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Several new 4(3H)-1,2,3-benzotriazinone derivatives were synthesized and tested for their anti-inflammatory activity and ulcerogenic effect. A docking study on the COX-2 binding pocket has been carried out for the target compounds to rationalize the possible selectivity. Among the tested compounds, the benzotriazinones linked to either thiadiazole (8) or oxadiazole (9) evoked the highest anti-inflammatory activity as well as the best binding profiles into the COX-2 binding site.

A photo-controlled version of the engrailed homeodomain (zENG) was created by inserting the homeodomain into a surface loop of a circularly permuted version of the photoactive yellow protein (cPYP). The two proteins fold independently as judged by NMR and fluorescence denaturation measurements. In the dark, the affinity of the zENG domain for its cognate DNA is inhibited >100-fold compared to wild-type zENG. Blue-light irradiation of the hybrid protein leads to enhanced conformational dynamics of the cPYP portion and a two-fold enhancement of the DNA binding affinity of the zENG domain. These results suggest that insertion into a surface loop of cPYP can be a general approach for conferring an initial level of photo-control on a given target protein. Focussed mutation/selection strategies may then be used to enhance the degree of photo-control.

DNA binding by bZIP-type coiled-coil proteins can be inhibited by dominant negative versions of the proteins in which the Nterminalbasic region is replaced by an acidic extension. Photocontrolof bZIP function can be achieved by introducing intramolecularazobenzene-based crosslinkers into dominant negatives. We show that the largest degree of photocontrol is achieved when the crosslinker is introduced into the zipper region of the dominant negative between Cys residues placed at f sites in the heptad segment showing the highest intrinsic helical propensity. The overall affinity of the dominant negative can then be tuned by varying the length of the acidic extension

Species belonging to the family Cyperaceae are an important source of active constituents with biological activity. Cyperaceae is a family of monocotyledonous known as sedges, which superficially resemble grasses or flowering plants rushes. The family comprises about 4000 species described in about 90 genera. These species are widely distributed in tropical Asia and tropical South America. While, sedges may be found growing in all types of soils, many are associated with wet lands or poor soils. The genus Cyperus includes about 600 species, some of which are used in folk medicine, the most important one is Cyperus rotundus L. In this review we focused on the phenolics and nitrogenous constituents isolated from different Cyperus species growing in Egypt.

Didemnaketals are rare terpenoid class reported only in the marine ascidian Didemnum species. They possess important biological activities like HIV-1 protease inhibitor, protein kinase inhibition, antimicrobial, antiproliferative, and cytotoxic. A compilation of new naturally occurring didemnaketals reported during 1991–2014 is provided with available physical and spectral data: mp,[a]D, UV, IR, 1H and 13C NMR as well as biological activities and references.

As a part of our continuing interest in identifying anticancer drug leads from natural sources, we have investigated the n-BuOH fraction of the root bark of Calotropis procera (Ait) R. Br. Seven new oxypregnane oligoglycosides: calotroposides H–N (1–7) were isolated and identified. Their structures were established on the basis of 1D and 2D NMR studies, HRMS, and GCMS spectral data. The in vitro growth inhibitory activity of the n-BuOH fraction and compounds 1–7 was evaluated against A549 non-small cell lung cancer (NSCLC), U373 glioblastoma (GBM), and PC-3 prostate cancer cell lines. Compounds 4 and 6 showed subnanomolar growth inhibition activity with IC50 ranging from 0.5 to 0.7 lM against U373 glioblastoma (GBM) and PC-3 prostate cancer cell lines. These results provide further insight into the chemical diversity and biological activities of this class of compounds.

Chemical examination of the fungus Aspergillus aegyptiacus isolated from cotton textile yielded two new pyrrolidine alkaloids: aegyptolidine A (3) and aegyptolidine B (4), together with two known ophiobolin sesterterpenoids: ()-5-deoxovariecolin (1) and variculanol (2). Compound 1 is reported for the first time from a natural source. The structures of the isolated compounds were unambiguously elucidated on the basis of extensive spectroscopic data analysis (1D (1H and 13C) and 2D (1H–1H COSY, HMQC, HMBC, and NOESY)NMR, MS, IR, and UV) and comparison with literature data. Compounds 1 and 2 showed moderate cytotoxic activity against murine lymphoma cancer cell line L5178Y with ED50 7.6 and 8.1 mg/mL, respectively.

2-(2-Phenylethyl) chromone (PEC), an uncommon class of chromones, possesses a phenylethyl substituent at the C2 position. They have been isolated from a few plant species. They have promising biological activities such as neuro-protective, cytotoxic, cetylcholinesterase inhibitory, antibacterial and anti-inflammatory. This review focuses on the naturally occurring PEC derivatives, their sources, physical and spectral data, as well as biological activities.