InCl3: A Versatile Catalyst for Synthesizing a Broad Spectrum of Heterocycles.

This review deals with the recent applications of the indium trichloride (InCl3) catalyst in the synthesis of a broad spectrum of heterocyclic compounds. Over the years, a number of reviews on the applications of InCl3-catalyzed organic synthesis have appeared in the literature. It is evident that InCl3 has emerged as a valuable catalyst for a wide range of organic transformations due to its stability when exposed to moisture and also in an aqueous medium. The most attractive feature of this review is the application of the InCl3 catalyst for synthesizing bioactive heterocyclic compounds. The study of InCl3-catalyzed organic reactions has high potential and better intriguing aspects, which are anticipated to originate from this field of research.

A bis-indole/carbazole based C5-curcuminoid fluorescent probe with large Stokes shift for selective detection of biothiols and application to live cell imaging.

A series of heterocyclic C5-curcuminoids (bis(arylmethylidene)acetones) (PJ1-PJ6) having a large Stokes shift (Δλ = 104-173 nm) have been synthesized for the selective detection of cysteine (Cys), homocysteine (Hcy) and glutathione (GSH) in living cells. The compounds were synthesized using a new methodology via deacetylation under microwave conditions. The photophysical properties of these compounds have been studied. Prominent colour changes from bright yellow to colourless in the presence of thiols were observed for PJ1. Live cell imaging has been employed with PJ1 for the utilization of the probe to detect homocysteine in A375 cells and apoptosis in AGS cells.

A lysosome-specific near-infrared fluorescent probe for in vitro cancer cell detection and non-invasive in vivo imaging.

Near-infrared (NIR) fluorescent probes have been developed as potential bio-materials having profound applications in diagnosis and clinical practice. Herein, we wish to disclose a highly photostable ultra-bright NIR probe for the specific detection of lysosomes in numerous cell lines. Furthermore, the applicability of the developed NIR probe was evaluated for in vivo imaging.

A Novel Spirooxindole Derivative Inhibits the Growth of Leishmania donovani Parasites both In Vitro and In Vivo by Targeting Type IB Topoisomerase.

Visceral leishmaniasis is a fatal parasitic disease, and there is an emergent need for development of effective drugs against this neglected tropical disease. We report here the development of a novel spirooxindole derivative, N-benzyl-2,2'α-3,3',5',6',7',7α,α'-octahydro-2methoxycarbonyl-spiro[indole-3,3'-pyrrolizidine]-2-one (compound 4c), which inhibits Leishmania donovani topoisomerase IB (LdTopIB) and kills the wild type as well as drug-resistant parasite strains. This compound inhibits catalytic activity of LdTopIB in a competitive manner. Unlike camptothecin (CPT), the compound does not stabilize the DNA-topoisomerase IB cleavage complex; rather, it hinders drug-DNA-enzyme covalent complex formation. Fluorescence studies show that the stoichiometry of this compound binding to LdTopIB is 2:1 (mole/mole), with a dissociation constant of 6.65 µM. Molecular docking with LdTopIB using the stereoisomers of compound 4c produced two probable hits for the binding site, one in the small subunit and the other in the hinge region of the large subunit of LdTopIB. This spirooxindole is highly cytotoxic to promastigotes of L. donovani and also induces apoptosis-like cell death in the parasite. Treatment with compound 4c causes depolarization of mitochondrial membrane potential, formation of reactive oxygen species inside parasites, and ultimately fragmentation of nuclear DNA. Compound 4c also effectively clears amastigote forms of wild-type and drug-resistant parasites from infected mouse peritoneal macrophages but has less of an effect on host macrophages. Moreover, compound 4c showed strong antileishmanial efficacies in the BALB/c mouse model of leishmaniasis. This compound potentially can be used as a lead for developing excellent antileishmanial agents against emerging drug-resistant strains of the parasite.