Synthesis, DNA-binding abilities and anticancer activities of triazole-pyrrolo[2,1-c][1,4]benzodiazepines hybrid scaffolds

Comparative (Q)SAR analysis of benzodiazepine derivatives with different biological activity

“…Other pharmacological applications of benzodiazepines were also studied and many proven biological effects of BZD can be named. In addition to their established anxiolytic activities, BZD also demonstrate activities as antiarrhythmic agents [2e6]; antagonists of cholecystokinin receptors [7e10]; non-nucleoside inhibitors of HIV-1 reverse transcriptase [11e16]; partial agonists of a 1 -adrenergic receptor [17], and a 2 -adrenoceptor antagonists [18]; compounds with k-opioid [19e22] and muscarinic [23] receptors activity; compounds affecting the hunger center [24,25]; inhibitors of cholesterol absorption [26]; antibacterial and antifungal [27], antimalarial [28], anticancer [29,30], anti-inflammatory [31] agents. These compounds are active within the central nervous system (CNS) or outside of it.…”

CD147 overexpression promotes tumorigenicity in Chinese hamster ovary cells

“…The two molecules belong to Bcl‐2 family, working as important anti‐apoptotic proteins. It is reported that the downregulation of Bcl‐2 and Bcl‐xL expression mediates an early‐stage apoptosis in tumor cells (Ma et al, ; Zorofchian Moghadamtousi et al, ; Chen et al, ). Overexpression of Bcl‐2 and Bcl‐xl can suppress early‐stage apoptosis in tumor cells (Criollo et al, ; Gajate et al, ) and normal cells (Zhao et al, ).…”

Solid-Phase Synthesis of Seven-Membered Heterocycles with Two Nitrogen Atoms

“…Synthetic benzo [1,4]diazepines have been identified as important molecules in drug discovery, especially as potent central nervous system (CNS) agents with strong antianxiety, muscle relaxant, and tranquilizing effects due to their specific binding sites within GABA A receptors [3]. Although the CNS effect of benzodiazepines is considered most important, there are many other beneficial properties, such as an antiarrhythmic effect [4], antagonism of cholecystokinin receptors [5], inhibition of HIV-1 reverse transcriptase [6], opioid receptor activity [7], anticancer [8] or anti-inflammatory [9] effects, and many others. For these reasons, benzodiazepines are conventionally classified as "privileged scaffolds".…”