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Cancer is one of the deadliest diseases in the world today, and the incidence of cancer is increasing. Leukemia is a type of blood cancer defined as the uncontrolled proliferation of abnormal leukocytes in the blood and bone marrow. The HL-60 (human promyelocytic leukemia) cell line, derived from a single patient with acute promyelocytic leukemia, provides a unique  in vitro  model system for studying the cellular and molecular events involved in the proliferation and differentiation of leukemic cells. In this study, antitumor activities on the HL-60 of some of the resynthesized benzoxazine derivatives ( BXN-01  and  BXN-02 ) were investigated. The results of  in vitro  studies obtained were compared a standard drug, etoposide.  In vitro  results showed that  BXN-01  and  BXN-02  were found to be extremely effective compared to etoposide (IC 50  value: 10 µM) with IC 50  values of  5 nM  and  25 nM , respectively. Furthermore, molecular docking studies were carried out for preliminary prediction of possible interaction modes between compounds and the active site of the target macromolecules, hTopo IIα, HDAC2, and RXRA. Then,  in silico  ADME/Tox studies were performed to predict drug-likeness and pharmacokinetic properties of  BXN-01  and  BXN-02 . Communicated by Ramaswamy H. Sarma

Antitumor activity against human promyelocytic leukemia and in silico studies of some benzoxazines