New Library of Iodo-Quinoline Derivatives Obtained by an Alternative Synthetic Pathway and Their Antimicrobial Activity.

6-Iodo-substituted carboxy-quinolines were obtained using a one-pot, three-component method with trifluoroacetic acid as a catalyst under acidic conditions. Iodo-aniline, pyruvic acid and 22 phenyl-substituted aldehydes (we varied the type and number of radicals) or O-heterocycles, resulting in different electronic effects, were the starting components. This approach offers advantages such as rapid response times, cost-effective catalysts, high product yields and efficient purification procedures. A comprehensive investigation was conducted to examine the impact of aldehyde structure on the synthesis pathway. A library of compounds was obtained and characterized by FT-IR, MS, 1H NMR and 13C NMR spectroscopy and single-ray crystal diffractometry. Their antimicrobial activity against S. epidermidis, K. pneumonie and C. parapsilosis was tested in vitro. The effect of iodo-quinoline derivatives on microbial adhesion, the initial stage of microbial biofilm development, was also investigated. This study suggests that carboxy-quinoline derivatives bearing an iodine atom are interesting scaffolds for the development of novel antimicrobial agents.

Therapeutic Management of Malignant Wounds: An Update.

OPINION STATEMENT: Malignant fungating wounds (MFW) are severe skin conditions generating tremendous distress in oncological patients with advanced cancer stages because of pain, malodor, exudation, pruritus, inflammation, edema, and bleeding. The classical therapeutic approaches such as surgery, opioids, antimicrobials, and application of different wound dressings are failing in handling pain, odor, and infection control, thus urgently requiring the development of alternative strategies. The aim of this review was to provide an update on the current therapeutic strategies and the perspectives on developing novel alternatives for better malignant wound management. The last decade screened literature evidenced an increasing interest in developing natural treatment alternatives based on beehive, plant extracts, pure vegetal compounds, and bacteriocins. Promising therapeutics can also be envisaged by involving nanotechnology due to either intrinsic biological activities or drug delivery properties of nanomaterials. Despite recent progress in the field of malignant wound care, the literature is still mainly based on in vitro and in vivo studies on small animal models, while the case reports and clinical trials (less than 10 and only one providing public results) remain scarce. Some innovative treatment approaches are used in clinical practice without prior extensive testing in fungating wound patients. Extensive research is urgently needed to fill this knowledge gap and translate the identified promising therapeutic approaches to more advanced testing stages toward creating multidimensional wound care strategies.

Structural, Electrical and Optical Properties of Pyrrolo[1,2-i][1,7] Phenanthroline-Based Organic Semiconductors.

This work reports a study on structural, electrical and optical properties of some recently synthesized pyrrolo[1,2-i][1,7] phenanthrolines derivatives in thin films. The thin films were deposited onto glass substrates by spin coating technique, using chloroform as solvent. The obtained films exhibited a polycrystalline structure with an n-type semiconductor behavior after heat treatment in the temperature range 293-543 K, specific to each sample. The thermal activation energy lies between 0.68 and 0.78 eV, while the direct optical band gap values were found in the range 4.17-4.24 eV. The electrical and optical properties of the investigated organic semiconductor films were discussed in relation to microstructural properties, determined by the molecular structure. The investigated organic compounds are promising for applications in organic optoelectronics and nanoelectronics.

Cytotoxic substituted indolizines as new colchicine site tubulin polymerisation inhibitors.

A potential microtubule destabilising series of new indolizine derivatives was synthesised and tested for their anticancer activity against a panel of 60 human cancer cell lines. Compounds 11a, 11b, 15a, and 15j showed a broad spectrum of growth inhibitory activity against cancer cell lines representing leukaemia, melanoma and cancer of lung, colon, central nervous system, ovary, kidney, breast, and prostate. Among them, compound 11a was distinguishable by its excellent cytostatic activity, showing GI50 values in the range of 10-100 nM on 43 cell lines. The less potent compounds 15a and 15j in terms of GI50 values showed a high cytotoxic effect against tested colon cancer, CNS cancer, renal cancer and melanoma cell lines and only on few cell lines from other types of cancer. In vitro assaying revealed tubulin polymerisation inhibition by all active compounds. Molecular docking showed good complementarity of active compounds with the colchicine binding site of tubulin.

Design, Synthesis, Molecular Modelling and Anticancer Activities of New Fused Phenanthrolines.

Three series of fused pyrrolophenanthroline derivatives were designed as analogues of phenstatin and synthesized in two steps starting with 1,7-phenanthroline, 4,7-phenanthroline and 1,10-phenanthroline, respectively. Two (Compounds 8a and 11c) of the four compounds tested against a panel of sixty human cancer cell lines of the National Cancer Institute (NCI) exhibited significant growth inhibition activity on several cell lines. Compound 11c showed a broad spectrum in terms of antiproliferative efficacy with GI50 values in the range of 0.296 to 250 µM. Molecular docking studies indicated that Compounds 8a and 11c are accommodated in the colchicine binding site of tubulin in two different ways.