Structure-based drug design and potent anti-cancer activity of tricyclic 5: 7: 5-fused diimidazo [4, 5-d: 4′, 5′-f][1, 3] diazepines

…, S Kondaskar, JC Fishbein, BA Carter-Cooper…

Index: Kondaskar, Atul; Kondaskar, Shilpi; Fishbein, James C.; Carter-Cooper, Brandon A.; Lapidus, Rena G.; Sadowska, Mariola; Edelman, Martin J.; Hosmane, Ramachandra S. Bioorganic and Medicinal Chemistry, 2013 , vol. 21, # 3 p. 618 - 631

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Citation Number: 11

Abstract

Judicial structural modifications of 5: 7-fused ring-expanded nucleosides (RENs), based on molecular modeling studies with one of its known targets, human RNA helicase (hDDX3), led to the lead, novel, 5: 7-5-fused tricyclic heterocycle (1). The latter exhibited promising broad-spectrum in vitro anti-cancer activity against a number of cancer cell lines screened. This paper describes our systematic, albeit limited, structure–activity relationship (SAR) ...