Department of Chemistry



Kazunori Koide



1201 CHVRN
Chevron Science Center
219 Parkman Avenue

Pittsburgh, PA 15260

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Research Overview

Organic synthesis of natural products, new synthetic methods, and organic fluorescent sensors

Total Syntheses and Biological Studies of Natural Products

We are currently studying FR901464, a natural product that regulates cancer-related genes by novel mechanisms. This compound inhibits cancer proliferation at concentrations as low as 1 nM. To study FR901464, we completed a chemical total synthesis of this natural product. Combination of this powerful, stereocontrolled chemical synthesis and cell biology will provide insights into the molecular mechanisms of FR901464. More recently, we have developed an exceptionally active FR901464 analog (meayamycin) that inhibits tumor growth at 10 pM (analogouus to one pack of sugar (5 grams) at a coffee shop in 400 Olympic swimming pools).

Increased thermotolerance associated with tumors is a major problem in cancer radiotherapy, and such tolerance is mediated by heat shock proteins. Therefore, inhibitors of heat shock proteins are of great interest in medicine. Stresgenin B is a densely functionalized natural product that inhibits heat shock proteins. We have developed a new conjugate addition reaction and are applying this method to synthesize stresgenin B.

Development of Fluorescent Probes for Metals and Biomacromolecules

DNA transcription is the pivotal step in many cellular processes, and regulation of this complex biological event is essential for homeostasis. Currently available methods used to study this process do not enable real-time monitoring of DNA transcription in intact cells. To gain insights into the transient RNA levels of living cells in real-time, we are currently developing fluorescent sensors that visualize RNA.

Although palladium is widely used in synthetic organic chemistry and materials, it is known to be toxic. We have developed a fluorescent probe that can detect palladium in drugs. A commercial Pd detection kit is now available from Luminos, LLC.

Other fluorescent probe projects include the development of ultra-sensitive fluorescent probes for environmentally and biologically important molecules such as mercury and reactive oxygen species.

New Synthetic Methods

We are developing new synthetic methods based on the reactivity of alkynes and alkenes. Unique reactivities of zirconium, silver, tin, ruthenium, and other metals are being explored to discover new carbon-carbon bond forming reactions. Additionally, we developed new synthetic technology based on cross-olefin metathesis that allows for the synthesis of functionally diverse library compounds. Using this technology, highly functionalized library compounds are being synthesized in our laboratory.


  • Merck Technology Collaboration Award (2014)
  • University of Pittsburgh Chancellor's Distinguished Research Award, 2009
  • University of Pittsburgh Innovator Award, 2008
  • Thieme Chemistry Journals Award, 2007
  • Merck Fellow of the Cancer Research Fund of the Damon Runyon-Walter Winchell Foundation, 1998-2000
  • Naito Foundation Fellowship, 1991-1992


“Non-effervescent method for catalysis-based palladium detection with color or fluorescence,” Nieberding, M.; Tracey, M.P.; Koide, K. , ACS Sens., Vol. 2, 2017, Pages 1737-1743
“Synthesis of violaceic acid and related compounds through aryl triazene,” Ando, S.; Burrows, J.; Koide, K. , Org. Lett., Vol. 19, 2017, Pages 1116-1119
“Online sensing of palladium in flowing streams,” Bu, X. D.; Williams, M.; Jo, J.; Koide, K.; Welch, C. J. , Chem. Commun. , Vol. 53, 2017, Pages 720-723
“A competitive and reversible deactivation approach to catalysis-based quantitative assays,” Koide, K.; Tracey, M. P.; Bu, X.; Jo, J.; Williams, M. J.; Welch, C. J. , Nat. Commun., Vol. 7, 2016, Pages Article Number 10691
“The SF3B1 inhibitor spliceostatin A (SSA) elicits apoptosis in Chronic Lymphocytic Leukemia cells through downregulation of Mcl-1,” Larrayoz, M.; Blakemore, S. J.; Dobson, R. C.; Blunt, M. D.; Rose-Zerilli, M. J.; Walewska, R.; Duncombe, A.; Oscier, D.; Koide, K.; Forconi, F.; Packham, G.; Yoshida, M.; Cragg, M. S.; Strefford, J. C.; Steele, A. J. , Leukemia, Vol. 30, 2016, Pages 351–360
“Fluorometric imaging methods for palladium and platinum and the use of palladium for imaging biomolecules,” Tracey, M. P.; Pham, D.; Koide, K. , Chem. Soc. Rev., Vol. 44, 2015, Pages 4769–4791
“An siRNA screen identifies the U2 snRNP spliceosome as a host restriction factor for recombinant adeno-associated viruses,” Schreiber, C. A.; Sakuma, T.; Izumiya, Y.; Holditch, S. J.; Hickey, R. D.; Bressin, R. K.; Basu, U.; Koide, K.; Asokan, A.; Ikeda, Y. , PLoS Pathog., Vol. 11, 2015, Pages e1005082
“Time-insensitive fluorescent sensor for human serum albumin and its unusual red shift,” Smith, S. E.; Williams, J. M.; Ando, S.; Koide, K. , Anal. Chem. , Vol. 86, 2014, Pages 2332–2336
“Palladium detection technologies for active pharmaceutical ingredients via cross-coupling,” Koide, K. , Recent Trends in Cross Couplings; Colacot, T., Ed., 2014,
“Regulation of HPV16 E6 and MCL1 by SF3B1 inhibitor in head and neck cancer cells,” Gao, Y.; Trivedi, S.; Ferris, R. L., Koide, K. , Sci. Rep., Vol. 4, 2014, Pages 6098
“Total synthesis and biological studies of TMC-205 and analogues as anticancer agents and activators of SV40 promoter,” Gao, Y.; Osman, S.; Koide, K. , ACS Med. Chem. Lett, Vol. 5, 2014, Pages 863–867
“Chemical perturbation of Mcl-1 pre-mRNA splicing to induce apoptosis in cancer cells,” Gao, Y.; Koide, K.,, ACS Chem. Biol., Vol. 8, 2013, Pages 895–900
“A high throughput method to detect palladium in ores,” Williams, J. M.; Koide, K., Ind. Eng. Chem. Res., Vol. 52, 2013, Pages 8612–8615
“Rapid analysis of residual palladium in pharmaceutical development using a catalysis-based fluorometric method,” Bu, X., Koide, K., Carder, E.J., and Welch, C.J., Org. Process Res. Dev., Vol. 17, 2013, Pages 108-113
“Comparison of splicing factor 3b inhibitors in human cells,” Gao, Y., Vogt, A., Forsyth, J., and Koide, K., ChemBioChem, Vol. 14, 2013, Pages 49-52
“Ruthenium-catalyzed olefin metathesis after tetra-n-butylammonium fluoride-mediated desilylation,” Osman, S., and Koide, K., Tetrahedron Lett., Vol. 53, 2012, Pages 6637-6640
“SF3B1 haploinsufficiency leads to formation of ring sideroblasts in myelodysplastic syndromes,” Visconte, V., Rogers, H.J., Singh, J., Barnard, J., Bupathi, M., Traina, F., McMahon, J., Makishima, H., Szpurka, A., Jankowska A., Jerez, A., Sekeres, M.A., Saunthararajah, Y., Advani, A.S., Copelan, E., Koseki, H., Isono, K., Padgett, R.A., Osman, S., Koide, K., O'Keefe, C., Maciejewski, J.P., and Tiu, R.V., Blood, Vol. 120, 2012, Pages 3173-3186
“Diastereoselective synthesis of diketopiperazine bis-α,β-epoxides,” Ando, S., Grote, A. L., and Koide, K., J. Org. Chem., Vol. 76, 2011, Pages 1155-1158
“Development and applications of fluorogenic probes for mercury(II) based on vinyl ether oxymercuration,” Ando, S., and Koide, K., J. Am. Chem. Soc., Vol. 133, 2011, Pages 2556-2566
“Structural requirements for the antiproliferative activity of pre-mRNA splicing inhibitor FR901464,” Osman, S., Albert, B. J., Wang, Y., Li, M., Czaicki, N. L., Koide, K., Chem.-Eur. J., Vol. 17, 2011, Pages 895–904
“Meayamycin inhibits pre-mRNA splicing and exhibits picomolar activity against multidrug resistant cells,” B. J. Albert, P. A. McPherson, K. O'Brien, N. L. Czaicki, V. DeStefino, S. Osman, M. Li, B. W. Day, P. J. Grabowski, M. Moore, A. Vogt, K. Koide, Mol. Cancer Ther., Vol. 8, 2009, Pages 2308-2318
“Specific fluorogenic probes for ozone in biological and atmospheric samples,” A. L. Garner, C. M. St. Croix, B. R. Pitt, G. D. Leikauf, S. Ando, and K. Koide, Nature Chem., Vol. 1, 2009, Pages 316-321