Thus, 1,2,3-triazole derivatives appear to represent a class of novel, biologically active ligands against histone deacetylases which deserve to be further evaluated in their applications in the cancer field.

2,4-Disubstituted thiophene derivatives were synthesized and assessed for antiinflammatory and anti-cancer activities by targeting two important enzymes of the arachidonic acid metabolism. Both lipoxygenase and cyclooxygenase enzymes play vital role in chronic inflammation and carcinogenesis. Previous studies have proved that COX-2 and 5-LOX are highly activated in various types of cancers; hence inhibition of these clinically important enzymes constitutes the essential criterion for the suppression of tumor progression and metastasis. Among the tested derivatives, 2d and 2g compounds emerged as potent inhibitors of lipoxygenase and cyclooxygenase enzymes. The potent inhibitor of cyclooxygenase was further tested for in vitro cytotoxicity on cervical cancer (HeLa) cells and in vivo tumor model studies using EAT bearing mice where 2-(3,4,5- trimethoxyphenyl)-4-(N-methylindol-3-yl) thiophene (2g) showed eloquent activity. Further, in silico modeling results confirmed the active catalytic ligand binding pockets, which is evident from higher atomic contact energy values of 2d and 2g than compared to standard drug. Thus, 2g may find better application in management of inflammation and in proapoptotic therapeutic engineering.

An efficient total synthesis of (+)-goniodiol was illustrated by using Carreira alkynylation and Sharpless asymmetric dihydroxylation as key steps.

The title compound, C21H19BrFN5O·0.5H2O, crystallizes as a hemihydrate with the water molecule located on a twofold rotation axis. The piperidine ring has a chair conformation, whereas the triazole and the benzisoxazole rings are planar (r.m.s. deviations = 0.006 and 0.009 Å, respectively). The N—C and C—C bonds connecting the triazole and benzisoxazole rings, respectively, to the piperidine ring lie in equatorial positions. In the crystal, molecules related by a twofold rotation axis are linkedviaO—H...N hydrogen bonds involving the water molecule and a pair of C—H...N hydrogen bonds forming dimers. The dimers are linkedviaa pair of C—H...F hydrogen bonds leading to the formation of chains propagating along [101].

Background: Indazoles are known for their anti-cancer properties. Objective: The current investigation was on the synthesis and evaluation of novel indazole derivatives for their anti-cancer properties. Method: A series of novel indazoles were synthesized and characterized by IR, NMR and LCMS. We performed cytotoxic studies for all synthesized compounds on different cell lines such as HeLa, MCF-7 and EAC using MTT assay. The lead compound was tested further for its anti-tumor and anti-angiogenic effect on EAT tumor model. Results: Amongst the series of compounds synthesized, compound KA8 showed potent antiproliferative effect against Hela, MCF-7 and EAC cell lines with IC50 values 10.4 to 11.5 and 13.5µM respectively. In addition, our compound KA8 significantly decreased the cell viability, body weight, ascites volume and it also showed superior survival ability of mice compared to control groups. Furthermore, it suppressed the formation of neovasculature in the peritoneum of EAT-bearing mice. Conclusion: The findings reveal that the lead compound KA8 possesses potent anti-tumor and anti-angiogenic properties thereby promising it to be developed as a novel anticancer agent with further mechanistic studies.