Letters in Drug Design & Discovery - Volume 12, Issue 3, 2015

Saponins enhance the cytotoxicity of the type I ribosome-inactivating protein (RIP-I) saporin. In the present study, the synergistic cytotoxicity of nine newly isolated gypsogenin-containing saponins from Gypsophila trichotoma in combination with RIP-I was evaluated in vitro and used to derive a quantitative structure – activity relationship (QSAR). The QSAR model distinguished two important structural features of the studied sa Read More

Novel disulfide analogues of isophosphoramide mustard (iPAM) were designed and synthesised. All compounds were hydrolytically stable and underwent reduction by L-glutathione with different kinetic parameters. Based on the HPLC-MS analysis a mechanism of activation by glutathione obtained disulfide analogues of iPAM was proposed. The compounds were tested for cytotoxic activity against human promyelocytic leuk Read More

Several oncogenic pathways may lead to cancer. Pharmaceutical research develops efficacious compounds to inhibit these pathways. Current inhibitor drugs may block several pathways simultaneously but cause adverse and side effects. Therefore, we designed novel acyl thiourea derivatives containing pyrazole ring to selectively inhibit a kinase dependent pathway in cancer. In this study, breast and bone cancer ce Read More

By coupling nitric oxide (NO)-donating moieties with ATPT, an orally active AT1 receptor antagonist, a series of novel NO-releasing derivatives with N-phenylpyrrolyl-2-tetrazole moiety were designed and synthesized. The NOreleasing assay indicated that compound 4c had good maximum amount of NO release. Moreover the target compounds were evaluated for their antagonism of AT1 receptor with induced contraction i Read More

The inhibition of glycosidases from bacteria and the liver of normal and diabetic rats by 2-(tetra-O-acetyl-β-Dglucopyranosylsulfanyl)- 5-(1-benzyl-1H-indol-2-yl)-1,3,4-oxadiazole BnM-3B; 3-(2,3,4,6-tetra-O-acetyl-β-D-galactopyranosyl)- 5-(1H-indol-2-yl)-1,3,4-oxadiazole- 2(3H)-thione MTB-4A; 3-(2-acetamido-3,4,6-tri-O-acetyl-2-deoxy-β-Dglucopyranosyl)- 5-(1-benzyl-1H-indol-2-yl)-1,3,4-oxadiazole-2(3H)-thione BnN-5A has been i Read More

The overexpression of anaplastic lymphoma kinase (ALK) had been found in many types of cancers, especially the non-small-cell lung cancers (NSCLCs). So the discovery of novel ALK inhibitor had attracted a great deal of interest in anticancer drugs research area. Presently, a combined study of 3D-quantitative structure-activity relationship (3DQSAR) and molecular docking was undertaken to explore the structural insight Read More

A novel series of FtsZ-targeted phenylacrylamides were designed, synthesized and evaluated for their antibacterial activity and cell division inhibitory activity against various Gram-positive and -negative strains. Among them, some compounds displayed preferable or comparable antibacterial activity and cell division inhibitory activity in comparison with their parent cinnamic acid. In particular, the compounds beari Read More

4-isopropylcyclohexa-1, 3-dienecarboxylic acid (dehydrocumic acid) was prepared from β-pinene, and a series of acylthiourea derivatives was obtained. The structures of title compounds were characterized by FT-IR, NMR, and MS. The insecticidal activities against ostrinia furnacclis and bemisia tabaci were evaluated. The title compounds exhibited moderate larvicidal activity against ostrinia furnacclis. The preliminary stu Read More