Open AccessA Green Synthesis of 1,5-Benzodiazepines using Reusable-Heterogeneous Silica Sulfuric Acid Catalyst under Solvent-Free Conditions and their Antileukemic Activity
Author(s) -
Kachigere B. Harsha,
C. Kavitha,
Toreshettahally R. Swaroop,
Shobith Rangappa,
Kanchugarakoppal S. Rangappa
Publication year - 2021
Publication title -
asian journal of chemistry/asian journal of chemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.145
H-Index - 34
eISSN - 0975-427X
pISSN - 0970-7077
DOI - 10.14233/ajchem.2021.23103
Subject(s) - chemistry , sulfuric acid , catalysis , solvent , atom economy , solid acid , combinatorial chemistry , diamine , k562 cells , organic chemistry , cell , biochemistry
1,5-Benzodiazepine derivatives are readily assembled from o-phenylene diamine and ketones containgα-hydrogen atoms by means of simple cyclocondensation via sp3 C-H activation promoted by anefficient heterogeneous silica sulfuric acid catalyst. Eco-friendliness, good yields, easy workup, reusablecatalyst, short reaction times, high atom economy and solvent-free conditions are the noteworthyfeatures of this protocol. These benzodiazepines are chosen for the evaluation of antiproliferativeactivity against different leukemia cell lines. Among the investigated compounds, 3g is the bestantiproliferative agent against all the cell lines tested. Also, current preliminary analysis showed thatcompound 3g phosphorylates ERK1/2 and induces G1 arrest in K562 cells