Synthesis of novel 4,6-disubstituted quinazoline derivatives, their anti-inflammatory and anti-cancer activity (cytotoxic) against U937 leukemia cell lines.

In view of the link between use of NSAIDs and altered cancer incidence and a growing evidence of COX-II implication in angiogenesis, a novel series of 4,6-disubstituted quinazoline derivatives have been synthesized starting from anthranilic acid derivatives 1 through conventional methods. Initially acylation followed by cyclisation to obtain benz-oxazinones 2 which on further treatment with ammonia yielded the crucial intermediate, 2-substituted benzamide (3). The products were subsequently cyclised to obtain quinazolones 4, chlorinated 5, then hooked to various optically pure alpha-amino acids to have 4,6-disubstituted quinazoline derivatives 6. All the derivatives 6 are screened for anti-inflammatory and anti-cancer activity against U937 leukemia cell lines. Some of the compounds exhibited promising anti-cancer activity with reference to standard drug Etoposide.

Petrosia testudinaria as a biomarker for metal contamination at Gulf of Mannar, southeast coast of India.

Coastal marine ecosystems in many parts of the world are under unrelenting stress caused by urban development, pollutants and other ecological impacts such as building of infrastructure, land reclamation for port and industrial development, habitat modification, tourism and recreational activities. The present work is a first extensive field study using the marine sponge, Petrosia testudinaria as a biomarker to detect heavy metal pollution between near and off shore environment of 'Gulf of Mannar', India. Sponges were collected from near shore (0.5-1 km) and offshore (5-7 km), locations and their metal concentrations were determined by inductively coupled plasma-mass spectrometry (ICPMS). Our results show that the near shore sponge accumulated greater concentrations of heavy metals (Al, Fe, Mn, As, Ni, Co, Cu, Se) ranging from 0.13 to 64 times higher concentration than the sponges located away from the shore. The results indicate that the accumulated metals alter the macromolecule composition (sugars, proteins and lipids) in near shore sponges. Frequent monitoring is necessary to assess the eco-health of the marine environment by choosing bioindicator species like sponges, which provide accurate, reliable measurement of environmental quality.

Sublethal effects of monocrotophos on locomotor behavior and gill architecture of the mosquito fish, Gambusia affinis.

Subacute studies of monocrotophos [Dimethyl (E)-1-methyl-2-(methyl-carbamoyl) vinyl phosphate] on mosquito fish, Gambusia affinis, were carried out in vivo for 24 days to assess the locomotor behavior, structural integrity of gill, and targeted enzyme acetylcholinesterase (AChE, EC: 3.1.1.7) interactions. Monocrotophos (MCP) can be rated as moderately toxic to G. affinis, with a median lethal concentration (LC(50)) of 20.49 +/- 2.45 mgL(-1). The fish exposed to sublethal concentration of LC(10) (7.74 mgL(-1)) were under stress and altered their locomotor behavior, such as distance traveled per unit time (m min(-1)) and swimming speed (cm sec(-1)) with respect to the length of exposure. Inhibition in the activity of brain AChE and deformities in the primary and secondary lamellae of gill may have resulted in failure of exchange of gases. The maximum inhibition of 95% of AChE activity was observed on days 20 and 24. Morphological aberrations in the gills were also studied during exposure to the sublethal concentration of monocrotophos for a period ranging from 8 to 24 days. The extent of damage in gill was dependent on the duration of exposure. The findings revealed that inhibition in brain AChE activity and structural alteration in gill were responsible for altering the locomotor behavior of exposed fish.