Combinatorial synthesis, lead identification, and antitumor study of a chalcone-based positional-scanning library.
作者： Bushra Mirza , Ahsan Ullah , Farzana Latif Ansari , Ihsan-ul-Haq , Samina Nazir
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摘要: A 175-member chalcone library was designed and synthesized from seven differently substituted acetophenones (A(1)-A(7)) 25 aryl or heteroaryl aldehydes (B(1)-B(25)). Potential lead compounds were identified by deconvolution of a two-dimensional matrix via positional scanning, the members most-active sub-libraries screened against crown-gall tumors with aid potato-disc assay. The resulting hits gave rise to significant antitumor activities, no antibacterial effect on tumor-producing bacterium Agrobacterium tumefaciens. Two structures, (2E)-3-(2-chlorophenyl)-1-phenylprop-2-en-1-one (A(1)B(9)) hydroxy analogue (2E)-3-(2-chlorophenyl)-1-(2-hydroxyphenyl)prop-2-en-1-one (A(2)B(9)), are promising candidates be developed into highly effective anticancer chemotherapeutics.
sci-hub.se 参考文章(59)
Karpas A, Viruses and leukemia. American Scientist. ,vol. 70, pp. 277- ,(1982)
The crown-gall potato disk bioassay as a primary screen for compounds with antitumor activity. Journal of the National Cancer Institute. ,vol. 67, pp. 689- 692 ,(1981) , 10.1093/JNCI/67.3.689
Edmund J. Moran, Sepehr Sarshar, John F. Cargill, Manouchehr M. Shahbaz, Anna Lio, Adnan M. M. Mjalli, Robert W. Armstrong, Radio Frequency Tag Encoded Combinatorial Library Method for the Discovery of Tripeptide-Substituted Cinnamic Acid Inhibitors of the Protein Tyrosine Phosphatase PTP1B Journal of the American Chemical Society. ,vol. 117, pp. 10787- 10788 ,(1995) , 10.1021/JA00148A039
Oliver Kayser, Albrecht F. Kiderlen, In vitro leishmanicidal activity of naturally occurring chalcones Phytotherapy Research. ,vol. 15, pp. 148- 152 ,(2001) , 10.1002/PTR.701
Michael C. Pirrung, Jrlung Chen, PREPARATION AND SCREENING AGAINST ACETYLCHOLINESTERASE OF A NON-PEPTIDE INDEXED COMBINATORIAL LIBRARY Journal of the American Chemical Society. ,vol. 117, pp. 1240- 1245 ,(1995) , 10.1021/JA00109A007
Sayed Alam, Synthesis, antibacterial and antifungal activity of some derivatives of 2-phenyl-chromen-4-one Journal of Chemical Sciences. ,vol. 116, pp. 325- 331 ,(2004) , 10.1007/BF02711433
Walter Glogowski, Alan G. Galsky, Agrobacterium tumefaciens Site Attachment as a Necessary Prerequisite for Crown Gall Tumor Formation on Potato Discs Plant Physiology. ,vol. 61, pp. 1031- 1033 ,(1978) , 10.1104/PP.61.6.1031
Yves Ambroise, Brian Yaspan, Mark H. Ginsberg, Dale L. Boger, Inhibitors of Cell Migration that Inhibit Intracellular Paxillin/α4 Binding: A Well-Documented Use of Positional Scanning Libraries Chemistry & Biology. ,vol. 9, pp. 1219- 1226 ,(2002) , 10.1016/S1074-5521(02)00246-6
B.A. Bhat, K.L. Dhar, S.C. Puri, A.K. Saxena, M. Shanmugavel, G.N. Qazi, Synthesis and biological evaluation of chalcones and their derived pyrazoles as potential cytotoxic agents. Bioorganic & Medicinal Chemistry Letters. ,vol. 15, pp. 3177- 3180 ,(2005) , 10.1016/J.BMCL.2005.03.121
Kit S. Lam, Sydney E. Salmon, Evan M. Hersh, Victor J. Hruby, Wieslaw M. Kazmierski, Richard J. Knapp, A new type of synthetic peptide library for identifying ligand-binding activity Nature. ,vol. 354, pp. 82- 84 ,(1992) , 10.1038/354082A0