Correction: Synthesis of medium-sized (6-7-6) ring compounds by iron-catalyzed C-H activation/annulation.

Correction for 'Synthesis of medium-sized (6-7-6) ring compounds by iron-catalyzed dehydrogenative C-H activation/annulation' by Niranjan Panda et al., Org. Biomol. Chem., 2018, 16, 7861-7870.

Design, synthesis, biological and in silico evaluation of coumarin-hydrazone derivatives as tubulin targeted antiproliferative agents.

Coumarin-based different series of hydrazone derivatives were synthesized and evaluated for anticancer activity against four different human cancer cell lines. The activity of the compounds were compared with doxorubicin as a standard drug and all the compounds exhibited good to moderate cytotoxicity with IC50 values ranging from 6.07 to 60.45 µM against all the examined cancer cell lines. Based on the screening results, it was concluded that the compounds 12a and 18a were the most promising medicinal entities. In vitro tubulin polymerisation inhibition assay was performed for the compounds 12a and 18a and these two compounds displayed good potency when compared with colchicine as the standard drug. The interaction of these compounds with tubulin protein was also studied with the help of molecular docking technique using Discovery studio software. Furthermore, the molecular and ADMET properties of the compounds were computed with Osiris property software and PreADMET server. The compounds exhibited exciting in vitro and in silico results. Hence we propose that the compounds 12a and 18a could be developed as tubulin targeted potential antiproliferative agents.

Synthesis of medium-sized (6-7-6) ring compounds by iron-catalyzed C-H activation/annulation [corrected].

In this report, we have described a FeCl3-catalyzed process involving intramolecular annulation of o-phenoxy diarylacetylenes via hydroarylation to afford a series of biologically potent fused seven-membered (6-7-6) ring compounds under mild reaction conditions. This reaction was believed to proceed through Friedel-Crafts type sequential carbometallation followed by protonation to produce phenyldibenz[b,f]oxepines. This method was also extended to synthesize seven-membered rings that are fused with coumarins.

Synthesis of Isocoumarins via Silver(I)-Mediated Annulation of Enol Esters.

Silver-mediated annulation of 2-iodo enol esters leading to 4- and 3,4-substituted isocoumarins was accomplished selectively at room temperature. Coupling of 2-iodo benzoic acids with enolates that were produced in situ from the simple esters was also performed to produce isocoumarins under analogous reaction conditions. Owing to the mildness of the current protocol, 4-acyl 3-substituted isocoumarins were efficiently produced without any deacylation.

Synthesis of Dibenzofurans via C-H Activation of o-Iodo Diaryl Ethers.

An efficient method for the synthesis of dibenzofuran from o-iododiaryl ether using reusable Pd/C under ligand-free conditions has been developed. Synthesis of o-iododiaryl ether was achieved in one pot through sequential iodination and O-arylation of phenol under mild reaction conditions.

Near-Infrared-Triggered Photodynamic, Photothermal, and on Demand Chemotherapy by Multifunctional Upconversion Nanocomposite.

In an attempt to integrate photodynamic therapy (PDT) with photothermal therapy and chemotherapy for enhanced anticancer activity, we have rationally synthesized a multifunctional upconversion nanoplatform using NaYF4:Yb/Tm/Er/Fe nanoparticles (NPs) as the core and NaYbF4:1% Tm as a shell. The as-synthesized core-shell upconversion (CSU) NPs exhibited diverse and enhanced photoluminescence emissions in a wide range (UV to NIR) consequent upon Fe3+ doping in the core and fabrication of an active shell. Subsequently, CSU was first decorated with titania NPs as photosensitizers. Next, the mesoporous silica (MS) shell loaded with doxorubicin (DOX) via a photocleavable Ru complex as the gating molecule was developed around titania-containing CSU. Finally, gold nanorods (GNRs) with localized surface plasmon resonance (LSPR) at 800 nm were incorporated around the MS layer to obtain the multifunctional nanoplatform. We demonstrated that the UV, blue, and NIR emissions from the CSU produced ROS-mediated PDT through titania activation, induced DOX release through photocleavage of the Ru complex, and generated hyperthermia by LSPR activity of GNRs, respectively, upon a single NIR excitation through FRET. The therapeutic efficacy was validated on HeLa cell lines in vitro by various microscopic and biochemical studies under a significantly milder NIR irradiation and lower dosage of the nanoplatforms, which have been further demonstrated as diagnostic nanoprobes for cell imaging.

One-pot two-step synthesis of 3-iodo-4-aryloxy coumarins and their Pd/C-catalyzed annulation to coumestans.

An efficient protocol for the synthesis of various coumestans from the intramolecular annulation of 3-iodo-4-aryloxy coumarins through C-H activation has been developed. When 3-iodo-4-aryloxy coumarins were treated with 10% Pd/C (0.3 mol% Pd) in the presence of sodium acetate, the corresponding coumestans were produced in good to excellent yield. Reusability of the palladium catalyst was investigated in up to three consecutive cycles and it was found that the yield of the reaction was almost unaltered. Sequential iodination and O-arylation of 4-hydroxy coumarins leading to the 3-iodo-4-aryloxy coumarins were also achieved in a one-pot two-step process starting from aryl iodides in high yield. Pivalic acid was revealed to be the most effective additive for the later method to produce 3-iodo-4-phenoxy coumarins. Different functional groups bearing electron-donating as well as withdrawing groups are also tolerant to the reaction conditions.