Antitumor activity against human promyelocytic leukemia and studies of some benzoxazines.

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 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 ( and ) were investigated. The results of studies obtained were compared a standard drug, etoposide. results showed that and were found to be extremely effective compared to etoposide (IC value: 10 µM) with IC values of and , 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, ADME/Tox studies were performed to predict drug-likeness and pharmacokinetic properties of and .Communicated by Ramaswamy H. Sarma.