Potential Antitumor Agents. 37. Synthesis and Antitumor Activity of Guanylhydrazones from Imidazo[2,1-b]thiazoles and from the New Heterocyclic System Thiazolo[2‘,3‘:2,3]imidazo[4,5-c]quinoline

Abstract

This paper reports synthesis and antitumor activity of new guanylhydrazones from imidazo[2,1-b]thiazoles and from the new heterocyclic system thiazolo[2',3':2,3]imidazo[4,5-c]quinoline. The compounds were tested as potential antitumor agents at the National Cancer Institute. The effect of the guanylhydrazone of 2-chloro-6-(2,5-dimethoxy-4-nitrophenyl)imidazo[2,1-b]thiazole-5-carbaldehyde (41) was investigated, and it was found to be an inhibitor of Complex III of the mitochondrial respiratory chain and is able to induce apoptosis in the cell lines HT29 and HL60.

Synthesis, Anthelmintic and Anti-inflammatory Activities of Some Novel Imidazothiazole Sulfides and Sulfones

“…Imidazothiazole derivatives have been shown to display potent antitumor and fungistatic activities. [2][3][4][5] In continuation of our work on nitrogen containing bridgehead heterocycles, 6-8 herein we report synthesis of sulfides and sulfones of thiazoloimidazoles expecting them to exhibit better anthelmintic and anti-inflammatory properties.…”

Imidazo[2,1b ] Thiazole: Introduction, Current and Perspective

“…Derivatives of this scaffold are especially attractive in the field of medicinal chemistry because of their broad spectrum of biological activities. The imidazo [2,1-b]thiazole system constitutes the core unit of the well-known anthelminthic and immunomodulatory agent Levamisole (2) (Figure 1 During last decades our group synthetized some series of imidazo [2,1-b]thiazole derivatives active against various cancer cell lines (3)(4)(5)(6)(7)(8). We discovered that, for some selected molecules, their ability to inhibit cellular proliferation was mediated by cell cycle arrest at the G2/M phase, accompanied by inhibition of ornithine some derivatives exhibit growth inhibition in submicromolar range.…”

Synthesis of New 6-(4-Fluorophenyl)-5-(2-substituted pyrimidin-4-yl)imidazo[2,1-b] thiazole Derivatives and their Antiproliferative Activity against Melanoma Cell Line

“…In addition, imidazo [2,1-b]thiazole derivatives demonstrated good antiproliferative activity against a variety of human cancer cell lines. [10][11][12][13][14] Recently, some pyrimidinyl substituted imidazo [2,1-b]thiazole derivatives have been reported as RAF kinases inhibitors. 15 It is well known that inhibitors of RAF kinases, such as Sorafenib, have demonstrated antiproliferative activity against different cancer types, such as melanoma.…”