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Design and synthesis of novel polycycles based on the 3 H ‐pyrrolo/6,7‐dihydropyrido[1,2‐ a ]indole scaffold as templates for pharmaceutical development
Author(s) -
Derudas Marco,
Pala Nicolino,
Sanna Vanna,
Dallocchio Roberto,
Dessì Alessandro,
Roggio Anna Maria,
Sechi Mario
Publication year - 2011
Publication title -
journal of heterocyclic chemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.321
H-Index - 59
eISSN - 1943-5193
pISSN - 0022-152X
DOI - 10.1002/jhet.710
Subject(s) - chemistry , template , indole test , scaffold , combinatorial chemistry , ring (chemistry) , topoisomerase , dna , polymerase , stereochemistry , drug design , computational biology , biochemistry , nanotechnology , organic chemistry , medicine , materials science , biomedical engineering , biology
In the course of our work aimed at developing novel heterocycles of pharmaceutical interest, we designed and synthesized several polycyclic templates as potential substrates to be used in drug design. We obtained a set of condensed ring systems as versatile structural platforms to generate potential DNA‐interactive agents and/or reversible inhibitors of enzymes such as topoisomerases, poly(ADP‐ribose) polymerase‐1 (PARP‐1), telomerase, and, in particular, cyclin dependent kinases. Herein, we report the design, synthesis, structural investigation, and preliminary DNA‐binding affinity of these heteroaromatic systems. J. Heterocyclic Chem., (2011).