Effect of Benzothiazole based conjugates in causing apoptosis by Regulating p53, PTEN and MAP Kinase proteins affecting miR-195a and miR-101-1

<p>Abstract</p> <p>Background</p> <p>Hepatocellular carcinoma (HCC) accounts for majority of liver cancers and is the leading cause of cancer related death in Asia. Like any other cancer, HCC develops when there is a mutation to the cellular machinery that causes the cell to replicate at a higher rate and results in the loss of apoptosis. Therefore, a delicate balance between the expression of various genes involved in proliferation and apoptosis decide the ultimate fate of the cell to undergo rapid proliferation (cancer) or cell death.</p> <p>Results</p> <p>The benzothiazole based compounds exhibited effective cytotoxicity at 4 μM concentration and have shown G1 cell cycle arrest with decrease in levels of G1 cell cycle proteins such as cyclin D1 and Skp2. Involvement of tumour suppressor proteins such as PTEN and p53 was studied. Interestingly these compounds displayed decrease in the phosphorylated forms of AKT, p38 MAPK and ERK1/2 which play a vital role in cell proliferation. Compounds have exhibited strong and significant effect on the expression of micro RNAs such as miR-195a & miR-101-1 which regulate hepatic cell proliferation.</p> <p>Conclusions</p> <p>The cell cycle arrest and apoptotic inducing nature of these compounds was revealed by FACS, BrdU cell proliferation and tunel assays. Compounds affected both tumour suppressor proteins as well as proteins that are involved in active cell proliferation. Micro RNAs whose target is Cyclin D1 such as miR-195a and miR-101-1 that is required for growth of hepatoma cells was drastically affected. These compounds caused apoptosis by activating caspase-3 and PARP.</p

Europium triflate: An efficient, cost-effective and recyclable solid acid catalyst for highly chemoselective allylation of aldehydes

1774-1778Aldehydes undergo smooth nucleophilic addition with allyl-n-tributylstannane in the presence of europium triflate under extremely mild reaction conditions to afford the corresponding homoallylic alcohols in excellent yields with high chemoselectivity. The catalyst can be recovered by simple filtration and can be recycled in subsequent reactions

Synthesis of novel benzothiozole and benzisoxazole functionalized unsymmetrical alkanes and study of their antimicrobial activity

996-1000Novel unsymmetrical alkanes 4 and 5 have been independently synthesized in single pot from 2-amino 5 / 6-hydroxybenzothiazole, 6-hydroxy-3-methyl-1,2-benzisoxazole and different dihaloalkanes [X-(CH2)n-X]. The compounds 4 and 5 have been screened for antimicrobial activity and some of them have been found to show promising activity