Pyrrole derivatives as potent inhibitors of lymphocyte-specific kinase: Structure, synthesis, and SAR

A QSAR Study on a Series of Pyrrole Derivatives Acting as Lymphocyte- Specific Kinase (Lck) Inhibitors

“…A series of pyrrole derivatives acting as Lck inhibitors ( Table 1) was reported by Takamaya et al [10]. The inhibition activity of these compounds and the relevant physicochemical parameters that were found to be correlated with the activity are listed in Table 2.…”

“…For the design and development of potent drugs, quantitative-structure-activity relationship (QSAR) studies have been of great help. In this paper we report a QSAR study on a series of pyrrole derivatives (1) studied by Takamaya et al [10] (1)…”

Active methylenes in the synthesis of a pyrrole motif: an imperative structural unit of pharmaceuticals, natural products and optoelectronic materials

“…In 2010, T. Takayama and co-workers reported the synthesis and characterization of a novel series of 2,3,4,5-tetrasubstituted pyrrole derivatives as lymphocyte-specic kinase (Lck) inhibitors through their enzyme inhibitory activity, cellular activity against mixed lymphocyte reaction (MLR14), and structureactivity relationships (SAR) (Scheme 12). 69 In 2013, C. Mukhopadhyay and his group described a onepot, organocatalyzed, multicomponent synthesis of 3H-pyrrole derivatives from ketones, malononitrile and thiols in ecobenign solvent (Scheme 13). 70 This novel 3H-pyrrole synthesis presented an entirely new approach involving the dual role of the cyano moiety acting both as a carbon center nucleophile and an electrophile.…”

Catalytic Reductive Synthesis and Direct Derivatization of Unprotected Aminoindoles, Aminopyrroles, and Iminoindolines

“…[1] In particular,3 -aminoindoles,3 -aminopyrroles, and related heterocycles mark structural motifs of molecules with striking biological activities. [2] Hence,there is aneed for efficient approaches to the corresponding synthetic precursors.M odern catalytic methods,h owever,u sually furnish electronically deactivated and N-protected derivatives that lead to undesired functional-group modifications in the ensuing synthetic applications. [3] This problem also applies to conventional anionic cyclizations to nitriles.…”