The study highlights the current progress in the development of coumarin scaffolds for drug discovery as novel anticancer agents in metastatic breast cancer. Eight compounds, combining the coumarin core and five membered heterocycles (isoxazoles and thiazoles) in hydrazinyldiene- -chroman-2,4-diones, were characterized in terms of a potential antiproliferative effect on bone (SCP1833) and lung ...

A new series of imidazo[2,1-b]thiazole analogs containing a methyl sulfonyl COX-2 pharmacophore was synthesized and evaluated for their COX-2 inhibitory activity. According to in-vitro COX-1/COX-2 inhibition data, all compounds (6a-g) were selective inhibitors of COX-2 isoenzyme with IC50 values in the highly potent 0.08-0.16 mM range. These results indicated that both potency and selectivity o...

A new series of imidazo[2,1-b]thiazole analogs containing a methyl sulfonyl COX-2 pharmacophore was synthesized and evaluated for their COX-2 inhibitory activity. According to in-vitro COX-1/COX-2 inhibition data, all compounds (6a-g) were selective inhibitors of COX-2 isoenzyme with IC50 values in the highly potent 0.08-0.16 mM range. These results indicated that both potency and selectivity o...

The synthesis and biological evaluation of 6,7-bis(hydroxymethyl)-1H,3H-pyrrolo[1,2-c]thiazoles as anticancer agents against MCF7 breast cancer cell lines is reported. The design of the new compounds has been guided considering (3R)-6,7-bis(hydroxymethyl)-5-methyl-3-phenyl-1H,3H-pyrrolo[1,2-c]thiazole as the lead compound due to its good performance against MCF7 breast cancer cell lines (IC(50)...

Background and aim: Leishmaniasis is a zoonotic disease with wide clinical diversity caused by protozoan parasite belonging to the genus of Leishmania. Treatment of human leishmaniases are still based on pentavalent antimonials but their toxicity and emerging resistance are problematic. This study was performed to assess the effect of Mimosa tenuiflora extract on L. tropica promastigotes ...

We have designed and synthesized novel bis-thiazole derivative. A 4-[bis(thiazol-2-ylamino)methyl]phenol was efficiently prepared in 71% yield by the reaction of 2-aminothiazole with 4-hydroxybenzaldehyde ethanol for 24 h. The structure newly obtained compound characterized 1H, 13C NMR mass spectrometry. Bis-thiazole derivative exhibits high tyrosinase inhibitory activity an IC50 value 29.71 μM...

BACKGROUND Many heterocyclic compounds containing thiazole or 1,3,4-thiadiazole ring in their skeletons have been reported to possess various pharmacological activities especially anticancer activities. RESULTS 4-Methyl-2-phenylthiazole-5-carbohydrazide (2) was used as a synthon to prepare 2-(4-methyl-2-phenylthiazole-5-carbonyl)-N-phenylhydrazinecarbothioamide (3) and 2-(2-(4-methyl-2-phenyl...