No abstract

In a search of new compounds active against cancer, synthesis of a series of C-5 curcumin analogues was carried out. The new compounds demonstrated good cytotoxicity against chronic myeloid leukemia (KBM5) and colon cancer (HCT116) cell lines. Further, these compounds were found to have better potential to inhibit TNF-α-induced NF-κB activation in comparison to curcumin, which show their potential to act as anti-inflammatory agents. Some compounds were found to show higher cytotoxicity against cancer cell lines in comparison to curcumin used as standard.

In recent times, the novel concept of generating hybrid molecules by pharmacophoric hybridisation approach is fast becoming an alternative to other existing strategies of drug development. These hybrids also known as 'dual drugs' or 'double drugs' are especially found to be effective in overcoming drug resistance problems. Towards this end, a lot of effort has been put for generating 4-aminoquinoline based hybrid molecules as next generation antimalarial drugs effective in malarial chemotherapy. This short review deals about the recent advances carried in the field of 4-aminoquinoline based molecular hybrids as potential antimalarial agents. It also presents a brief and simplified story on the development of 4-aminoquinolines as a mainstay in malarial research programmes.

Um grande número de reações de formação de ligações carbono-carbono (tais como: acoplamentos de Heck, Suzuki, Stille, Negishi e Sonogashira, entre outros) é facilitado pela catálise com compostos de paládio. Neste artigo de revisão, apresentamos uma visão detalhada e compreensiva da literatura sobre a versatilidade do uso de líquidos iônicos em conjunto com paládio em vários tipos de reações.A number of carbon-carbon bond forming reactions in organic chemistry (such as the Heck, Suzuki, Stille, Negishi, Sonogashira coupling etc) are facilitated by catalysis with palladium compounds. An attempt has been made to present a detailed and comprehensive literature collection about the versatility of ionic liquid in conjunction with palladium for various types of reactions.

Trioxane based compounds such as artemisinin and its synthetic and semi-synthetic analogues constitute promising class of antimalarial agents. The pharmaceutical development of artemisinin was started in 1971 after the isolation from Chinese medicinal plant Artemisia annua and this compound has drawn much attention from medical chemist and pharmacologist worldwide. Researchers from across the globe have independently and collaboratively conducted various studies on the artemisinin system in an attempt to identify lead molecules for malaria chemotherapy. This systematic study led to the discovery of artemether, arteether, dihydroartemisinin, and sodium artesunate which are being used as antimalarial drug for the treatment of Plasmodium falciparum related infections. These studies also revealed that the trioxane bridge is essential for the antimalarial activity of this class of compounds. Another class of structurally simple peroxides that emerged from these studies was the 1,2,4,5-tetraoxanes. Some of the tetraoxane based compounds have shown promising antimalarial potential, and much of work has been done on this type of compound in recent years. Apart from their antimalarial activity, these classes of compounds have also shown promising anticancer and antibacterial activity. To this end, an attempt has been made to describe the medicinal potential of trioxane and tetraoxane-based compounds. Literature from 1999 has been critically reviewed and an attempt has been made to discuss structure activity relationship study among the series of trioxane and tetraoxane based compounds.