ACS Combinatorial Science
Research Article
caspase-based high throughput screening assay. 4. Structure−activity
relationships of N-alkyl substituted pyrrole fused at the 7,8-positions. J.
Med. Chem. 2008, 51, 417−423.
ASSOCIATED CONTENT
* Supporting Information
Details of experimental procedures and compound character-
ization data for synthesized compounds. This material is
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S
(7) Kemnitzer, W.; Jiang, S.; Wang, Y.; Kasibhatla, S.; Crogan-
Grundy, C.; Bubenik, M.; Labrecque, D.; Denis, R.; Lamothe, S.;
Attardo, G.; Gourdeau, H.; Tseng, B.; Drewe, J.; Cai, S. X. Discovery
of 4-aryl-4H-chromenes as a new series of apoptosis inducers using a
cell- and caspase-based HTS assay. Part 5: Modifications of the 2- and
3-positions. Bioorg. Med. Chem. Lett. 2008, 18, 603−607.
(8) Gourdeau, H.; Leblond, L.; Hamelin, B.; Desputeau, C.; Dong,
K.; Kianicka, I.; Custeau, D.; Boudreau, C.; Geerts, L.; Cai, S.-X.;
Drewe, J.; Labrecque, D.; Kasibhatla, S.; Tseng, B. Antivascular and
antitumor evaluation of 2-amino-4-(3-bromo-4,5-dimethoxy-phenyl)-
3-cyano-4H-chromenes, a novel series of anticancer agents. Mol.
Cancer Ther. 2004, 3, 1375−1384.
AUTHOR INFORMATION
Corresponding Author
+7(499)1355328.
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Present Address
§State Scientific Research Institute of Organic Chemistry and
Technology, 23 Sh. Entuziastov, 111024, Moscow, Russian
Federation
(9) Litvinov, Yu. M.; Shestopalov, A. M. Synthesis, structure,
chemical reactivity, and practical significance of 2-amino-4H-pyrans. In
Advances in Heterocyclic Chemistry; Katritzky, A. R., Ed.; Elsevier:
London, UK, 2011; Vol 103, Chapter 3, pp 175−260.
(10) (a) Cai, S. X.; Drewe, J.; Kemnitzer, W. Discovery of 4-aryl-4H-
chromenes as potent apoptosis inducers using a cell- and caspase-
based anti-cancer screening apoptosis program (ASAP): SAR studies
and the identification of novel vascular disrupting agents. Anti-Cancer
Corporation. All Rights Reserved. (c) ClinicalTrials.gov Identifier:
NCT01240590.
Funding
This work was supported by a grant from Chemical Block Ltd.
Notes
The authors declare no competing financial interest.
ACKNOWLEDGMENTS
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We thank the National Cancer Institute (NCI) (Bethesda, MD,
USA) for screening compounds 5{3,1}, 5{1,2}, 5{5,4}, 5{1,5},
and 5{5,5} by the Developmental Therapeutics Program at
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Janik, M. E.; Bhattacharyya, B. Oxalone and lactone moieties of
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ABBREVIATIONS
PT, podophyllotoxin; SAR, structure−activity relationship
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dx.doi.org/10.1021/co300062e | ACS Comb. Sci. 2012, 14, 484−490