One-Pot Multicomponent Synthesis and Cytotoxic Evaluation of Novel 7-Substituted-5-(1H-Indol-3-yl)Tetrazolo[1,5-a] Pyrimidine-6-Carbonitrile

Abstract

A series of novel 7-substituted-5-(1H-indol-3-yl)tetrazolo[1,5-a]pyrimidine-6-carbonitrile was synthesized via a one-pot, three-multicomponent reaction of appropriate aldehydes, 1H-tetrazole-5-amine and 3-cyanoacetyl indole in catalytic triethylamine. The cytotoxic activity of the new synthesized tetrazolopyrimidine-6-carbonitrile compounds was investigated against HCT-116, MCF-7, MDA-MB-231, A549 human cancer cell lines and one human healthy normal cell line (RPE-1) using the MTT cytotoxicity assay. Compounds 4h, 4b, 4c, 4i and 4a showed potent anticancer activities against human colon cancer. Additionally, all the compounds showed potent anticancer activities on human lung cancer.

Synthesis of new pyridines with sulfonamide moietyviaa cooperative vinylogous anomeric-based oxidation mechanism in the presence of a novel quinoline-based dendrimer-like ionic liquid

“…[30][31][32][33][34] Therefore, pyridine and its derivatives (particularly 2-aminonicotinonitrile) have received extensive consideration and several efficacious methods have been developed by synthetic and medicinal chemists for their preparation. [35][36][37][38][39][40][41][42][43][44][45][46][47][48][49][50][51] So, it is predicted that multicomponent synthesis [52][53][54][55][56] of a single molecule bearing sulfonamide and pyridine centers simultaneously gives unique features to that structure inherited characteristics of both cores.…”

One‐potandtwo‐potmethods for chalcone derived pyrimidines synthesis and applications

“…[13] moiety due to their potential and applications in electrochromic, solvatochromic, optical, photochromic, [14] anti-corrosive, [15] chemosensor, [16] optoelectronics or organic light-emitting diodes, [17] and photoproduct of DNA. [18] In therapeutic industry, pyrimidine derivatives have also been reported to have a broad spectrum of biological properties, that is, anticancer, [19][20][21][22][23][24][25][26][27][28][29][30] antihistamine, [31,32] antinociceptive, [33] antilipase, [34] antifilarial, [35] antiparasitic, [36] antioxidant, [37,38] antituberculosis, [39,40] antihypertensive, [41] antimicrobial, [42][43][44][45][46][47] anticonvulsant, [48,49] antiallergic, [50,51] antipyretic, [52] anti-inflammatory. [53,54] antifungal, [55,56] antiviral, [57]…”

Synthesis and Antiproliferative Activity of Chalcone-Imide Derivatives Based on 3,4-Dichloro-1H-Pyrrole-2,5-dione

“…1. Extending our previous efforts that focused on the synthesis and development of biologically active compounds [38][39][40][41][42][43][44][45][46][47][48][49][50],in the current manuscript and in order to achieve constructive results, a combination between chalcones and maleimide wasaccomplished, sequentially a series of 4'aminochalcone-based 3,4-dichloromaleimides was synthesized, and their cytotoxicity against breast cancer cells (MCF-7), and human hepatocellular carcinoma(HepG2) cells was investigated.…”