatives as new microtubule-targeting agents[J].Bioorg Med Chem Lett,2014,24(21):5055-5058.
[16] Lintnerova L,Garcia-Caballero M,Gregan F,et al.A development of chimeric VEGFR2 TK inhibitor based on two ligand conformers from PDB:1Y6A complex-medicinal chemistry consequences of a TKs analysis[J].Eur J Med Chem,2014,72:146-159.
[17] Wang L,Mei X,Wang C,et al.Biomimetic semi-synthesis of fradcarbazole A and its analogues[J].Tetrahedron,2015,71(42):7990-7997.
[18] Mathew JE,Divya G,Vachala SD,et al.Synthesis and characterization of novel 2,4-diphenyloxazole derivatives and evaluation of their in vitro antioxidant and anticancer activity[J].J Pharm Res,2013,6(1):210-213.
[19] Colabufo NA,Contino M,Cantore M,et al.Naphthalenyl derivatives for hitting P-gp/MRP1/BCRP transporters[J].Bioorg Med Chem,2013,21(5):1324-1332.
[20] Fuwa H,Noguchi T,Kawakami M,et al.Synthesis and biological evaluation of (+)-neopeltolide analogues:Importance of the oxazole-containing side chain[J].Bioorg Med Chem Lett,2014,24(11):2415-2419.
[21] Guerra-Bubb JM,Bowers AA,Smith WB,et al.Synthesis and HDAC inhibitory activity of isosteric thiazoline-oxazole largazole analogs[J].Bioorg Med Chem Lett,2013,23(21):6025-6028.
[22] Han F,Wang P,Zhang W,et al.CA-1H,a novel oxazole bearing analogue of combretastatin A-4,disrupts the tumor vasculatures and inhibits the tumor growth via inhibiting tubulin polymerization[J].Biomed Pharmacother,2016,80:151-161.
[23] Zhou J,Jin J,Zhang Y,et al.Synthesis and antiproliferative evaluation of novel benzimidazole contained oxazole-bridged analogs of combretastatin A-4[J].Eur J Med Chem,2013,68:222-232.
[24] Maini R,Dedkova LM,Paul R,et al.Ribosome-mediated incorporation of dipeptides and dipeptide analogues into proteins in vitro[J].J Am Chem Soc,2015,137(35):11206-11209.
[25] Choi MJ,No ES,Thorat DA,et al.Synthesis and biological evaluation of aryloxazole derivatives as antimitotic and vascular-disrupting agents for cancer therapy[J].J Med Chem,2013,56(22):9008-9018.
[26] Wieczorek A,Plazuk D,Zakrzewski J,et al.Synthesis and unusual ring transformation of 1-acyl-3- (ferrocenylmethylidene)-piperazine-2,5-diones[J].J Organomet Chem,2013,745-746:373-378.
[27] Zhou Y,Murphy AC,Samborskyy M,et al.Iterative mechanism of macrodiolide formation in the anticancer compound conglobatin[J].Chem Biol,2015,22(6):745-754.
[28] Ohnmacht SA,Ciancimino C,Vignaroli G,et al.Optimization of anti-proliferative activity using a screening approach with a series of bis-heterocyclic G-quadruplex ligands[J].Bioorg Med Chem Lett,2013,23(19):5351-5355.
[29] Speed AWH,Mann TJ,O'Brien RV,et al.Catalytic Z-selective cross-metathesis in complex molecule synthesis:A convergent stereoselective route to disorazole C1[J].J Am Chem Soc,2014,136(46):16136-16139.
[30] Fukuhara K,Takada K,Okada S,et al.Nazumazoles A-C,cyclic pentapeptides dimerized through a disulfide bond from the marine sponge Theonella swinhoei[J].Org Lett,2015,17(11):2646-2648.
[31] Bae SY,Kim GD,Jeon J,et al.Anti-proliferative effect of (19Z)-halichondramide,a novel marine macrolide isolated from the sponge Chondrosia corticata,is associated with G2/M cell cycle arrest and suppression of mTOR signaling in human lung cancer cells[J].Toxicol in Vitro,2013,27(2):694-699.
[32] Blankson GA,Pilch DS,Liu AA,et al.Macrocyclic biphenyl tetraoxazoles:Synthesis,evaluation as G-quadruplex stabilizers and cytotoxic activity[J].Bioorg Med Chem,2013,21(15):4511-4520.
[33] Chung WJ,Heddi B,Tera M,et al.Solution structure of an intramolecular(3+1) human telomeric G-quadruplex bound to a telomestatin derivative[J].J Am Chem Soc,2013,135(36):13495-13501.
[34] Marchand A,Granzhan A,Iida K,et al.Ligand-induced conformational changes with cation ejection upon binding to human telomeric DNA G-quadruplexes[J].J Am Chem Soc,2015,137(2):750-756.
[35] Shi W,Hu J,Bao N,et al.Design,synthesis and cytotoxic activities of scopoletin-isoxazole and scopoletin-pyrazole hybrids[J].Bioorg Med Chem Lett,2017,27(1):147-151.
[36] Im D,Jung K,Yang S,et al.Discovery of 4-arylamido 3-methyl isoxazole derivatives as novel FMS kinase inhibitors[J].Eur J Med Chem,2015,102:600-610.
[37] Balaji NV,Ramani MV,Viana AG,et al.Design,synthesis and in vitro cell-based evaluation of the anti-cancer activities of hispolon analogs[J].Bioorg Med Chem,2015,23(9):2148-2158.
[38] Emmerich J,Koppen CJ,Burkhart JL,et al.Lead optimization generates CYP11B1 inhibitors of pyridylmethyl isoxazole type with improved pharmacological profile for the treatment of Cushing's disease[J].J Med Chem,2017,60(12):5086-5098.
[39] 戴红,姚炜,叶林玉,等.新型含取代异噁唑结构的吡唑酰胺类衍生物的合成及其生物活性研究[J].有机化学,2017,37(8):2165-2171.
[40] Dhar G,Chakravarty D,Hazra J,et al.Actin-curcumin interaction:Insights into the mechanism of actin polymerization inhibition[J].Biochem,2015,54(4):1132-1143.
[41] Kumar RN,Dev GJ,Ravikumar N,et al.Synthesis of novel triazole/isoxazole functionalized 7-(trifluoromethyl)pyrido[2,3-d]pyrimidine derivatives as promising anticancer and antibacterial agents[J].Bioorg Med Chem Lett,2016,26(12):2927-2930.
[42] Crawford TD,Ndubaku CO,Chen H,et al.Discovery of selective 4-amino-pyridopyrimidine inhibitors of MAP4K4 using fragment-based lead identification and optimization[J].J Med Chem,2014,57(8):3484-3493.
[43] Yin BT,Yan CY,Peng XM,et al.Synthesis and biological evaluation of α-triazolyl chalcones as a new type of potential antimicrobial agents and their interaction with calf thymus DNA and human serum albumin[J].Eur J Med Chem,2014,71:148-159.
[44] Wan M,Xu L,Hua L,et al.Synthesis and evaluation of novel isoxazolyl chalcones as potential anticancer agents[J].Bioorg Chem,2014,54:38-43.
[45] Sun J,Lin C,Qin X,et al.Synthesis and biological evaluation of 3,5-disubstituted-4-alkynylisoxozales as a novel class of HSP90 inhibitors[J].Bioorg Med Chem Lett,2015,25(16):3129-3134.
[46] Al-Dosari MS,Ghorab MM,Alsaid MS,et al.Synthesis and anticancer activity of some novel trifluoromethylquinolines carrying a biologically active benzenesulfonamide moiety[J].Eur J Med Chem,2013,69:373-383.
[47] Weaver MJ,Kearns AK,Stump S,et al.AIMing towards improved antitumor efficacy[J].Bioorg Med Chem Lett,2015,25(8):1765-1770.
[48] Zhang C,Wang X,Liu H,et al.Design,synthesis and pharmacological evaluation of 4,5-diarylisoxazols bearing amino acid residues within the 3-amido motif as potent heat shock protein 90 (Hsp90) inhibitors[J].Eur J Med Chem,2017,125:315-326.
[49] Steiger SA,Li C,Backos DS,et al.Dimeric isoxazolyl-1,4-dihydropyridines have enhanced binding at the multi-drug resistance transporter[J].Bioorg Med Chem,2017,25(12):3223-3234.
[50] Kuzikov AV,Dugin NO,Stulov SV,et al.Novel oxazolinyl derivatives of pregna-5,17(20)-diene as 17(-hydroxylase/17,20-lyase (CYP17A1) inhibitors[J].Steroids,2014,88:66-71.
[51] Akhtar J,Khan AA,Ali Z,et al.Structure-activity relationship (SAR) study and design strategies of nitrogen-containing heterocyclic moieties for their anticancer activities[J].Eur J Med Chem,2017,125:143-189.
[52] Plano D,Amin S,Sharma AK.Importance of sphingosine kinase(SphK) as a target in developing cancer therapeutics and recent developments in the synthesis of novel SphK inhibitors[J].J Med Chem,2014,57(13):5509-5524.
[53] Cai J,Wei H,Hong KH,et al.Discovery,bioactivity and docking simulation of Vorinostat analogues containing 1,2,4-oxadiazole moiety as potent histone deacetylase inhibitors and antitumor agents[J].Bioorg Med Chem,2015,23(13):3457-3471.
[54] Moniot S,Forgione M,Lucidi A,et al.Development of 1,2,4-oxadiazoles as potent and selective inhibitors of the human deacetylase Sirtuin 2:Structure-activity relationship,X-ray crystal structure,and anticancer activity[J].J Med Chem,2017,60(6):2344-2360.
[55] Cai J,Wei H,Hong KH,et al.Discovery and preliminary evaluation of 2-aminobenzamide and hydroxamate derivatives containing 1,2,4-oxadiazole moiety as potent histone deacetylase inhibitors[J].Eur J Med Chem,2015,96:1-13.
[56] Xu LL,Zhang X,Jiang ZY,et al.Molecular similarity guided optimization of novel Nrf2 activators with 1,2,4-oxadiazole core[J].Bioorg Med Chem,2016,24(16):3540-3547.
[57] Kamal A,Reddy TS,Vishnuvardhan MVPS,et al.Synthesis of 2-aryl-1,2,4-oxadiazolo-benzimidazoles:Tubulin polymerization inhibitors and apoptosis inducing agents[J].Bioorg Med Chem,2015,23(15):4608-4623.
[58] Avanzo RE,Padron JM,D'Accorso NB,et al.Synthesis and in vitro antiproliferative activities of (5-aryl-1,2,4-oxadiazole-3-yl) methyl D-ribofuranosides[J].Bioorg Med Chem Lett,2017,27(16):3674-3677.
[59] Ragab FAF,Abou-Seri SM,Abdel-Aziz SA,et al.Design,synthesis and anticancer activity of new monastrol analogues bearing 1,3,4-oxadiazole moiety[J].Eur J Med Chem,2017,138:140-151.
[60] Naresh KR,Poornachandra Y,Nagender P,et al.Synthesis of novel nicotinohydrazide and (1,3,4-oxadiazol-2-yl)-6-(trifluoromethyl)pyridine derivatives as potential anticancer agents[J].Bioorg Med Chem Lett,2016,26(19):4829-4831.
[61] Hewitt MC,Leblanc Y,Gehling VS,et al.Development of methyl isoxazoleazepines as inhibitors of BET[J].Bioorg Med Chem Lett,2015,25(9):1842-1848.
[62] Basoglu A,Dirkmann S,Golpayegani NZ,et al.Oxadiazole-substituted naphtho[2,3-b]thiophene-4,9-diones as potent inhibitors of keratinocyte hyperproliferation.Structure activity relationships of the tricyclic quinone skeleton and the oxadiazole substituent[J].Eur J Med Chem,2017,134:119-132.
[63] Kovacs D,Wolfling J,Szabo N,et al.Efficient access to novel androsteno-17-(10,30,40)-oxadiazoles and 17b-(1',3',4')-thiadiazoles via N-substituted hydrazone and N,N'-disubstituted hydrazine intermediates,and their pharmacological evaluation in vitro[J].Eur J Med Chem,2015,98:13-29.
[64] Wurz RP,Pettus LH,Jackson C,et al.The discovery and optimization of aminooxadiazoles as potent Pim kinase inhibitors[J].Bioorg Med Chem Lett,2015,25(4):847-855.
[65] Mochona B,Qi X,Euynni S,et al.Design and evaluation of novel oxadiazole derivatives as potential prostate cancer agents[J].Bioorg Med Chem Lett,2016,26(12):2847-2851.
[66] Li YB,Yan X,Li RD,et al.Discovery of novel hetero-arylmethylcarbamodithioates as potent anticancer agents:Synthesis,structure-activity relationship analysis and biological evaluation[J].Eur J Med Chem,2016,112:217-230.
[67] Altintop MD,Sever B,Ciftci GA,et al.Design,synthesis,in vitro and in silico evaluation of a new series of oxadiazole-based anticancer agents as potential Akt and FAK inhibitors[J].Eur J Med Chem,2018,155:905-924.
[68] Fathi MAA,El-Hafeez AAA,Abdelhamid D,et al.1,3,4-oxadiazole/chalcone hybrids:Design,synthesis,and inhibition of leukemia cell growth and EGFR,Src,IL-6 and STAT3 activities[J].Bioorg Chem,2019,84:150-163.
[69] Al-Ghorbani M,Vigneshwaran V,Ranganatha VL,et al.Synthesis of oxadiazole–morpholine derivatives and manifestation of the repressed CD31 Microvessel Density(MVD) as tumoral angiogenic parameters in Dalton's Lymphoma[J].Bioorg Chem,2015,60:136-146.
[70] Zhao JJ,Wang XF,Li BL,et al.Synthesis and in vitro antiproliferative evaluation of novel nonsymmetrical disulfides bearing 1,3,4-oxadiazole moiety[J].Bioorg Med Chem Lett,2016,26(18):4414-4416.
[71] Rashid M,Husain A,Mishra R,et al.Design and synthesis of benzimidazoles containing substituted oxadiazole,thiadiazole and triazolo-thiadiazines as a source of new anticancer agents[J].Arab J Chem,2015.https://doi.org/10.1016/j.arabjc.2015.08.019.
[72] Akhtar MJ,Siddiqui AA,Khan AA,et al.Design,synthesis,docking and QSAR study of substituted benzimidazole linked oxadiazole as cytotoxic agents,EGFR and erbB2 receptor inhibitors[J].Eur J Med Chem,2017,126:853-869.
[73] Slawinski J,Szafranski K,Pogorzelska A,et al.Novel 2-benzylthio-5-(1,3,4-oxadiazol-2-yl)benzenesulfonamides with anticancer activity:Synthesis,QSAR study,and metabolic stability[J].Eur J Med Chem,2017,132:236-248.
[74] El-Din MMG,El-Gamal MI,Abdel-Maksoud MS,et al.Synthesis and in vitro antiproliferative activity of new 1,3,4-oxadiazole derivatives possessing sulfonamide moiety[J].Eur J Med Chem,2015,90:45-52.
[75] Yadagiri B,Gurrala S,Bantu R,et al.Synthesis and evaluation of benzosuberone embedded with 1,3,4-oxadiazole,1,3,4-thiadiazole and 1,2,4-triazole moieties as new potential anti proliferative agents[J].Bioorg Med Chem Lett,2015,25(10):2220-2224.
[76] Subba RAV,Vishnu VMVPS,Subba RNV,et al.Synthesis and biological evaluation of imidazopyridinyl-1,3,4-oxadiazole conjugates as apoptosis inducers and topoisomerase II( inhibitors[J].Bioorg Chem,2016,69:7-19.
[77] Kamal A,Srikanth PS,Vishnuvardhan MVPS,et al.Combretastatin linked 1,3,4-oxadiazole conjugates as a potent tubulin polymerization inhibitors[J].Bioorg Chem,2016,65:126-136.
[78] El-Din MMG,El-Gamal MI,Abdel-Maksoud MS,et al.Synthesis and broad-spectrum antiproliferative activity of diarylamides and diarylureas possessing 1,3,4-oxadiazole derivatives[J].Bioorg Med Chem Lett,2015,25(8):1692-1699.
[79] Pidugu VR,Yarla NS,Pedada SR,et al.Design and synthesis of novel HDAC8 inhibitory 2,5-disubstituted-1,3,4-oxadiazoles containing glycine and alanine hybrids with anticancer activity[J].Bioorg Med Chem,2016,24(21):5611-5617.
[80] Zhang F,Wang XL,Shi J,et al.Synthesis,molecular modeling and biological evaluation of N-benzylidene-2-((5-(pyridin-4-yl)-1,3,4-oxadiazol-2-yl)thio) acetohydrazide derivatives as potential anticancer agents[J].Bioorg Med Chem,2014,22(1):468-477.
[81] Li YT,Wang JH,Pan CW,et al.Syntheses and biological evaluation of 1,2,3-triazole and 1,3,4-oxadiazole derivatives of imatinib[J].Bioorg Med Chem Lett,2016,26(5):1419-1427.
[82] Chaves JDS,Tunes LG,Franco CHJ,et al.Novel gold(I) complexes with 5-phenyl-1,3,4-oxadiazole-2-thione and phosphine as potential anticancer and antileishmanial agents[J].Eur J Med Chem,2017,127:727-739.
[83] Porta F,Facchetti G,Ferri N,et al.An in vivo active 1,2,5-oxadiazole Pt(II) complex:A promising anticancer agent endowed with STAT3 inhibitory properties[J].Eur J Med Chem,2017,131:196-206.
[84] Sankhe NM,Durgashivaprasad E,Kutty NG,et al.Novel 2,5-disubstituted-1,3,4-oxadiazole derivatives induce apoptosis in HepG2 cells through p53 mediated intrinsic pathway[J].Arab J Chem,2015.http://dx.doi.org/10.1016/j.arabjc.2015.04.030.
[85] Sun J,Ren SZ,Lu XY,et al.Discovery of a series of 1,3,4-oxadiazole-2(3H)-thione derivatives containing piperazine skeleton as potential FAK inhibitors[J].Bioorg Med Chem,2017,25(9):2593-2600.
[86] Shahzad SA,Yar M,Bajda M,et al.Synthesis,thymidine phosphorylase inhibition and molecular modeling studies of 1,3,4-oxadiazole-2-thione derivatives[J].Bioorg Chem,2015,60:37-41.
[87] Labib MB,Philoppes JN,Lamie PF,et al.Azole-hydrazone derivatives:Design,synthesis,in vitro biological evaluation,dual EGFR/HER2 inhibitory activity,cell cycle analysis and molecular docking study as anticancer agents[J].Bioorg Chem,2018,76:67-80.
[88] El-Hady HA,Abubshait SA.Synthesis and anticancer evaluation of imidazolinone and benzoxazole derivatives[J].Arab J Chem,2017,10(2):S3725-S3731.
[89] Abdelgawad MA,Bakr RB,Omar HA.Design,synthesis and biological evaluation of some novel benzothiazole/benzoxazole and/or benzimidazole derivatives incorporating a pyrazole scaffold as antiproliferative agents[J].Bioorg Chem,2017,74:82-90.
[90] Sun M,Zhang X,Hao H,et al.Nocarbenzoxazoles A-G,benzoxazoles produced by halophilic Nocardiopsis lucentensis DSM 44048[J].J Nat Prod,2015,78(8):2123-2127.
[91] Zhang J,Yao D,Jiang Y,et al.Synthesis and biological evaluation of benzimidazole derivatives as the G9a Histone Methyltransferase inhibitors that induce autophagy and apoptosis of breast cancer cells[J].Bioorg Chem,2017,72:168-181.
[92] Costales A,Mathur M,Ramurthy S,et al.2-Amino-7-substituted benzoxazole analogs as potent RSK2 inhibitors[J].Bioorg Med Chem Lett,2014,24(6):1592-1596.
[93] An Y,Lee E,Yu Y,et al.Design and synthesis of novel benzoxazole analogs as Aurora B kinase inhibitors[J].Bioorg Med Chem Lett,2016,26(13):3067-3072.
[94] Vojtickova M,Dobias J,Hanquet G,et al.Ynamide click chemistry in development of triazole VEGFR2 TK modulators[J].Eur J Med Chem,2015,103:105-122.
[95] Salome C,Ribeiro N,Chavagnan T,et al.Benzofuran derivatives as anticancer inhibitors of mTOR signaling[J].Eur J Med Chem,2014,81:181-191.
[96] Ashwini N,Garg M,Mohan CD,et al.Synthesis of 1,2-benzisoxazole tethered 1,2,3-triazoles that exhibit anticancer activity in acute myeloid leukemia cell lines by inhibiting histone deacetylases,and inducing p21 and tubulin acetylation[J].Bioorg Med Chem,2015,23(18):6157-6165.
[97] Jiang X,Liu H,Song Z,et al.Discovery and SAR study of c-Met kinase inhibitors bearing an 3-amino-benzo[d]isoxazole or 3-aminoindazole scaffold[J].Bioorg Med Chem,2015,23(3):564-578.
[98] Maftei CV,Fodor E,Jones PG,et al.N-Heterocyclic carbenes(NHC) with 1,2,4-oxadiazole-substituents related to natural products:Synthesis,structure and potential antitumor activity of some corresponding gold(I) and silver(I) complexes[J].Eur J Med Chem,2015,101:431-441.