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1.
A compact three-step synthesis of a new fused bisindole system isomeric with the heterocyclic skeleton present in the marine natural product iheyamine A has been achieved. The structure of the synthetic product was confirmed by a single-crystal X-ray structure.  相似文献   
2.
To further expand the structure–cytotoxic activity relationships of isatin derivatives and to reduce flexibility in substituent groups at nitrogen, 20 analogues incorporating a ring system between the N1 and C7 atoms of isatin were prepared using a variety of synthetic strategies. This yielded pyrroloindole-, pyrroloquinoline-, pyrroloacridine-, pyrrolophenanthridine- and benzopyrrolophenanthridine-based systems with embedded isatin moieties, the latter possessing a novel carbon skeleton. These compounds were subsequently assessed for their in vitro cytotoxicity against human U937 lymphoma cells, with the brominated pyrroloacridine dione 27 showing the most promising activity (IC50 3.01 μM) after 24 h.  相似文献   
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We consider arrays of size 2?×?2?×?2 and 2?×?2?×?2?×?2 over the fields with two and three elements. We use computer algebra to determine the canonical forms of these arrays with respect to the action of the semidirect product of general linear groups with the symmetric group. For each canonical form, we determine the size of its orbit and the rank of the arrays in its orbit.  相似文献   
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We use computer algebra to determine all the multilinear polynomial identities of degree ≤7 satisfied by the trilinear operations (a·bc and a·(b·c) in the free dendriform dialgebra, where a·b is the pre-Lie or the pre-Jordan product. For the pre-Lie triple products, we obtain one identity in degree 3, and three independent identities in degree 5, and we show that every identity in degree 7 follows from the identities of lower degree. For the pre-Jordan triple products, there are no identities in degree 3, five independent identities in degree 5, and ten independent irreducible identities in degree 7. Our methods involve linear algebra on large matrices over finite fields, and the representation theory of the symmetric group.  相似文献   
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We introduce degree n Sabinin algebras, which are defined by the polynomial identities up to degree n in a Sabinin algebra. Degree 4 Sabinin algebras can be characterized by the polynomial identities satisfied by the commutator, associator, and two quaternators in the free nonassociative algebra. We consider these operations in a free power associative algebra and show that one of the quaternators is redundant. The resulting algebras provide the natural structure on the tangent space at the identity element of an analytic loop for which all local loops satisfy monoassociativity, a 2 a ≡ aa 2. These algebras are the next step beyond Lie, Malcev, and Bol algebras. We also present an identity of degree 5 which is satisfied by these three operations but which is not implied by the identities of lower degree.  相似文献   
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As of mid-2017, only one structure of the human immunodeficiency virus (HIV) integrase core domain co-crystallised with an active site inhibitor was reported. In this structure (1QS4), integrase is complexed with a diketo-acid based strand-transfer inhibitor (INSTI). This structure has been a preferred platform for the structure-based design of INSTIs despite concerns relating to structural irregularities arising from crystallographic packing effects. A survey of the current pool of 297 reported integrase catalytic core structures indicated that the anatomy of the active site in the complex structure 1QS4 exhibits subtle variations relative to all other structures examined. Consequently, the 1QS4 structure was employed for docking studies. From the docking of twenty-seven allyltyrosine analogues, a 3-point inhibitor binding motif required for activity was established and successfully utilised in the development of a tripeptide displaying an EC50 value of 10 ± 5 μM in HIV infected human T-cells. Additional docking of “in-house” compound libraries unearthed a methyl ester based nitrile derivative displaying an IC50 value of 0.5 μM in a combined 3′-processing and strand-transfer assay.  相似文献   
10.
Addition of Michael acceptors to the C-4 position in ceph-3-ems followed by oxidation, de-esterification, and de-carboxylation results in the formation of new 4-monosubstituted ceph-3-ems; an unusually mild de-oxygenation process for ceph-2-em sulphoxides is also described.  相似文献   
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