Letters in Drug Design & Discovery - Volume 13, Issue 6, 2016

An efficient method was developed for the synthesis of pamidronic acid involving the reaction of β-alanine with three equivalents of phosphorus trichloride and two equivalents of phosphorous acid at 75 °C in the presence of 0.3 or 0.6 equivalents of [BMIM][PF6] as an additive.

A new series of indolizine derivatives were synthesized and screened for the antiproliferative potential against NCI 60 tumor cell line panel. The results of the study revealed a selective and good antitumor growth inhibitory activity against SNB-75 CNS cancer cell line for 1-cyanoindolizine derivative 10b. Moreover, a supplementary in vitro biological evaluation showed that compound 9d exhibited a significant farnesyltransf Read More

A series of macamides (1-4) and their synthetic analogs (5-14) were synthesized and evaluated for in vitro inhibitory activities against breast cancer cell MCF-7. The results of bioactive assay showed that two of the macamides (compound 1 and 4) and one synthetic analog (compound 5) displayed comparable inhibitory activities against MCF-7 cell line, with IC50 values of 29.6, 36.2 and 27.2 μM, respectively.

Resveratrol (3,4,5'-trihydroxy-trans-stilibene) is a famous natural product which exhibits potential antitumor activity both in vitro and in vivo. In this article, A series of formamide derivatives of resveratrol (C1-27) were synthesized and their cytotoxic activities were evaluated, with results indicating that most of the compounds exhibited antitumor activity against both Smmc7721 and SGC7901 cancer cell lines. Among them Read More

A base catalyzed sequential one-pot protocol for an effective preparation of 3-(substitutedphenyl) -6,6-dimethyl-2-(substitutedphenylcarbonyl)-3,5,6,7-tetrahydro-1-benzofuran- 4(2H)-one derivatives have been described. One-pot reaction of aromatic aldehydes, various phenacyl bromide and dimedone gives corresponding substituted benzofurans in economically affordable yields with stereo spec Read More

Background: The prediction of physicochemical properties is important task of the natural sciences. Quantitative structure – property relationships (QSPR) are a tool to solve the task. Objective: QSPR for dispersibility of graphene in various organic solvents has been built up by means of the CORAL software (http://www.insilico.eu/coral). Method: The Monte Carlo technique is the basis of the models for dispersibility of graphen Read More

A novel series of novel 1,2,4-triazolo[4,3-a]pyridines were designed and synthesized under microwave irradiation condition. The structures were identified by 1H NMR, MS and elemental analysis, and the antifungal activities of them were evaluated at 100 ppm. It was found that some of the 1,2,4-triazolo[4,3-a]pyridines displayed good antifungal activity. Among them, compound 2e exhibited good antifungal activity against St Read More

Tropomysin receptor kinase A (TrkA) is an excellent drug target for its important roles in pain sensation as well as tumour cell growth. Up to now, the discovered TrkA inhibitors belong mostly to type-I class targeting the ATP binding site, while we aim to find type-II inhibitors because they are deemed to have improved kinase selectivity and slower off-rates than their counterparts. The type-II inhibitors can induce TrkA in an ina Read More

With ever-increasing drug resistant clinical isolates, novel antibiotics with new targets are urgently needed. Tuberculosis, caused by Mycobacterium tuberculosis, showed formidable antibiotics resistance. InhA, the enoyl-acyl carrier protein (ACP) reductase involved in the type II fatty acid synthesis pathway (FASII) in Mycobacterium tuberculosis, represents an appealing target for the development of new anti-tuberculosis ( Read More

The new series of 2-(substituted-phenyl)acetohydrazides analogs, S-alkylated 5-substituted-1,3,4-oxadiazoles- 2-thione derivatives and 5-arylidene-3-substituted-1,2,4-triazines have been synthesized in good yields and characterized by IR, NMR, mass spectral and elemental analyses. All the synthesized compounds 4(a-d), 5(a-d), 7(a-b), and 8(a-f) are evaluated for their in vitro DPPH scavenging, antimicrobial activity, in vivo a Read More

The synthesis of 2-arylidene 6-(2-aryl-2-oxoethoxy)benzofuran-3-one derivatives was reported and selected compounds were determined for their anticancer activity evaluation in National Cancer Institute NCI, USA according to the drug screening protocol of the institute against approximately 60 tumor cell lines derived from nine cancer diseases. Compound 3r, namely 2-(4- chlorobenzylidene)-6-[2-(4-methoxyphenyl)-2-oxoeth Read More

6-mercaptopurine (6-MP) is the first active metabolite inhibitor shown to suppress cancer cells. The aim of this study is to investigate the bioactivity of 6-MP derivatives and discover new anti-cancer agents. Four 6-mercaptopurine (6-MP) derivatives were synthesized and their anti-cancer activities were analyzed. All of the compounds showed anti-proliferative effects against HepG2 and A2780 cancer cells. Among the synth Read More