Current Issue : April - June Volume : 2019 Issue Number : 2 Articles : 5 Articles
Antibiotic resistance has become a serious global problem that threatens public health.\nIn our previous work, we found that ocotillol-type triterpenoid saponin showed good antibacterial\nactivity. Based on preliminary structure-activity relationship, novel serious C-3 substituted\nocotillol-type derivatives 7â??26 were designed and synthesized. The in vitro antibacterial activity was\ntested on five bacterial strains...............
Introduction: Benzotriazine-1,4-dioxides (BTDOs) such as tirapazamine (TPZ) and\nits derivatives act as radiosensitizers of hypoxic tissues. The benzotriazine-1-monoxide\n(BTMO) metabolite (SR 4317, TPZMO) of TPZ also has radiosensitizing properties, and via\nunknown mechanisms, is a potent enhancer of the radiosensitizing effects of TPZ. Unlike their\n2-nitroimidazole radiosensitizer counterparts, radiolabeled benzotriazine oxides have not been\nused as radiopharmaceuticals for diagnostic imaging or molecular radiotherapy (MRT) of hypoxia.\nThe radioiodination chemistry for preparing model radioiodinated BTDOs and BTMOs is now\nreported. Hypothesis: Radioiodinated 3-(2-iodoethoxyethyl)-amino-1,2,4- benzotriazine-1,4-dioxide\n(I-EOE-TPZ), a novel bioisosteric analogue of TPZ, and 3-(2-iodoethoxyethyl)-amino-1,2,4-\nbenzotriazine-1-oxide (I-EOE-TPZMO), its monoxide analogue, are candidates for in vivo and in vitro\ninvestigations of biochemical mechanisms in pathologies that develop hypoxic microenvironments.\nIn theory, both radiotracers can be prepared from the same precursors. Methods: Radioiodination\nprocedures were based on classical nucleophilic [131I]iodide substitution on Tos-EOE-TPZ (P1) and by\n[131I]iodide exchange on I-EOE-TPZ (P2). Reaction parameters, including temperature, reaction time,\nsolvent and the influence of pivalic acid on productsâ?? formation and the corresponding radiochemical\nyields (RCY) were investigated. Results: The [131I]iodide labeling reactions invariably led to the\nsynthesis of both products, but with careful manipulation of conditions the preferred product could\nbe recovered as the major product. Radioiodide exchange on P2 in ACN............
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Three types of pyrazole-fused heterobicycles, i.e., 1,5-, 1,7-, and 2,5-dihydropyrano[3,2-c]\npyrazoles, were synthesized from 4-allyloxy-1H-pyrazoles. A sequence of the Claisen rearrangement\nof 4-allyloxy-1H-pyrazoles, ruthenium-hydride-catalyzed double bond migration, O-allylation, and\nring-closing metathesis was employed in this study....
New 10-substituted derivatives of 3,6-diazaphenothiazine, containing the triple bond\nlinker terminated with tertiary cyclic and acyclic amine groups, were synthesized and screened\nfor their anticancer action. The compounds exhibited varied anticancer activities against human\nglioblastoma SNB-19, melanoma C-32, and breast cancer MDA-MB231 cell lines, depending on\nthe nature of the substituents. The most active 3,6-diazaphenothiazine, 4, was the derivative\nwith the N,N-diethylamino-2-butynyl substituent against glioblastoma SNB-19, and was ten times\nmore potent than cisplatin. For this compound, the expression of H3, TP53, CDKN1A, BCL-2,\nand BAX genes was detected by the RT-qPCR method. The gene expression ratio BAX/BCL-2\nindicated the induction of mitochondrial apoptosis in cancer cell lines. The transformation of\nthe propynyl substituent into amino-2-butynyl can be a method applicable to the search for more\nanticancer-active azaphenothiazines....
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