Variable-Temperature and Ph Studies of a Dna Minor-Groove Binder, Hoechst-32985, by H-1-Nmr Spectroscopy

Cross, KJ, Embrey, KJ, Coles, M, Bicknell, W and Craik, DJ (1994) Variable-Temperature and Ph Studies of a Dna Minor-Groove Binder, Hoechst-32985, by H-1-Nmr Spectroscopy. Magnetic Resonance in Chemistry, 32 9: 509-516. doi:10.1002/mrc.1260320903


Author Cross, KJ
Embrey, KJ
Coles, M
Bicknell, W
Craik, DJ
Title Variable-Temperature and Ph Studies of a Dna Minor-Groove Binder, Hoechst-32985, by H-1-Nmr Spectroscopy
Journal name Magnetic Resonance in Chemistry   Check publisher's open access policy
ISSN 0749-1581
Publication date 1994-09-01
Sub-type Article (original research)
DOI 10.1002/mrc.1260320903
Open Access Status Not Open Access
Volume 32
Issue 9
Start page 509
End page 516
Total pages 8
Language eng
Abstract This study details the synthesis and biological evaluation of a collection of 19 structurally related Minor Groove Binders (MGBs), derived from the natural product distamycin, which were designed to probe antifungal and antimycobacterial activity. From this initial set, we report several MGBs that are worth more detailed investigation and optimisation. MGB-4, MGB-317 and MGB-325 have promising MIC80s of 2, 4 and 0.25 μg/mL, respectively, against the fungus C. neoformans.MGB-353 and MGB-354 have MIC99s of 3.1 μM against the mycobacterium M. tuberculosis. The selectivity and activity of these compounds is related to their physicochemical properties and the cell wall/membrane characteristics of the infective agents.
Keyword Nmr
H-1 Nmr
C-13 Nmr
Hoechst 32985
Dynamics of Piperazine Rings
Pk(a)
Rotating Frame
B-Dna
Binding
Coherence
Mode
Q-Index Code C1
Q-Index Status Provisional Code
Institutional Status Unknown

Document type: Journal Article
Sub-type: Article (original research)
Collection: ResearcherID Downloads - Archived
 
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