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Items: 1 to 50 of 449

1.

DNA Binding and Cleavage Modes of Shishijimicin A.

Zhang H, Li R, Ba S, Lu Z, Pitsinos EN, Li T, Nicolaou KC.

J Am Chem Soc. 2019 May 15;141(19):7842-7852. doi: 10.1021/jacs.9b01800. Epub 2019 May 3.

PMID:
31050893
2.

The Role of Organic Synthesis in the Emergence and Development of Antibody-Drug Conjugates as Targeted Cancer Therapies.

Nicolaou KC, Rigol S.

Angew Chem Int Ed Engl. 2019 Aug 12;58(33):11206-11241. doi: 10.1002/anie.201903498. Epub 2019 Jul 8. Review.

PMID:
31012193
3.

Correction to "Short Total Synthesis of Δ12-Prostaglandin J2 and Related Prostaglandins. Design, Synthesis, and Biological Evaluation of Macrocyclic Δ12-Prostaglandin J2 Analogues".

Nicolaou KC, Pulukuri KK, Rigol S, Peitsinis Z, Yu R, Kishigami S, Cen N, Aujay M, Sandoval J, Zepeda N, Gavrilyuk J.

J Org Chem. 2019 Feb 15;84(4):2377-2378. doi: 10.1021/acs.joc.9b00159. Epub 2019 Feb 4. No abstract available.

PMID:
30715889
4.

Total Synthesis in Search of Potent Antibody-Drug Conjugate Payloads. From the Fundamentals to the Translational.

Nicolaou KC, Rigol S.

Acc Chem Res. 2019 Jan 15;52(1):127-139. doi: 10.1021/acs.accounts.8b00537. Epub 2018 Dec 21.

PMID:
30575399
5.

Short Total Synthesis of Δ12-Prostaglandin J2 and Related Prostaglandins. Design, Synthesis, and Biological Evaluation of Macrocyclic Δ12-Prostaglandin J2 Analogues.

Nicolaou KC, Pulukuri KK, Rigol S, Peitsinis Z, Yu R, Kishigami S, Cen N, Aujay M, Sandoval J, Zepeda N, Gavrilyuk J.

J Org Chem. 2019 Jan 4;84(1):365-378. doi: 10.1021/acs.joc.8b03057. Epub 2018 Dec 20. Erratum in: J Org Chem. 2019 Feb 15;84(4):2377-2378.

PMID:
30557504
6.

Syntheses of Cyclopropyl Analogues of Disorazoles A1 and B1 and Their Thiazole Counterparts.

Nicolaou KC, Buchman M, Bellavance G, Krieger J, Subramanian P, Pulukuri KK.

J Org Chem. 2018 Oct 19;83(20):12374-12389. doi: 10.1021/acs.joc.8b02137. Epub 2018 Oct 2.

PMID:
30277774
7.

Streamlined Total Synthesis of Shishijimicin A and Its Application to the Design, Synthesis, and Biological Evaluation of Analogues thereof and Practical Syntheses of PhthNSSMe and Related Sulfenylating Reagents.

Nicolaou KC, Li R, Lu Z, Pitsinos EN, Alemany LB, Aujay M, Lee C, Sandoval J, Gavrilyuk J.

J Am Chem Soc. 2018 Sep 26;140(38):12120-12136. doi: 10.1021/jacs.8b06955. Epub 2018 Sep 14.

PMID:
30216054
9.

Total Synthesis and Full Structural Assignment of Namenamicin.

Nicolaou KC, Li R, Lu Z, Pitsinos EN, Alemany LB.

J Am Chem Soc. 2018 Jul 5;140(26):8091-8095. doi: 10.1021/jacs.8b04592. Epub 2018 Jun 22.

PMID:
29932325
10.

Improved Total Synthesis of Tubulysins and Design, Synthesis, and Biological Evaluation of New Tubulysins with Highly Potent Cytotoxicities against Cancer Cells as Potential Payloads for Antibody-Drug Conjugates.

Nicolaou KC, Erande RD, Yin J, Vourloumis D, Aujay M, Sandoval J, Munneke S, Gavrilyuk J.

J Am Chem Soc. 2018 Mar 14;140(10):3690-3711. doi: 10.1021/jacs.7b12692. Epub 2018 Jan 30.

PMID:
29381062
11.

Enantioselective Total Synthesis of Antibiotic CJ-16,264, Synthesis and Biological Evaluation of Designed Analogues, and Discovery of Highly Potent and Simpler Antibacterial Agents.

Nicolaou KC, Pulukuri KK, Rigol S, Buchman M, Shah AA, Cen N, McCurry MD, Beabout K, Shamoo Y.

J Am Chem Soc. 2017 Nov 8;139(44):15868-15877. doi: 10.1021/jacs.7b08749. Epub 2017 Oct 24.

12.

Total Syntheses of Disorazoles A₁ and B₁ and Full Structural Elucidation of Disorazole B₁.

Nicolaou KC, Bellavance G, Buchman M, Pulukuri KK.

J Am Chem Soc. 2017 Nov 8;139(44):15636-15639. doi: 10.1021/jacs.7b09843. Epub 2017 Oct 24.

PMID:
29064682
13.

Streamlined Total Synthesis of Trioxacarcins and Its Application to the Design, Synthesis, and Biological Evaluation of Analogues Thereof. Discovery of Simpler Designed and Potent Trioxacarcin Analogues.

Nicolaou KC, Chen P, Zhu S, Cai Q, Erande RD, Li R, Sun H, Pulukuri KK, Rigol S, Aujay M, Sandoval J, Gavrilyuk J.

J Am Chem Soc. 2017 Nov 1;139(43):15467-15478. doi: 10.1021/jacs.7b08820. Epub 2017 Oct 20.

PMID:
29052423
14.

Experimental Evolution of Diverse Strains as a Method for the Determination of Biochemical Mechanisms of Action for Novel Pyrrolizidinone Antibiotics.

Beabout K, McCurry MD, Mehta H, Shah AA, Pulukuri KK, Rigol S, Wang Y, Nicolaou KC, Shamoo Y.

ACS Infect Dis. 2017 Nov 10;3(11):854-865. doi: 10.1021/acsinfecdis.7b00135. Epub 2017 Sep 27.

15.

A brief history of antibiotics and select advances in their synthesis.

Nicolaou KC, Rigol S.

J Antibiot (Tokyo). 2018 Feb;71(2):153-184. doi: 10.1038/ja.2017.62. Epub 2017 Jul 5. Review.

PMID:
28676714
16.

12,13-Aziridinyl Epothilones. Stereoselective Synthesis of Trisubstituted Olefinic Bonds from Methyl Ketones and Heteroaromatic Phosphonates and Design, Synthesis, and Biological Evaluation of Potent Antitumor Agents.

Nicolaou KC, Rhoades D, Wang Y, Bai R, Hamel E, Aujay M, Sandoval J, Gavrilyuk J.

J Am Chem Soc. 2017 May 31;139(21):7318-7334. doi: 10.1021/jacs.7b02655. Epub 2017 May 17.

PMID:
28513142
17.

Asymmetric Alkylation of Anthrones, Enantioselective Total Synthesis of (-)- and (+)-Viridicatumtoxins B and Analogues Thereof: Absolute Configuration and Potent Antibacterial Agents.

Nicolaou KC, Liu G, Beabout K, McCurry MD, Shamoo Y.

J Am Chem Soc. 2017 Mar 15;139(10):3736-3746. doi: 10.1021/jacs.6b12654. Epub 2017 Mar 3.

18.

Total Synthesis of Thailanstatin A.

Nicolaou KC, Rhoades D, Lamani M, Pattanayak MR, Kumar SM.

J Am Chem Soc. 2016 Jun 22;138(24):7532-5. doi: 10.1021/jacs.6b04781. Epub 2016 Jun 13.

PMID:
27266914
19.

Streamlined Total Synthesis of Uncialamycin and Its Application to the Synthesis of Designed Analogues for Biological Investigations.

Nicolaou KC, Wang Y, Lu M, Mandal D, Pattanayak MR, Yu R, Shah AA, Chen JS, Zhang H, Crawford JJ, Pasunoori L, Poudel YB, Chowdari NS, Pan C, Nazeer A, Gangwar S, Vite G, Pitsinos EN.

J Am Chem Soc. 2016 Jul 6;138(26):8235-46. doi: 10.1021/jacs.6b04339. Epub 2016 Jun 27.

PMID:
27266267
20.

Total Synthesis of Δ(12) -Prostaglandin J3 : Evolution of Synthetic Strategies to a Streamlined Process.

Nicolaou KC, Pulukuri KK, Yu R, Rigol S, Heretsch P, Grove CI, Hale CR, ElMarrouni A.

Chemistry. 2016 Jun 13;22(25):8559-70. doi: 10.1002/chem.201601449. Epub 2016 May 17.

PMID:
27187634
21.

Synthesis and Biological Investigation of Δ(12)-Prostaglandin J3 (Δ(12)-PGJ3) Analogues and Related Compounds.

Nicolaou KC, Pulukuri KK, Rigol S, Heretsch P, Yu R, Grove CI, Hale CR, ElMarrouni A, Fetz V, Brönstrup M, Aujay M, Sandoval J, Gavrilyuk J.

J Am Chem Soc. 2016 May 25;138(20):6550-60. doi: 10.1021/jacs.6b02075. Epub 2016 May 12.

PMID:
27171618
22.

Efficient Synthesis of Dimeric Oxazoles, Piperidines and Tetrahydroisoquinolines from N-Substituted 2-Oxazolones.

He Y, Agarwal PK, Kiran IN, Yu R, Cao B, Zou C, Zhou X, Xu H, Xu B, Zhu L, Lan Y, Nicolaou KC.

Chemistry. 2016 Jun 1;22(23):7696-701. doi: 10.1002/chem.201601471. Epub 2016 Apr 26.

PMID:
27113382
23.

Selective activation of TNFR1 and NF-κB inhibition by a novel biyouyanagin analogue promotes apoptosis in acute leukemia cells.

Savva CG, Totokotsopoulos S, Nicolaou KC, Neophytou CM, Constantinou AI.

BMC Cancer. 2016 Apr 20;16:279. doi: 10.1186/s12885-016-2310-5.

24.

Susceptibilities of enterovirus D68, enterovirus 71, and rhinovirus 87 strains to various antiviral compounds.

Smee DF, Evans WJ, Nicolaou KC, Tarbet EB, Day CW.

Antiviral Res. 2016 Jul;131:61-5. doi: 10.1016/j.antiviral.2016.04.003. Epub 2016 Apr 7.

25.

Total Synthesis of Trioxacarcins DC-45-A1, A, D, C, and C7″-epi-C and Full Structural Assignment of Trioxacarcin C.

Nicolaou KC, Cai Q, Sun H, Qin B, Zhu S.

J Am Chem Soc. 2016 Mar 9;138(9):3118-24. doi: 10.1021/jacs.5b12687. Epub 2016 Feb 24.

PMID:
26910506
26.

Total Synthesis and Biological Evaluation of Natural and Designed Tubulysins.

Nicolaou KC, Yin J, Mandal D, Erande RD, Klahn P, Jin M, Aujay M, Sandoval J, Gavrilyuk J, Vourloumis D.

J Am Chem Soc. 2016 Feb 10;138(5):1698-708. doi: 10.1021/jacs.5b12557. Epub 2016 Feb 1.

PMID:
26829208
27.

Synthesis and Biopharmaceutical Evaluation of Imatinib Analogues Featuring Unusual Structural Motifs.

Nicolaou KC, Vourloumis D, Totokotsopoulos S, Papakyriakou A, Karsunky H, Fernando H, Gavrilyuk J, Webb D, Stepan AF.

ChemMedChem. 2016 Jan 5;11(1):31-7. doi: 10.1002/cmdc.201500510. Epub 2015 Nov 20.

PMID:
26585829
28.

Synthesis and Biological Evaluation of Novel Epothilone B Side Chain Analogues.

Nicolaou KC, Rhoades D, Wang Y, Totokotsopoulos S, Bai R, Hamel E.

ChemMedChem. 2015 Dec;10(12):1974-9. doi: 10.1002/cmdc.201500401. Epub 2015 Oct 8.

PMID:
26447977
29.

Practical Synthesis of p- and o-Amino- and Methoxyphenolic Anthraquinones.

Nicolaou KC, Lu M, Chen P, Shah AA.

Angew Chem Int Ed Engl. 2015 Oct 19;54(43):12687-91. doi: 10.1002/anie.201507007. Epub 2015 Aug 31.

PMID:
26332286
30.

Total Synthesis of Shishijimicin A.

Nicolaou KC, Lu Z, Li R, Woods JR, Sohn TI.

J Am Chem Soc. 2015 Jul 15;137(27):8716-9. doi: 10.1021/jacs.5b05575. Epub 2015 Jul 2.

PMID:
26133230
31.

Total Synthesis and Structural Revision of Antibiotic CJ-16,264.

Nicolaou KC, Shah AA, Korman H, Khan T, Shi L, Worawalai W, Theodorakis EA.

Angew Chem Int Ed Engl. 2015 Aug 3;54(32):9203-8. doi: 10.1002/anie.201504337. Epub 2015 Jun 19.

32.

Synthesis and biological evaluation of dimeric furanoid macroheterocycles: discovery of new anticancer agents.

Nicolaou KC, Nilewski C, Hale CR, Ahles CF, Chiu CA, Ebner C, ElMarrouni A, Yang L, Stiles K, Nagrath D.

J Am Chem Soc. 2015 Apr 15;137(14):4766-70. doi: 10.1021/jacs.5b00141. Epub 2015 Apr 1.

PMID:
25827338
33.

Total synthesis of trioxacarcin DC-45-A2.

Nicolaou KC, Cai Q, Qin B, Petersen MT, Mikkelsen RJ, Heretsch P.

Angew Chem Int Ed Engl. 2015 Mar 2;54(10):3074-8. doi: 10.1002/anie.201410369. Epub 2015 Jan 12.

PMID:
25583408
34.

Synthesis and biological evaluation of QRSTUVWXYZA' domains of maitotoxin.

Nicolaou KC, Heretsch P, Nakamura T, Rudo A, Murata M, Konoki K.

J Am Chem Soc. 2014 Nov 19;136(46):16444-51. doi: 10.1021/ja509829e. Epub 2014 Nov 6.

35.

Total synthesis of viridicatumtoxin B and analogues thereof: strategy evolution, structural revision, and biological evaluation.

Nicolaou KC, Hale CR, Nilewski C, Ioannidou HA, ElMarrouni A, Nilewski LG, Beabout K, Wang TT, Shamoo Y.

J Am Chem Soc. 2014 Aug 27;136(34):12137-60. doi: 10.1021/ja506472u. Epub 2014 Aug 15.

36.

In vitro chronic effects on hERG channel caused by the marine biotoxin azaspiracid-2.

Ferreiro SF, Vilariño N, Louzao MC, Nicolaou KC, Frederick MO, Botana LM.

Toxicon. 2014 Dec;91:69-75. doi: 10.1016/j.toxicon.2014.09.012. Epub 2014 Oct 5.

37.

The chemistry-biology-medicine continuum and the drug discovery and development process in academia.

Nicolaou KC.

Chem Biol. 2014 Sep 18;21(9):1039-45. doi: 10.1016/j.chembiol.2014.07.020.

38.

Total synthesis of myceliothermophins C, D, and E.

Nicolaou KC, Shi L, Lu M, Pattanayak MR, Shah AA, Ioannidou HA, Lamani M.

Angew Chem Int Ed Engl. 2014 Oct 6;53(41):10970-4. doi: 10.1002/anie.201406815. Epub 2014 Aug 27.

39.

Total synthesis of Δ¹²-prostaglandin J₃, a highly potent and selective antileukemic agent.

Nicolaou KC, Heretsch P, ElMarrouni A, Hale CR, Pulukuri KK, Kudva AK, Narayan V, Prabhu KS.

Angew Chem Int Ed Engl. 2014 Sep 22;53(39):10443-7. doi: 10.1002/anie.201404917. Epub 2014 Aug 5.

40.

Marinopyrrole derivatives with sulfide spacers as selective disruptors of Mcl-1 binding to pro-apoptotic protein Bim.

Cheng C, Liu Y, Balasis ME, Garner TP, Li J, Simmons NL, Berndt N, Song H, Pan L, Qin Y, Nicolaou KC, Gavathiotis E, Sebti SM, Li R.

Mar Drugs. 2014 Jul 29;12(8):4311-25. doi: 10.3390/md12084311.

41.

Advancing the drug discovery and development process.

Nicolaou KC.

Angew Chem Int Ed Engl. 2014 Aug 25;53(35):9128-40. doi: 10.1002/anie.201404761. Epub 2014 Jul 13.

PMID:
25045053
42.

Academic-industrial partnerships in drug discovery and development.

Nicolaou KC.

Angew Chem Int Ed Engl. 2014 May 5;53(19):4730-1. doi: 10.1002/anie.201402816. Epub 2014 Apr 6. No abstract available.

PMID:
24706618
43.
44.

Cyclic marinopyrrole derivatives as disruptors of Mcl-1 and Bcl-x(L) binding to Bim.

Cheng C, Liu Y, Balasis ME, Simmons NL, Li J, Song H, Pan L, Qin Y, Nicolaou KC, Sebti SM, Li R.

Mar Drugs. 2014 Mar 7;12(3):1335-48. doi: 10.3390/md12031335.

45.

Microsphere-based immunoassay for the detection of azaspiracids.

Rodríguez LP, Vilariño N, Louzao MC, Dickerson TJ, Nicolaou KC, Frederick MO, Botana LM.

Anal Biochem. 2014 Feb 15;447:58-63. doi: 10.1016/j.ab.2013.10.035. Epub 2013 Nov 8.

46.

Synthesis and antioxidant evaluation of (S,S)- and (R,R)-secoisolariciresinol diglucosides (SDGs).

Mishra OP, Simmons N, Tyagi S, Pietrofesa R, Shuvaev VV, Valiulin RA, Heretsch P, Nicolaou KC, Christofidou-Solomidou M.

Bioorg Med Chem Lett. 2013 Oct 1;23(19):5325-8. doi: 10.1016/j.bmcl.2013.07.062. Epub 2013 Aug 2.

47.

In vivo arrhythmogenicity of the marine biotoxin azaspiracid-2 in rats.

Ferreiro SF, Vilariño N, Carrera C, Louzao MC, Santamarina G, Cantalapiedra AG, Rodríguez LP, Cifuentes JM, Vieira AC, Nicolaou KC, Frederick MO, Botana LM.

Arch Toxicol. 2014 Feb;88(2):425-34. doi: 10.1007/s00204-013-1115-4. Epub 2013 Aug 11.

48.

Total synthesis and structural revision of viridicatumtoxin B.

Nicolaou KC, Nilewski C, Hale CR, Ioannidou HA, ElMarrouni A, Koch LG.

Angew Chem Int Ed Engl. 2013 Aug 12;52(33):8736-41. doi: 10.1002/anie.201304691. Epub 2013 Jul 24. No abstract available.

49.

Synthesis and biological evaluation of new paclitaxel analogs and discovery of potent antitumor agents.

Nicolaou KC, Valiulin RA.

Org Biomol Chem. 2013 Jul 7;11(25):4154-63. doi: 10.1039/c3ob40654g.

50.

General synthetic approach to functionalized dihydrooxepines.

Nicolaou KC, Yu R, Shi L, Cai Q, Lu M, Heretsch P.

Org Lett. 2013 Apr 19;15(8):1994-7. doi: 10.1021/ol4006689. Epub 2013 Apr 4.

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