904912-40-9Relevant academic research and scientific papers
Antitumor agents. 250. Design and synthesis of new curcumin analogues as potential anti-prostate cancer agents
Lin, Li,Shi, Qian,Nyarko, Alexander K.,Bastow, Kenneth F.,Wu, Chin-Chung,Su, Ching-Yuan,Shih, Charles C.-Y.,Lee, Kuo-Hsiung
, p. 3963 - 3972 (2006)
In a continuing study of curcumin analogues as potential drug candidates to treat prostate cancer at both androgen-dependent and androgen-refractory stages, we designed and synthesized over 40 new analogues classified into four series: monophenyl analogues (series A), heterocycle-containing analogues (series B), analogues bearing various substituents on the phenyl rings (series C), and analogues with various linkers (series D). These new compounds were tested for cytotoxicity against two human prostate cancer cell lines, androgen-dependent LNCaP and androgen-independent PC-3. Antiandrogenic activity was also evaluated in LNCaP cells and PC-3 cells transfected with wild-type androgen receptor. Ten compounds possessed potent cytotoxicity against both LNCaP and PC-3 cells, seven only against LNCaP, and one solely against PC-3. This study established an advanced structure-activity relationship (SAR), and these correlations will guide the further design of new curcumin analogues with better anti-prostate cancer activity.
A comparative study on the antioxidant properties of tetrahydrocurcuminoids and curcuminoids
Portes, Elise,Gardrat, Christian,Castellan, Alain
, p. 9092 - 9099 (2008/02/10)
Several curcuminoids and tetrahydrocurcuminoids (THCs), bearing various hydroxyl and/or methoxy groups on their benzene rings, have been synthesized to study their antioxidant and hydrogen donating capacities using the DPPH method at 25 °C in methanol. The results show that the tetrahydrocurcuminoids are in general much more efficient than their curcuminoid analogs if they include a phenol group in meta- or para-position of the linking chain and a neighboring phenol or methoxy group. This efficiency gain of THCs by comparison to curcuminoids was attributed to the presence of benzylic hydrogens involved in the oxidation process of these compounds and not to the beta-diketone moiety in the chain.
Synthesis of some curcumin derivatives and their antiinflammatory activity
Nurfina, A. N.,Reksohadiprodjo, M. S.,Timmerman, H.,Jenie, U. A.,Sugiyanto, D.,Goot, H. van der
, p. 320 - 328 (2007/10/03)
Curcumin is not only a frequently used food additive, but it is also a well-known constituent of Indonesian traditional medicines.Several beneficial effects are ascribed to curcumin, eg, its antiinflammatory properties.In order to study the antiinflammatory activity, a series of curcumin derivatives were prepared and the inhibition of the carrageenin-induced oedema by these compounds was investigated.It appeared that the para hydroxy groups in curcumin are important for antiinflammatory activity.This activity is enhanced when, in combination with the para hydroxy groups, the meta positions ore accupied with alkyl groups.Since the methyl derivatives are more active than the corresponding ethyl and tert-butyl derivatives, it is suggested that sterical hindrance is involved. - Keywords: curcumin/ antiinflammatory activity/ carrageenin-induced oedenoma.
