Kachigere B. Harsha
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Chandagirikoppal V. Kavitha
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Toreshettahally R. Swaroop
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Shobith Rangappa
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Kanchugarakoppal S. Rangappa
1,5-Benzodiazepine derivatives are readily assembled from o-phenylene diamine and ketones containg
α-hydrogen atoms by means of simple cyclocondensation via sp3 C-H activation promoted by an
efficient heterogeneous silica sulfuric acid catalyst. Eco-friendliness, good yields, easy workup, reusable
catalyst, short reaction times, high atom economy and solvent-free conditions are the noteworthy
features of this protocol. These benzodiazepines are chosen for the evaluation of antiproliferative
activity against different leukemia cell lines. Among the investigated compounds, 3g is the best
antiproliferative agent against all the cell lines tested. Also, current preliminary analysis showed that
compound 3g phosphorylates ERK1/2 and induces G1 arrest in K562 cells