Ag-Catalyzed Domino Decarboxylative Alkylation/Dearomative Annulation: Entry to Fused-Pyrido[4,3-]Indolones.

Here we report the development of unprecedented silver-catalyzed intramolecular annulations of -acrolyl-2-(3-indolyl) benzimidazoles with alkyl carboxylic acids to construct complex fused-pentacyclic alkaloid scaffolds. Divergent reactivities are noticed with altered groups at C2-indole of the substrate. The reaction proceeds through decarboxylative alkylation, followed by dearomative annulation in a domino manner with excellent diastereoselectivity.

Flow and On-Water Synthesis and Cancer Cell Cytotoxicity of Caffeic Acid Phenethyl Amide (CAPA) Derivatives.

Caffeic acid phenethyl ester (CAPE) is a phenolic natural product with a wide range of biological activities, including anticancer activity; however, the ester group of CAPE is metabolically labile. The corresponding amide, CAPA, has improved metabolic stability but limited anticancer activity relative to CAPE. We report the synthesis using flow and on-water Wittig reaction approaches of five previously reported and five novel CAPA analogues.

One-Pot Synthesis of -Fused Benzimidazo-β-carbolines through Sequential Propargylation/-Cycloisomerization Approach.

The first sequential acid-catalyzed propargylation/base-mediated -cycloisomerization between indolyl-benzimidazoles and propargylic alcohols is described. This protocol enables the one-pot construction of -fused benzimidazo-β-carbolines in good yields. The synthetic utility of this approach is demonstrated by the assembly of an -helicene and also by a gram-scale reaction.

Dearomative -Cyclization to Spiropseudoindoxyls: An Extendable Approach To Access Indolo[3,2-]quinolinones and Isocryptolepine.

A metal-free oxidative intramolecular dearomative spirocyclization of indole-3-formyl-2-carboxamides has been developed for the first time, affording spiropseudoindoxyls in good yields. This domino process proceeds through sequential oxidation, decarboxylation and -arylation. The unique feature of this approach includes the compatibility of -protected-indole-2-carboxamides.

Unveiling the anticancer mechanism of 1,2,3-triazole-incorporated thiazole-pyrimidine-isoxazoles: insights from docking and molecular dynamics simulations.

Cancer is a major global health concern, and the constant search for novel, selective anticancer compounds with low toxicity is never ending. Nitrogen heterocyclic compounds such as pyrimidine and triazole have been identified as potential candidates for cancer treatment. A novel series of 1,2,3-triazole incorporated thiazole-pyrimidine-isoxazole derivatives ) were designed, synthesized and evaluated for antitumorigenic activities against human breast cancer (MCF-7), human lung cancer (A549) and human prostate (PC3 & DU-145) various cell-lines by employing MTT assay using etoposide as the positive control.