Synthesis and in vitro antiproliferative activity of novel (4-chloro- and 4-acyloxy-2-butynyl)thioquinolines

The series of new acetylenic thioquinolines containing propargyl, 4-chloro-2-butynyl, and 4-acyloxy-2-butynyl groups have been prepared and tested for antiproliferative activity in vitro against human [SW707 (colorectal adenocarcinoma), CCRF/CEM (leukemia), T47D (breast cancer)] and murine [P388 (leukemia), B16 (melanoma)] cancer lines. Most of the obtained compounds exhibited antiproliferative activity, especially compounds 8, 12, and 21 showed the ID50 values ranging from 0.4 to 3.8 μg/ml comparable to that of cisplatin used as reference compounds

Cultural and Strategic Factors in South Asian Nuclear Arms Control

Future efforts at arms control are shifting to LDCs. We believe future agreements is could look very different from their cold war predecessors because third world decision making processes are influenced by many unaddressed factors, ranging from culture to historical antagonism, in addition to strategic and technical concerns. Utilizing game theory as well as historical and cultural analysis, we examine likely possibilities for arms control agreements in South Asia as a case study, and then analyze the logic behind these possibilities. Our findings about the cultural mind set and political preferences of leaders and their constituents lead us toward a specific hypothesis about how these factors influence the decision making process, a direction for the future study of other regions

Contemporary analytical techniques reveal the secret composition of a 19th century Jerusalem Balsam

In 1719, Antonio Menzani di Cuna from the Saint Savior monastery published an alcoholic extract formula made from plant and herb resins under the name Jerusalem Balsam. The Balsam gained high popularity due to its remedial benefits. At the end of the 19 th century, Jerusalem Balsam produced by the hermit Johannes Treutler was found to be particularly popular. We analysed a sample of a valuable find coming from the last decade of the 19 th century, making it probably the oldest surviving Jerusalem Balsam in the world. The purpose of this work was to investigate the composition of the historical sample and to try to determine the origin of its components. This was achieved by comparing the profile of volatile compounds extracted from the balsam using HS-SPME technique with the profile characteristic for plant resins as classic ingredients of the Johannes Treutler formula. The use of two chromatographic columns of different polarity, as well as the transformation of the polar components of the sample into TMS derivatives, allowed to obtain new information on the historical composition of the Balsam. Also, it can be stated with high probability that plant resins were indeed used in the production of the Balsam as referred to in the original recipe of Johannes Treutler. We also discuss challenges in determining the original composition of the Balsam

Lodz City Tour: The Changing Nature of the Urban Restructuring of a Post-Socialist Industrial City

This paper describes the restructuring of Poland’s third-largest city, Lodz (Łódź). Once a thriving metropolitan hub of textile and clothing manufacturing, Lodz was confronted with the closure of its numerous factories in the early 1990s with Poland’s transition from a planned to a global market economy. The city suffered an abrupt and dramatic decline followed by a redefinition of its economic, spatial and social structures. The paper focuses on the major economic and spatial phenomena taking place in the city in the three decades after the economic collapse. Using an evolutionary approach, it identifies and discusses the gradual shift of Lodz’s restructuring. We claim that the restructuring initially involved mostly organic and spontaneous initiatives of dynamic local and non-local actors, with minor and circumstantial involvement from the local authorities. However, over time, the restructuring of Lodz has become influenced and driven by nationally and EU-set objectives and targeted urban policies, with urban and infrastructural projects as driving vehicles.Jakub Zasina’s portion of this work was supported by the National Science Centre in Poland (grant agreement no. 2016/23/N/HS4/03390)

Natural and synthetic 5,8-quinolinedione derivatives exhibited biological activity

The compounds produced by a living organisms are most commonly used as medicinal agents and starting materials to the preparation of new semi-synthetic derivatives. It is estimated that over 23% of currently used medicinal products are natural substances. Natural compounds and their semisynthetic derivatives are most often used in the treatment of cancer and the treatment of infectious diseases. One of the groups of compounds obtained from Gram-positive bacterium are 5,8-quinolinedione antibiotics, like: streptonigrin, lavendamycin and streptonigron. The all compounds exhibit high anticancer, antimicrobial and antiviral activity. Unfortunately due to high toxicity this alkaloids did not find place in the therapy. The mechanism of action depends on interaction of compounds with the nicotinamide quinone oxidoreductase 1 (NQO1). The 5,8-quinolinedione can be reduced by the NAD(P)H as a cofactor to form the semiquinone or hydroquinone intermediates. These compounds can react with oxygen yielding a regenerated 5,8-quinolinedione fragment and creating the hydroxyl radicals, which are ultimately responsible for the DNA strands cleavage. The structure–activity relationship study has shown that the most important part of the molecule is the 5,8-quinolinedione moiety. Furthermore, it was found, that the introduction of amine, hydroxyl or thiol substituents at position 6 or 7 of the 5,8-quinolinedione moiety results in an enhanced biological activity. A lot of synthetic derivatives of 5,8-quinolinediones which containing amine, alkoxyl and thiol groups at the C-6 or/and C-7 positions have been obtained during the last few years. Commonly this compounds are obtained in the reaction of 6,7-dichloro-5,8-quinolinedione with nucleophilic factor. Depending on the reaction conditions, mono- or di-substituted derivatives are obtained. Most of synthesized compounds exhibit high biological activity, like: anticancer, antibacterial, antiviral, anti-inflammatory