Letters in Drug Design & Discovery - Volume 12, Issue 7, 2015

DMU-212, a methoxylated resveratrol analog, has significant anticancer activity, and selectively targets tumor cells. A library of E-diarylstilbenes structurally related to DMU-212 has been synthesized and evaluated for anticancer activity against a large panel of 45 human cancer cell lines. From this study, DMU-212 (3a) exhibited an average growth inhibitory effect (GI50) of 3.5 μM against all the human cancer cell lines in th Read More

A series of 6-bromo-2,3-dioxoindolin phenylacetamide derivatives was synthesized and evaluated for inhibitory activity against CDC25B and PTP1B. Most of the synthesized compounds showed potential inhibitory activities for CDC25B and PTP1B with compound 12 being the most potent (IC50=3.87 μmol/L and 2.98 μmol/L, respectively). Compound 12 also exhibited higher cytotoxic activity against three cancer cell lines ( Read More

During the last century, flavonoids have been identified as multifunctional compounds with properties and biological activities that depend on their diverse functional groups, which may include hydroxyl, methyl, methoxy, glycosyl, isoprenyl, and various polymeric groups. In particular, methoxy groups located on the basic flavonoid structure are intimately interrelated to bioavailability and translocation in cells. The relationships b Read More

From various studies it is now clear that in addition to nucleic acids, enediynes also target other biomolecules, the most prominent of which are the proteins. Since a major portion of currently available drug targets are proteins (enzymes and receptors), this aspect of enediyne chemistry has opened a new window for further exploitation. Newer enediyne-based therapeutics targeting proteins may be possible to design. Moreo Read More

Monopolar spindle 1 (Mps1), a crucial component of spindle assembly checkpoint, essential to maintain the chromosomal stability, is an attractive cancer drug target. Now the accessibility to multiple crystal structures of Mps1 ligand complexes and inhibitors with known biological activities have accelerated the identification of novel molecular scaffolds by means of computer. In this paper, we developed the structure-based and li Read More

Five Lapatinib derivatives were designed by structurally modifying the side chain as well as the aniline substituent. The ELISA assay showed that the derivatives retained or even improved the inhibitory activity of Lapatinib against HER1/HER2. In vitro cytotoxicity assay revealed that the derivatives significantly inhibited the proliferation of the HER1/HER2-overexpressing cancer cells. Furthermore, molecular modeling study suggested Read More

Osteoarthritis is no doubt a difficult disease to manage. Targeted delivery of drugs to bone may not only enhance the treatment efficacy, but also reduces the quantity of drug administered. In this paper, we have synthesized two series of NSAID-Glu oligopeptide conjugates built up by the therapeutic moiety (naproxen and ibuprofen) and the targeting moieties (Glutamic oligopeptides) via amide linkage, as novel potential b Read More

Various bioisosteres of ethyl pyruvate (EP), where the oxygen atom in the ethoxy group was replaced by the corresponding bioisosteric atom such as carbon, nitrogen, and sulfur atoms, were synthesized and their inhibitory effects were tested for nitric oxide (NO) production and inducible NO synthase (iNOS) expression in lipopolysaccharide (LPS)-induced BV2 cells. The synthesized compounds generally revealed better activity Read More

In the present study, a series of dibenzoazepine triazole derivatives (24-39) were synthesized and evaluated for their in vitro bioactivities including antiglycation, antibacterial, DPPH radical scavenging, urease inhibition, antileishmanial and immunomodulatory activities. The compounds were found to be moderately active only against leishmania. Within this series, compound 26 was found to be the most active antileishaminal Read More

Some furan-based chalcone derivatives were synthesized via the Claisen-Schmidt condensation of 5-arylfurfural derivatives with 4'-cyanoacetophenone. The synthesized derivatives were investigated for their antimicrobial activity using a broth microdilution assay. Among these compounds, 1-(4-cyanophenyl)-3-[5-(4-nitrophenyl)-2-furyl]-2-propen-1-one (4) can be considered as the most promising antimicrobial a Read More