Correction: Click activated protodrugs against cancer increase the therapeutic potential of chemotherapy through local capture and activation

Correction for ‘Click activated protodrugs against cancer increase the therapeutic potential of chemotherapy through local capture and activation’ by Kui Wu et al., Chem. Sci., 2021, 12, 1259–1271, DOI: 10.1039/D0SC06099B.

The authors regret that the reference to the bond-breaking bioorthogonal chemistry, termed ‘click-to-release’ was omitted from the original article. In addition, we would like to include a reference describing the synthesis of compound 1, which is an intermediate to the protodrugs described in the original article. These references are listed below as ref. 1 and 2.The Royal Society of Chemistry apologizes for these errors and any consequent inconvenience to authors and readers.     

Copper dipyridine dichloride as a mild and efficient catalyst for a one pot condensation bigenelli reaction

The condensation reaction of aldehydes, β‐ketoesters and urea/thiourea in presence of a catalytic amount of CuPy₂Cl₂ complex proceeded under very mild reaction conditions in high yield (80‐90%).     

Regio- and stereoselective transfer of p-toluenesulfonamido group from sulfur to carbon: preparation of aminoalcohol derivatives from allylalcohols

A novel methodology for the regio- and stereoselective synthesis of amino alcohol derivatives from allylalcohols/ethers via intramolecular nucleophilic participation by the sulfilimine moiety is disclosed. The sulfilimine moiety is stereospecifically transformed to a sulfinyl moiety with an inverted configuration. The reaction is general and affords highly functionalised products.     

Synthesis of 4-Dicyclohexylaminomethyl Antipyrine and Its Metal Complexes: Spectral Characterization and Evaluation of Thermodynamic Parameters

Complexes of Fe(III), Co(II), Ni(II), and Cu(II) with 4-dicyclohexylaminomethyl antipyrine (DCHAMA, L) were prepared and characterized by elemental and chemical analyses, IR, electronic absorption, ¹H NMR and EPR spectroscopies, thermal analysis, and magnetic susceptibility measurements. The stoichiometry of the complexes was found to be MLX₂, MLX₃, or MLX₂(H₂O)₂ where X = Cl or NO₃. The ligand exhibits a bidentate mode of coordination. Thermal analysis of the chloro complexes shows a three stage decomposition pattern for the Cu(II) complex and a two stage decomposition pattern for Fe(III) and Co(II) complexes to yield the respective metal oxides as the end product. Kinetic and thermodynamic parameters such as n, E _a, H ^#, S ^#, and G ^# were calculated using Coats–Redfern and Madhusudhanan–Krishnan–Ninan integral methods. The coordination number of the metal atom is found to influence the thermal stability of the complexes. The antimicrobial screening shows that the four-coordinated complexes are more active than the five- and six-coordinated ones and DCHAMA.     

Control over the Self‐Assembly Modes of PtII Complexes by Alkyl Chain Variation: From Slipped to Parallel π‐Stacks

We report the self‐assembly of a new family of hydrophobic, bis(pyridyl) Pt^II complexes featuring an extended oligophenyleneethynylene‐derived π‐surface appended with six long (dodecyloxy ( 2 )) or short (methoxy ( 3 )) side groups. Complex 2 , containing dodecyloxy chains, forms fibrous assemblies with a slipped arrangement of the monomer units (d_Pt???Pt≈14 Å) in both nonpolar solvents and the solid state. Dispersion‐corrected PM6 calculations suggest that this organization is driven by cooperative π–π, C?H???Cl and π–Pt interactions, which is supported by EXAFS and 2D NMR spectroscopic analysis. In contrast, nearly parallel π‐stacks (d_Pt???Pt≈4.4 Å) stabilized by multiple π–π and C?H???Cl contacts are obtained in the crystalline state for 3 lacking long side chains, as shown by X‐ray analysis and PM6 calculations. Our results reveal not only the key role of alkyl chain length in controlling self‐assembly modes but also show the relevance of Pt‐bound chlorine ligands as new supramolecular synthons.     

Development of Petri Net-Based Dynamic Model for Improved Production of Farnesyl Pyrophosphate by Integrating Mevalonate and Methylerythritol Phosphate Pathways in Yeast

In this case study, we designed a farnesyl pyrophosphate (FPP) biosynthetic network using hybrid functional Petri net with extension (HFPNe) which is derived from traditional Petri net theory and allows easy modeling with graphical approach of various types of entities in the networks together. Our main objective is to improve the production of FPP in yeast, which is further converted to amorphadiene (AD), a precursor of artemisinin (antimalarial drug). Natively, mevalonate (MEV) pathway is present in yeast. Methyl erythritol phosphate pathways (MEP) are present only in higher plant plastids and eubacteria, but not present in yeast. IPP and DAMP are common isomeric intermediate in these two pathways, which immediately yields FPP. By integrating these two pathways in yeast, we augmented the FPP synthesis approximately two folds higher (431.16 U/pt) than in MEV pathway alone (259.91 U/pt) by using HFPNe technique. Further enhanced FPP levels converted to AD by amorphadiene synthase gene yielding 436.5 U/pt of AD which approximately two folds higher compared to the AD (258.5 U/pt) synthesized by MEV pathway exclusively. Simulation and validation processes performed using these models are reliable with identified biological information and data.     

A Facile Synthesis of 7,8-DI Aryl Coumarino and Flavano Benzo-Thiophenes

The key step for the synthesis of 7-hydroxy 2,3-diarylsubstituted benzothiophenes 5a-f , by starting from substituted 2-aryl-2-((2-methoxy phenyl)thio)acetophenones 3a-f as an intermediate, consists of a Friedel-Crafts cyclization followed by demethylation by Lewis acids like BF 3 OEt 2 and AlCl 3 in DCM.