Synthesis, electrophilic substitution and structure-activity relationship studies of polycyclic aromatic compounds towards the development of anticancer agents.

Polycyclic aromatic hydrocarbons (PAH) are considered potentially carcinogenic. Substituted PAH derivatives, in contrast, may serve as anticancer agents, and as chemotherapeutics. This article presents a review of their use. Particular emphasis is placed on the synthesis of these new compounds, electrophilic substitution reactions and novel synthetic methodologies developed in our laboratory. Based on numerous reports and the data available, we believe that DNA-intercalating and membrane-interacting sites are the target for their effects.

Anticancer drug design using scaffolds of ß-lactams, sulfonamides, quinoline, quinoxaline and natural products. Drugs advances in clinical trials.

Eleven years after the start of a new millennium characterized by amazing scientific development, the cure for cancer remains a major challenge for humanity. In this regard, scientific efforts have focused on the search for new therapeutic targets that involve specific recognition and stop the spread of cancer cells, as well as the development of new therapeutic options that show greater specificity and better therapeutic efficacy. This review includes recent published literature about new anticancer drug design using scaffolds of ß-lactams, sulfonamides, quinoline, quinoxaline and natural products, and focuses on the structure-activity relationships of scaffolds that have been reported to potently inhibit cell growth of human tumor cell lines. It describes not only those synthetic or natural compounds aimed at specific molecular targets of cancer cells in vitro, but also compounds currently in clinical trials.

Deterioration of water quality of Surma river.

Surma River is polluted day by day by human activities, poor structured sewerage and drainage system, discharging industrial and household wastes. The charas (natural channels) are responsible for surface runoff conveyance from its urban catchments to the receiving Surma River. Water samples have been collected from a part of Surma River along different points and analyzed for various water quality parameters during dry and monsoon periods. Effects of industrial wastes, municipal sewage, and agricultural runoff on river water quality have been investigated. The study was conducted within the Chattak to Sunamganj portion of Surma River, which is significant due to the presence of two major industries--a paper mill and a cement factory. The other significant feature is the conveyors that travel from India to Chattak. The river was found to be highly turbid in the monsoon season. But BOD and fecal coliform concentration was found higher in the dry season. The water was found slightly acidic. The mean values of parameters were Conductivity 84-805 micros; DO: dry-5.52 mg/l, monsoon-5.72 mg/l; BOD: dry-1mg/l, monsoon-0.878 mg/l; Total Solid: dry-149.4 mg/l, monsoon-145.7 mg/l. In this study, an effort has been taken to investigate the status of concentration of phosphate (PO(-4)) and ammonia-nitrogen (NH4-N) at four entrance points of Malnichara to the city, Guali chara, Gaviar khal and Bolramer khal. Data has been collected from March-April and September-October of 2004. Concentrations have been measured using UV Spectrophotometer. Although the phosphate concentration has been found within the limit set by DOE for fishing, irrigation and recreational purposes, however ammonia-nitrogen has been found to exceed the limit.

Polycyclic aromatic compounds as anticancer agents: synthesis and biological evaluation of some chrysene derivatives.

Synthesis and biological evaluation of new chrysene derivatives aimed at the development of anticancer agents were carried out.

Polycyclic aromatic compounds as anticancer agents: structure-activity relationships of chrysene and pyrene derivatives.

A large number of diamides and diamines were synthesized using 6-amino chrysene and 1-amino pyrene as starting materials. A structure activity study with cis-platinum as internal control against animal and human tumor lines was carried out in vitro. This study indicated that the in vitro cytotoxicity toward these lines depends on the functionality present in the molecules. The diamino compounds were found to be more potent than the diamides, and these were equally active irrespective of the end heterocyclic group, whereas the activity of the diamides was strongly dependent on the terminal unit. In general, the diamides containing chrysene as the chromophore were more active than those with a pyrene ring. The size of the end heterocyclic ring, along with the nature of the spacer connecting the polycyclic ring to the heterocyclic ring, seemed to affect the biological activity in certain cell lines. Hemolysis experiments on a lead compound established that it had activities similar to those described for membrane-stabilizing agents. This agent also demonstrated the capacity to produce differentiation in leukemia cell lines.

Polycyclic aromatic compounds as anticancer agents: synthesis and biological evaluation of dibenzofluorene derivatives.

Highly regioselective electrophilic substitution of dibenzofluorene was achieved and the nitro derivative was transformed to a variety of new anticancer agents.