32690-76-9Relevant academic research and scientific papers
Design of tRNALys3 Ligands: Fragment evolution and linker selection guided by NMR spectroscopy
Chung, Florence,Tisne, Carine,Lecourt, Thomas,Seijo, Bili,Dardel, Frederic,Micouin, Laurent
scheme or table, p. 7108 - 7116 (2010/04/05)
A fragment-based approach for the synthesis of ligands of tRNA Lys3, the HIV reverse-transcription primer, is described. The use of NMR spectroscopy has proved to be very useful in this approach, not only to detect lowaffinity complexes between small compounds and RNA, but also to provide information on their binding mode and on the way they can be connected. This NMR-spectroscopy-guided analysis enabled us to design micromolar ligands after the optimisation and connection of millimolar fragments with an appropriate linker. The influence of the linker region on the binding affinity and selectivity outlines the importance of having a flexible assemblage strategy with a variety of linkers in such an approach. 2009 Wiley-VCH Verlag GmbH & Co. KGaA.
NMR-guided fragment-based approach for the design of tRNALys3 ligands
Chung, Florence,Tisne, Carine,Lecourt, Thomas,Dardel, Frederic,Micouin, Laurent
, p. 4489 - 4491 (2008/03/27)
Two in one: Two ligands for tRNALys3 that were identified from a compound library by flow-injection NMR spectroscopic screening and found to have millimolar dissociation constants (on the left in the picture) inspired the fragment-based synthesis of a new family of ligands with the general structural features of both initial compounds. Ligand 1 of this family is a selective D-stem binder of tRNALys3 with a micromolar Kd value.
Synthesis and antitumor activity of 7-substituted 20(RS)-camptothecin analogues
Jew, Sang-Sup,Kim, Hee-Jin,Kim, Myoung Goo,Roh, Eun-Young,Cho, Youn-Sang,Kim, Joon-Kyum,Cha, Kyung-Hoe,Lee, Kang-Keun,Han, Hyun-Jung,Choi, Jae-Young,Lee, Heesoon
, p. 845 - 848 (2007/10/03)
Novel water-soluble camptothecin analogues with excellent antitumor activity have been designed and synthesized by total synthesis. The analogues were evaluated for cytotoxic activity against five tumor cell lines. The most potent analogue 6c exhibited significant antitumor activity at wider range of doses as compared with camptothecin (T/C 243% at 70 mg/kg; T/C 150% at 8.75-140 mg/kg).
