Synthesis and cytotoxicity studies of novel benzhydrylpiperazine carboxamide and thioamide derivatives

Abstract

Synthesis and cytotoxic activities of 32 benzhydrylpiperazine derivatives with carboxamide and thioamide moieties were reported. In vitro cytotoxic activities of compounds were screened against hepatocellular (HUH-7), breast (MCF-7) and colorectal (HCT-116) cancer cell lines by sulphorhodamine B assay. In general, 4-chlorobenzhydrylpiperazine derivatives were more cytotoxic than other compounds. In addition, thioamide derivatives (6a-g) have higher growth inhibition than their carboxamide analogs.

Ruthenium (II) complexes containing 2-mercaptothiazolinates as ligands and evaluation of their antimicrobial activity

“…Thioamides are extensively studied due to their clinical applications, for example, as antituberculosis [17,18], antibacterial [19], anti-influenza [20] and antitumor [21] agents. Among the thioamides, the N-heterocyclic thiones can be highlighted as ligands in coordination chemistry due to their potential as metallodrugs [22,23].…”

Syntheses and structural and serum protein protecting activity of ruthenium(ii)–DMSO complexes containing a mercapto ligand

“…8i,13 Thioamides have been extensively studied due to their therapeutic applicability as antituberculosis, 14,15 antibacterial, 16 anti-influenza 17 and anticancer drugs. 18 Because of their potential use as metallodrugs, N-heterocyclic thiones can be highlighted as a ligand in the coordination chemistry of thioamides. 19,20 As a result, lots of transition metal complexes based on pyridine-2thiones, 21 pyrimidine-2-thiones, [22][23][24] and thiouracils [25][26][27][28][29][30] and their biological activity have been explored.…”

Cytotoxic activities of some benzothiazole-piperazine derivatives

“…Agents caused induction of senescence-associated cell death through the inhibition of some kinase proteins 8 . In addition, Yarim and her co-workers previously reported various piperazine derivatives with high cytotoxic activity against liver (HUH-7, FOCUS, MAHLAVU, HepG-2, Hep-3B), breast (MCF-7, BT20 and T47D), colon (HCT-116), gastric (KATO-3), cervix (HeLa) and endometrial (MFE-296) cancer cell lines [9][10][11] . According to anticancer activity studies of benzothiazolepiperazine backbone, arylsulphonamides and arylthiol derivatives have potent cytotoxicity against a large scale of cancer cell lines such as breast (MCF-7), hepatocellular (HepG-2), prostate (DU-145) cancers and CD4 + human acute T-lymphoblastic leukaemia (CCRF-CEM) 12,13 .…”