Integrated Platform for Expedited Synthesis-Purification-Testing of Small Molecule Libraries

ACS Medicinal Chemistry Letters

Volumn 8, Issue 4, 2017, Pages 461-465

  Baranczak, Aleksandra ^a   Tu, Noah P ^a   Marjanovic, Jasmina ^b   Searle, Philip A ^b   Vasudevan, Anil ^b   Djuric, Stevan W ^b  

^a AbbVie Inc ^*

^b ABBVIE INC   (United States)

Author keywords

automated drug discovery; Automated synthesis; bioassay; EED; purification

Indexed keywords

EMBRYONIC ECTODERM DEVELOPMENT PROTEIN;

ARTICLE; CHEMICAL MODIFICATION; DRUG DETERMINATION; DRUG PURIFICATION; DRUG SCREENING; DRUG SOLUBILITY; DRUG SYNTHESIS; LABORATORY AUTOMATION; MEDICINAL CHEMISTRY; MOLECULAR LIBRARY; PRIORITY JOURNAL; TURNAROUND TIME;

EID: 85017566918     PISSN: None     EISSN: 19485875     Source Type: Journal    
DOI: 10.1021/acsmedchemlett.7b00054     Document Type: Article

References (12)

1. Nettekoven, M.; Thomas, A. W. Accelerating drug discovery by integrative implementation of laboratory automation in the work flow Curr. Med. Chem. 2002, 9, 2179-2190 10.2174/0929867023368764
2. Desai, B.; Dixon, K.; Farrant, E.; Feng, Q.; Gibson, K. R.; van Hoorn, W. P.; Mills, J.; Morgan, T.; Parry, D. M.; Ramjee, M. K.; Selway, C. N.; Tarver, G. J.; Whitlock, G.; Wright, A. G. Rapid discovery of a novel series of Abl kinase inhibitors by application of an integrated microfluidic synthesis and screening platform J. Med. Chem. 2013, 56, 3033-3047 10.1021/jm400099d
3. Czechtizky, W.; Dedio, J.; Desai, B.; Dixon, K.; Farrant, E.; Feng, Q.; Morgan, T.; Parry, D. M.; Ramjee, M. K.; Selway, C. N.; Schmidt, T.; Tarver, G. J.; Wright, A. G. Integrated Synthesis and Testing of Substituted Xanthine Based DPP4 Inhibitors: Application to Drug Discovery ACS Med. Chem. Lett. 2013, 4, 768-772 10.1021/ml400171b
4. Werner, M.; Kuratli, C.; Martin, R. E.; Hochstrasser, R.; Wechsler, D.; Enderle, T.; Alanine, A. I.; Vogel, H. Seamless integration of dose-response screening and flow chemistry: efficient generation of structure-activity relationship data of beta-secretase (BACE1) inhibitors Angew. Chem., Int. Ed. 2014, 53, 1704-1708 10.1002/anie.201309301
5. Hochlowski, J. E.; Searle, P. A.; Tu, N. P.; Pan, J. Y.; Spanton, S. G.; Djuric, S. W. An Integrated Synthesis-Purification System to Accelerate the Generation of Compounds in Pharmaceutical Discovery J. Flow Chem. 2011, 2, 56-61 10.1556/jfchem.2011.00013
6. Sutherland, J. D.; Tu, N. P.; Nemcek, T. A.; Searle, P. A.; Hochlowski, J. E.; Djuric, S. W.; Pan, J. Y. An Automated Synthesis-Purification-Sample-Management Platform for the Accelerated Generation of Pharmaceutical Candidates J. Lab. Aut. 2014, 19, 176-182 10.1177/2211068213516325
7. Tu, N. P.; Sarris, K.; Searle, P. A. An Automated Microwave Assisted Synthesis-Purification System for Rapid Generation of Compound Libraries J. Lab. Aut. 2016, 21, 459-469 10.1177/2211068215590580
8. Di Croce, L.; Helin, K. Transcriptional regulation by Polycomb group proteins Nat. Struct. Mol. Biol. 2013, 20, 1147-1155 10.1038/nsmb.2669
9. He, Y.; Selvaraju, S.; Curtin, M. L.; Jakob, C. G.; Zhu, H.; Comess, K. M.; Shaw, B.; Galasinski, S.; The, J.; Lima-Fernandes, E.; Szewczyk, M.; Cheng, D.; Klinge, K. L.; Li, H.-Q.; Pliushchev, M.; Algire, M. A.; Maag, D.; Guo, J.; Panchal, S. C.; Sweis, R. F.; Torrent, M.; Bigelow, L. J.; Senisterra, G.; Li, F.; Kennedy, S.; Wu, Q.; Osterling, D. J.; Lindley, D. J.; Gao, W.; Petros, A. M.; Dietrich, J.; Barsyte-Lovejoy, D.; Vedadi, M.; Arrowsmith, C. H.; Chiang, G. G.; Sun, C.; Pappano, W. N.; Buchanan, F. G. The EED protein-protein interaction inhibitor A-395 inactivates the PRC2 complex Nat. Chem. Biol. 2017, 13, 389 10.1038/nchembio.2306
10. Curtin, M. L.; Pliushchev, M. A.; Li, H. Q.; Torrent, M.; Dietrich, J. D.; Jakob, C. G.; Zhu, H.; Zhao, H.; Wang, Y.; Ji, Z.; Clark, R. F.; Sarris, K. A.; Selvaraju, S.; Shaw, B.; Algire, M. A.; He, Y.; Richardson, P. L.; Sweis, R. F.; Sun, C.; Chiang, G. G.; Michaelides, M. R. Amino pyrrolidines as potent and novel protein-protein interaction inhibitors of the PRC2 complex Bioorg. Med. Chem. Lett. 2017, 27, 1576 10.1016/j.bmcl.2017.02.030
11. Almeling, S.; Ilko, D.; Holzgrabe, U. Charged aerosol detection in pharmaceutical analysis J. Pharm. Biomed. Anal. 2012, 69, 50-63 10.1016/j.jpba.2012.03.019
12. Dixon, R. W.; Peterson, D. S. Development and testing of a detection method for liquid chromatography based on aerosol charging Anal. Chem. 2002, 74, 2930-2937 10.1021/ac011208l