Medicinal Chemistry - Volume 12, Issue 7, 2016

Background: The Morita-Baylis-Hillman reaction is an organocatalyzed chemical transformation that allows access to small poly-functionalized molecules and has considerable synthetic potential and promising biological profiles. The Morita–Baylis–Hillman adducts (MBHA) are a new class of bioactive compounds and highlight its potentialities to the discovery of new cheaper and efficient drugs, e.g. as anti-Leishmania chagasi Read More

Background: The tumor pyruvate kinase M2 (PKM2) is involved in the glycolytic pathway of lung cancer and targeting this kinase has been observed to radiosensitize non-small cell lung cancer (NSCLC). Objective: An integration of in silico virtual screening and in vitro kinase assay was described to discover novel PKM2 inhibitors from a candidate library containing >400,000 commercially available compounds. Method: The metho Read More

A novel series of 2,4,6-trisubstituted 1,3,5-triazine derivatives bearing aryl hydrazone moiety were designed and synthesized under the guidance of scaffold hopping and bioisosterism from the autophagy inhibitor VLX600. The target compounds were evaluated for cytotoxicity against HT-29 by MTT assay with VLX600 as positive control. Then, ten potent target compounds (5c-5f, 5i-5r, 5s, 5t) were further evaluated against two c Read More

Background: Based on the biological significance of benzisoselenazolone and 1,3,4-thiadiazole, a series of novel 1,3,4-thiadiazole derivatives incorporating benzisoselenazolone scaffold were designed and synthesized with ebselen as a lead compound. Methods: Meanwhile, their in vitro antitumor activities were evaluated against SMMC-7721, MCF-7 and A549 human cancer cell lines by CCK-8 assay. Results: The prelimina Read More

Background: Cutaneous and invasive fungal infections are constant threats to human health that substantiate the need for the development of new efficacious and safe antimycotics. Methods: A series of N1-alkyl, N1-acyl and N1-sulfonyl derivatives of 4,6- dimethylisoxazolo[3,4-b]pyridin-3(1H)-one (1) were synthesized. The antimicrobial activities of title compounds against 21 pathogenic yeast-like fungal clinical isolates and 5 re Read More

Background: This paper describes the synthesis of three different subfamilies of cyclic imides: methylphtalimides, carboxyl acid phtalimides and itaconimides. Methods: Fifteen compounds (five of each sub-family) were obtained by the reaction of appropriated anhydrides and different aromatic amines, using the manual Topliss method. Their structures were confirmed by spectral data (IR and NMR). The antifungal activi Read More

Two new limonoids, named rubescins D-E (1-2) along with eight known compounds, including five havanensin type limonoids, TS1 (3), TS3 (4), rubescins A-C (5-7) and three known phytosterols, β-sitosterol, stigmasterol and its 3β-O-glucopyranoside derivative were isolated from the roots and stem bark of Trichilia rubescens, collected from Cameroon. The structures of the new compounds were determined by detailed anal Read More

Background: Since the anti-inflammatory activity of arachidonic acid derivatives was previously reported, we synthesized three new amide derivatives of arachidonic acid (AA-Ds) and tested their anti-inflammatory effects on an in vitro skin inflammation model. Aim of our study was to find derivatives of natural compounds able to down regulate inflammatory signal transduction pathway. Methods: Human keratinocytes Read More

Background: Synthesis of 7,7´-linked bicoumarins, 3,3´-linked bi(2-isopropyl)psoralens as well as 1H-1,2,3-triazole linked coumarin–2,3-dihydrofurocoumarin and furocoumarin–2,3-dihydrofurocoumarin hybrids was performed by two alternative pathways, either involving a catalyzed transformations of the ethynyl derivatives of plant coumarins – peucedanin or peuruthenicin. Objective and Methods: The Sonogashira r Read More

Background: Introducing new candidates for various biological targets is a prime characteristic of the present day medicinal research and development. Guanidines are the important bioactive compounds and are well recognized for their diverse biological activities, especially as anticancer, antimicrobial and antioxidant agents. Due to the favorable electronic properties of ferrocene like lipophilicity, redox activity, Read More