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Synthesis of the first example of a C2-C3/C2 ‘-C3 ‘-endo unsaturated pyrrolo[2,1-c][1,4]benzodiazepine dimer

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Date
2001-11-05
ICR Author
Kelland, Lloyd
Author
Gregson, SJ
Howard, PW
Corcoran, KE
Jenkins, TC
Kelland, LR
Thurston, DE
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Type
Journal Article
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Abstract
We report the first example of a C2-C3/C2’-C3’-endo unsaturated pyrrolo[2,1-c][1,4]benzodiazepine (PBD) dimer 16 synthesised through a new and efficient route, thus establishing that C2-C3-endo unsaturation enhances both cytotoxicity and DNA-binding affinity in A-Ring-linked PBD dimers but to a lesser extent than C2/C2’-exo-unsaturation. This new route has allowed the preparation of multi-gram quantities of the related clinical candidate 1 and should lead to more structurally diverse PBD dimer analogues. (C) 2001 Elsevier Science Ltd. All rights reserved.
URI
https://repository.icr.ac.uk/handle/internal/2850
DOI
https://doi.org/10.1016/S0960-894X(01)00560-1
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  • Other ICR Research
Language
eng
License start date
2001-11-05
Citation
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2001, 11 pp. 2859 - 2862

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