+ Resolve Article
+ Follow Us
Follow on FacebookFollow on Facebook
Follow on TwitterFollow on Twitter

+ Translate
+ Subscribe to Site Feed
GeoScience Most Shared ContentMost Shared Content

Design and synthesis of novel 5-aminosalicylate (5-ASA)-4-thiazolinone hybrid derivatives with promising antiproliferative activity

, : Design and synthesis of novel 5-aminosalicylate (5-ASA)-4-thiazolinone hybrid derivatives with promising antiproliferative activity. Bioorganic & Medicinal Chemistry Letters 26(7): 1647-1650

Two privileged pharmacophores were assembled in one molecular frame involving 5-aminosalicylate and 4-thiazolinones that can be found in different stereochemical features. The compounds were fully characterized and evaluated for antiproliferative activity against four human cancer cell lines and some are equipotent to doxorubicin with lower cytotoxicity to normal cells. The most interesting finding relates to compound 10, which shows an IC50 value of 70nM against MCF-7 cells, while the IC50 against human fibroblasts is 10μM. The results of this study indicate that the new compounds are optimal anti-cancer leading compounds and merit further studies to optimize their structure, detect their biotargets and in vivo activity.


PMID: 26947606

DOI: 10.1016/j.bmcl.2016.02.073

Other references

Vemana, K.; Sitaramaiah, K.; Naidu, P.D.; Reddy, K.S., 1999: Comparative efficacy of organic amendments and a nematicide on population dynamics of Tylenchorhynchus brevilineatus, microbial activity, groundnut pod disease and yield. The efficacy of different organic amendments on the population dynamics of plant parasitic nematodes including Tylenchorhynchus brevilineatus, microbial population (total fungi, bacteria, actinomycetes) and the pod disease severity of groundnut wa...

Coran, S.A.; Giannellini, V.; Furlanetto, S.; Bambagiotti Alberti, M.; Pinzauti, S., 2001: Improving gas chromatographic determination of residual solvents in pharmaceuticals by the combined use of headspace solid-phase microextraction and isotopic dilution. Cyclohexane and toluene were gas chromatographically determined via headspace solid-phase microextraction both in ketoprofen drug substance and ketoprofen capsules by a procedure relying on isotopic (ID), an analytical tool derived from mass spect...

Ledakowich, A., 1975: A unique malpractice decision. Medical Times 103(10): 147, 151-142, 155

Montserrat, VJ.; Diaz-Aranda, LM., 1989: Contribucion al conocimiento de los neuropteros de Castellon (Insecta, Neuropteroidea, Planipennia) (1). Mediterranea, 47-57 No. 11

Gool, J.Van, 1978: News from the Netherlands. L'article resume l'histoire recente des cooperatives de consommation aux Pays-Bas. Summary: The article summarizes the recent history of consumer cooperatives in the Netherlands.

Isenberg, S.F., 2003: Reimbursement basics. Ear, Nose, & Throat Journal 82(4): 260-260

Gavrilova, L.N.; Mikhailov, A.I.; Obukhova, G.P.; Khananashvili, M.M., 1975: Electro encephalographic correlates of a pathological inert motor reaction in dogs. Changes in the EEG were examined during the development of a pathological inert motor reaction in dogs with parts of the tongue brought out and electrodes implanted in the motor cortical area and limbic structures. The reaction was formed when com...

Christodoulou, G.E., 1969: On the geology of the Thivai-Paralimni area. Geological and Geophysical Research, 13: 1-54

Grubaugh, N.D.; Massey, A.; Shives, K.D.; Stenglein, M.D.; Ebel, G.D.; Beckham, J.David., 2016: West Nile Virus Population Structure, Injury, and Interferon-Stimulated Gene Expression in the Brain From a Fatal Case of Encephalitis. Background.  West Nile virus (WNV) infection in humans can result in severe, acute encephalitis typically involving subcortical gray matter brain regions. West Nile virus replication within specific human brain regions from a human case of acute...

K.S.imizu; K.G.toh; M.T.haya; F.S.gawa; H.O.ada; K.H.rumi, 1988: Histological study of atrioventricular node of the autopsied hearts. Journal of Electrocardiology 21(1): 1